Cambridge Healthtech Institute's 12th Annual Discovery on Target will showcase current and emerging “hot” targets for the pharmaceutical industry, October 8 – 10, 2014 in Boston, MA. Spanning three days, the meeting will bring together more than 900 global attendees, including scientists/technologists, executives, directors, and managers from biopharma, academic, and healthcare organizations. In 2014 the event is comprised of 14 conference tracks which include Epigenetic Readers, Ubiquitin Proteasome, Big Data Discovery, GPCR Drug Discovery, RNAi-Screens-Functional-Genomics, PPI Targets, Protein-Targets, Histone-Methyltransferases-Demethylases, Drug Transporters, Maximizing Efficiency, GPCR Therapeutics, Genomics Screening, Cancer Metabolism and Membrane Production. The 2014 event will offer 200+ scientific presentations across 14 conference tracks, 1 Symposium and 15 conference short courses, 40+ interactive breakout discussion groups, an exhibit hall of 40+ companies, and dedicated poster viewing and networking sessions.
New Drug Discovery And Development (part-2)swatisejwani
The document discusses the steps involved in preclinical trials for new drug development. Preclinical trials involve laboratory and animal testing to evaluate safety and efficacy before human testing. Key steps include: identifying a drug target and developing a bioassay; screening the drug in the bioassay; establishing effective and toxic doses; filing for Investigational New Drug approval with the FDA; and conducting various studies like toxicity, pharmacokinetic, and animal model testing under Good Laboratory Practice standards. The goal of preclinical trials is to obtain sufficient safety and efficacy data to justify moving a drug into clinical trials with human subjects.
New drug discovery and development (Part - 1)swatisejwani
The document discusses the process of new drug discovery and development. It begins with definitions of key terms like drug, discovery phase, and development phase. It then describes the various stages of drug discovery and development, including target identification, lead identification, lead optimization, preclinical testing, clinical trials, and regulatory approval. The process takes 12-15 years and costs $900 million to $2 billion on average due to the need to test thousands of potential drug candidates. Characterization, formulation, preclinical safety testing, and clinical trials are described as important steps to develop a new drug for patients.
This document discusses various aspects of drug discovery and pharmacogenomics. It defines drugs and the drug discovery process, which involves identifying lead compounds and developing drugs. It also describes computer-aided drug design, pharmacogenomics as the study of an individual's genetic makeup and response to drugs, and antisense technology for treating disease. The goal is to develop personalized medicine by optimizing drug therapy based on a patient's genotype.
OVERVIEW OF MODERN DRUG DISCOVERY PROCESSSweety gupta
The document provides an overview of the modern drug discovery process, which involves 5 main steps:
1) Target identification and validation to find the molecular structures involved in the disease.
2) Hit identification and validation to find small molecule leads that have the desired effect on the targets.
3) Moving from a hit to a lead by refining hits into more selective compounds.
4) Lead optimization to improve properties and address any deficiencies while maintaining desired effects.
5) Late lead optimization to further assess safety before clinical trials.
Modern drug discovery is an expensive process that can cost over $1 billion on average due to large investments required. Bioinformatics and genomic/proteomic technologies help accelerate the process and reduce
Drug discovery clinical evaluation of new drugsKedar Bandekar
The document discusses the process of new drug development from initial idea to market launch. It takes 12-15 years and over $1 billion. The process involves identifying a biological target, screening compounds to find hits, optimizing hits to develop leads, and conducting preclinical and clinical trials. Key steps include target identification and validation, high-throughput screening to find initial hits, hit-to-lead and lead optimization processes to improve properties, and progression through preclinical and clinical phases of drug development. Characteristics of ideal lead compounds include high target affinity and selectivity, efficacy, appropriate physicochemical properties, and favorable ADME profile.
Drug discovery involves identifying candidate medications through screening chemical libraries, natural products, or virtual screening. It is a lengthy and expensive process to bring a new drug to market. Traditionally, drugs were discovered from plants or microbes, and modern techniques involve high-throughput screening of large compound libraries against biological targets of interest. Hits are then optimized for properties like potency, selectivity, stability, and bioavailability. Once a lead compound is identified, drug development studies are conducted prior to clinical trials to seek regulatory approval. Natural products continue to provide useful structures for drug design despite advances in synthesis and screening methods.
Introduction to the drug discovery processThanh Truong
This document discusses the drug discovery process from target identification through FDA approval. It describes methods used for target identification such as genomics, bioinformatics, and proteomics. The stages of lead identification through high-throughput screening and structure-based drug design are outlined. Key aspects of lead optimization like characterizing potency, efficacy, pharmacokinetics, and toxicity are summarized. Details are provided on preclinical and clinical trial phases from Phase 0 through Phase IV post-marketing surveillance. Factors contributing to the declining drug approval rate like increased safety demands are noted. The high costs and failure rates associated with drug development are highlighted.
Presentation by MicroConstants at BIOCOM CRO event May 2013: Virtual Drug Dev...BIOCOMCRO
May 2013
8-10am
Location: BIOCOM
Speaker(s):
Joining the presenters for a follow-on panel discussion will be: Jennifer Spinella, Vice President, Regulatory Affairs & Quality Assurance at Rare Disease Therapeutics Greg Ruppert, Sr. Study Director and Director of Sales for MPI Research Richard Lin, CEO of Explora Biolabs.
New Drug Discovery And Development (part-2)swatisejwani
The document discusses the steps involved in preclinical trials for new drug development. Preclinical trials involve laboratory and animal testing to evaluate safety and efficacy before human testing. Key steps include: identifying a drug target and developing a bioassay; screening the drug in the bioassay; establishing effective and toxic doses; filing for Investigational New Drug approval with the FDA; and conducting various studies like toxicity, pharmacokinetic, and animal model testing under Good Laboratory Practice standards. The goal of preclinical trials is to obtain sufficient safety and efficacy data to justify moving a drug into clinical trials with human subjects.
New drug discovery and development (Part - 1)swatisejwani
The document discusses the process of new drug discovery and development. It begins with definitions of key terms like drug, discovery phase, and development phase. It then describes the various stages of drug discovery and development, including target identification, lead identification, lead optimization, preclinical testing, clinical trials, and regulatory approval. The process takes 12-15 years and costs $900 million to $2 billion on average due to the need to test thousands of potential drug candidates. Characterization, formulation, preclinical safety testing, and clinical trials are described as important steps to develop a new drug for patients.
This document discusses various aspects of drug discovery and pharmacogenomics. It defines drugs and the drug discovery process, which involves identifying lead compounds and developing drugs. It also describes computer-aided drug design, pharmacogenomics as the study of an individual's genetic makeup and response to drugs, and antisense technology for treating disease. The goal is to develop personalized medicine by optimizing drug therapy based on a patient's genotype.
OVERVIEW OF MODERN DRUG DISCOVERY PROCESSSweety gupta
The document provides an overview of the modern drug discovery process, which involves 5 main steps:
1) Target identification and validation to find the molecular structures involved in the disease.
2) Hit identification and validation to find small molecule leads that have the desired effect on the targets.
3) Moving from a hit to a lead by refining hits into more selective compounds.
4) Lead optimization to improve properties and address any deficiencies while maintaining desired effects.
5) Late lead optimization to further assess safety before clinical trials.
Modern drug discovery is an expensive process that can cost over $1 billion on average due to large investments required. Bioinformatics and genomic/proteomic technologies help accelerate the process and reduce
Drug discovery clinical evaluation of new drugsKedar Bandekar
The document discusses the process of new drug development from initial idea to market launch. It takes 12-15 years and over $1 billion. The process involves identifying a biological target, screening compounds to find hits, optimizing hits to develop leads, and conducting preclinical and clinical trials. Key steps include target identification and validation, high-throughput screening to find initial hits, hit-to-lead and lead optimization processes to improve properties, and progression through preclinical and clinical phases of drug development. Characteristics of ideal lead compounds include high target affinity and selectivity, efficacy, appropriate physicochemical properties, and favorable ADME profile.
Drug discovery involves identifying candidate medications through screening chemical libraries, natural products, or virtual screening. It is a lengthy and expensive process to bring a new drug to market. Traditionally, drugs were discovered from plants or microbes, and modern techniques involve high-throughput screening of large compound libraries against biological targets of interest. Hits are then optimized for properties like potency, selectivity, stability, and bioavailability. Once a lead compound is identified, drug development studies are conducted prior to clinical trials to seek regulatory approval. Natural products continue to provide useful structures for drug design despite advances in synthesis and screening methods.
Introduction to the drug discovery processThanh Truong
This document discusses the drug discovery process from target identification through FDA approval. It describes methods used for target identification such as genomics, bioinformatics, and proteomics. The stages of lead identification through high-throughput screening and structure-based drug design are outlined. Key aspects of lead optimization like characterizing potency, efficacy, pharmacokinetics, and toxicity are summarized. Details are provided on preclinical and clinical trial phases from Phase 0 through Phase IV post-marketing surveillance. Factors contributing to the declining drug approval rate like increased safety demands are noted. The high costs and failure rates associated with drug development are highlighted.
Presentation by MicroConstants at BIOCOM CRO event May 2013: Virtual Drug Dev...BIOCOMCRO
May 2013
8-10am
Location: BIOCOM
Speaker(s):
Joining the presenters for a follow-on panel discussion will be: Jennifer Spinella, Vice President, Regulatory Affairs & Quality Assurance at Rare Disease Therapeutics Greg Ruppert, Sr. Study Director and Director of Sales for MPI Research Richard Lin, CEO of Explora Biolabs.
Basics of Drug Discovery and DevelopmentJhony Sheik
The document outlines the process of drug discovery and development from initial screening of chemicals to determine biological activity through clinical trials and regulatory approval. It notes that of 10,000 initially screened chemicals, only 1 may reach the market place due to the high costs, risks and regulatory hurdles. The key stages discussed are preclinical testing in animals, filing an Investigational New Drug application for human trials, conducting clinical trials in four phases, filing a New Drug Application providing trial results for regulatory review and approval, large-scale manufacturing, and filing an Abbreviated New Drug Application for generic approvals relying on previously approved drugs.
The document discusses the principles and process of drug discovery, which involves identifying a target, screening compounds, preclinical testing, and clinical trials. It takes an average of 12-15 years and $600-800 million to bring a new drug to market. Key stages include target identification and validation, screening compounds through various techniques, preclinical studies in animals, and clinical trials in phases I-III to test safety and efficacy in humans. Novel approaches like microarrays, peptidomimetics, pharmacogenomics, and cheminformatics can aid the drug discovery process.
Drug discovery and development is a long, expensive, and complex process that takes an average of 10-12 years and $800 million to $1.7 billion. It involves identifying candidate drugs through methods like molecular designing, screening, and serendipity. Only one in 5000 compounds makes it through preclinical and clinical testing to be approved. The process includes target selection and validation, lead discovery and optimization, and drug development to satisfy regulatory requirements before a new drug can be approved and marketed.
clinical and preclinical approaches to drug discovery.Here we mainly deals with preclinical approaches, ie. Pharmacological approach and toxicological approach
Drug discovery challenges and different discovery approachesHitesh Soni
The document discusses several challenges in drug discovery and different discovery approaches. It outlines issues with the traditional high-throughput screening approach such as low success rates. It then describes alternative approaches like considering transient binding drugs that interact weakly with multiple targets, leveraging natural products as drug leads, and exploring a multi-target drug discovery strategy to address complex diseases involving multiple molecular dysfunctions.
The document provides an overview of the modern drug discovery process, focusing on lead identification and lead optimization. It discusses how lead compounds are initially identified through screening compound libraries or structure-based drug design. These leads are then optimized through chemical modifications to improve properties like efficacy, potency, pharmacokinetics and toxicity profile. The goal is to develop compounds suitable for preclinical and clinical testing towards becoming an approved drug. Methods for lead optimization include modifying functional groups, exploring structure-activity relationships, and altering aspects like stereochemistry.
Drug discovery By Neelima Sharma WCC chennai,neelima.sharma60@gmail.comNeelima Sharma
The document provides an overview of the drug discovery process, including the need for new drugs, approaches to discovery, and changes over time. It discusses target identification, validation, lead identification, optimization, and preclinical pharmacology/toxicology. The phases of clinical trials are also summarized, including Phase I safety trials in healthy volunteers, Phase II therapeutic exploration trials, and large Phase III randomized controlled trials. The roles of various parties in clinical trials are also outlined.
Drug development process and clinical trial for UGsSameerKhasbage
This document summarizes the process of drug development from discovery through clinical trials and approval. It discusses the main goals and requirements of each phase of clinical trials: Phase I focuses on safety and dosing in healthy volunteers, Phase II evaluates efficacy and side effects in patients, Phase III tests efficacy versus existing treatments in hundreds to thousands of patients, and Phase IV monitors long-term safety and efficacy after approval and marketing. The overall process from discovery to approval takes 10-15 years and costs over $2 billion on average.
The document discusses lead identification in drug development. It defines a lead compound as one that shows desired pharmaceutical activity and could potentially be developed into a drug. The document outlines the content to be presented, including an introduction to lead identification, what a lead is, properties of leads, and methods for identifying leads. Key methods discussed are random screening, non-random screening, high-throughput screening, and structure-based drug design.
The document summarizes the principles of drug discovery, including the following key points:
1) Drug discovery is a lengthy, expensive, and inefficient process involving target identification, screening, preclinical testing, and clinical trials that can take over 10 years from initial compound to approved drug.
2) Natural products, especially from plants, microbes, and marine organisms, have historically been an important source of leads for drug discovery due to their chemical diversity.
3) The modern drug discovery process involves high-throughput screening of large libraries of synthetic compounds and natural products to identify initial hits, which are then optimized in the hit-to-lead phase through medicinal chemistry and further testing.
This document provides an overview of careers in drug discovery and development. It discusses the multi-stage process of discovering new drugs, from identifying drug targets through clinical trials and regulatory approval. The document notes that drug development is a highly time-intensive and costly process involving many disciplines. It also aims to dispel common myths about careers in the pharmaceutical industry, emphasizing that industry scientists have opportunities for publication, innovation, and interesting work.
The document summarizes the key events in the discovery and development of penicillin. Alexander Fleming first discovered penicillin in 1928 after noticing bacteria-killing properties of the Penicillium mold in one of his petri dishes. However, he was not able to purify or characterize penicillin at the time. In the 1940s, a team at Oxford led by Howard Florey and Ernst Chain managed to purify and mass produce penicillin, paving the way for clinical trials. The first successful human trials demonstrated penicillin's ability to cure bacterial infections. By the mid-1940s, large-scale production was established. Fleming, Florey and Chain received the 1945 Nobel Prize for their discoveries. Over time, resistance
This document discusses drug discovery and the process of identifying potential new drug targets. It outlines the need for drug discovery to develop treatments for diseases without existing therapies. The key steps in drug discovery include target identification using genomics and proteomics to study the genome and map protein-protein interactions, as well as target validation using techniques like RNA interference and transgenic animal models. Bioinformatics plays an important role in analyzing large datasets to aid in drug target discovery and validation.
This document discusses methods for drug discovery including extracting compounds from natural sources and rational drug design. It describes accidental discoveries like LSD and penicillin. Rational drug design uses structure-based and ligand-based approaches including determining biological targets, virtual screening, molecular docking, and optimization. High-throughput screening tests small molecules and virtual high-throughput screening uses computational methods. Chirality and absolute configuration can be determined through techniques like x-ray crystallography and vibrational circular dichroism. Future directions include continued computational and high-throughput approaches.
The stages of Drug Discovery and Development processA M O L D E O R E
Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regulatory status, such as via the United States Food and Drug Administration for an investigational new drug to initiate clinical trials on humans, and may include the step of obtaining regulatory approval with a new drug application to market the drug
The document discusses the drug development process from discovery to approval. It covers key stages including discovery research, preclinical testing, clinical trials, regulatory review and approval, and product launch. Key aspects addressed are screening compounds for drug candidates, assessing safety and efficacy in animal and human studies, developing formulations, and engaging regulatory agencies for approval to market a new drug. The overall goal is to discover, develop and launch new pharmaceutical products that treat diseases and conditions.
LEAD IDENTIFICATION BY SUHAS PATIL (S.K.)suhaspatil114
This document provides an overview of lead identification in drug discovery. It discusses various methods for identifying lead compounds, including combinatorial chemistry, high-throughput screening, and in silico lead discovery techniques. Combinatorial chemistry allows for the rapid production and screening of large compound libraries. High-throughput screening assays test large numbers of compounds against biological targets using automated technologies. In silico methods like molecular docking use computer simulations to predict how compounds may bind and interact with targets. The goal is to find initial "hit" compounds that can then be optimized into drug candidates.
Genetic discoveries can identify drug targets by finding loss-of-function mutations that mimic the desired effect of a drug. These "drug surrogate mutations" provide strong evidence of a target's validity. Two examples are given: 1) A mutation causing sclerosteosis identified SOST as a target for osteoporosis drugs. Antibodies blocking SOST are now in clinical trials. 2) Loss-of-function mutations in IL23 were linked to reduced Crohn's disease risk, identifying IL23 as a drug target before genetic mapping was available, and IL23 antagonists are now in clinical trials. Genetically identifying targets through drug surrogate mutations can significantly improve drug development success rates and lower costs.
Basics of Drug Discovery and DevelopmentJhony Sheik
The document outlines the process of drug discovery and development from initial screening of chemicals to determine biological activity through clinical trials and regulatory approval. It notes that of 10,000 initially screened chemicals, only 1 may reach the market place due to the high costs, risks and regulatory hurdles. The key stages discussed are preclinical testing in animals, filing an Investigational New Drug application for human trials, conducting clinical trials in four phases, filing a New Drug Application providing trial results for regulatory review and approval, large-scale manufacturing, and filing an Abbreviated New Drug Application for generic approvals relying on previously approved drugs.
The document discusses the principles and process of drug discovery, which involves identifying a target, screening compounds, preclinical testing, and clinical trials. It takes an average of 12-15 years and $600-800 million to bring a new drug to market. Key stages include target identification and validation, screening compounds through various techniques, preclinical studies in animals, and clinical trials in phases I-III to test safety and efficacy in humans. Novel approaches like microarrays, peptidomimetics, pharmacogenomics, and cheminformatics can aid the drug discovery process.
Drug discovery and development is a long, expensive, and complex process that takes an average of 10-12 years and $800 million to $1.7 billion. It involves identifying candidate drugs through methods like molecular designing, screening, and serendipity. Only one in 5000 compounds makes it through preclinical and clinical testing to be approved. The process includes target selection and validation, lead discovery and optimization, and drug development to satisfy regulatory requirements before a new drug can be approved and marketed.
clinical and preclinical approaches to drug discovery.Here we mainly deals with preclinical approaches, ie. Pharmacological approach and toxicological approach
Drug discovery challenges and different discovery approachesHitesh Soni
The document discusses several challenges in drug discovery and different discovery approaches. It outlines issues with the traditional high-throughput screening approach such as low success rates. It then describes alternative approaches like considering transient binding drugs that interact weakly with multiple targets, leveraging natural products as drug leads, and exploring a multi-target drug discovery strategy to address complex diseases involving multiple molecular dysfunctions.
The document provides an overview of the modern drug discovery process, focusing on lead identification and lead optimization. It discusses how lead compounds are initially identified through screening compound libraries or structure-based drug design. These leads are then optimized through chemical modifications to improve properties like efficacy, potency, pharmacokinetics and toxicity profile. The goal is to develop compounds suitable for preclinical and clinical testing towards becoming an approved drug. Methods for lead optimization include modifying functional groups, exploring structure-activity relationships, and altering aspects like stereochemistry.
Drug discovery By Neelima Sharma WCC chennai,neelima.sharma60@gmail.comNeelima Sharma
The document provides an overview of the drug discovery process, including the need for new drugs, approaches to discovery, and changes over time. It discusses target identification, validation, lead identification, optimization, and preclinical pharmacology/toxicology. The phases of clinical trials are also summarized, including Phase I safety trials in healthy volunteers, Phase II therapeutic exploration trials, and large Phase III randomized controlled trials. The roles of various parties in clinical trials are also outlined.
Drug development process and clinical trial for UGsSameerKhasbage
This document summarizes the process of drug development from discovery through clinical trials and approval. It discusses the main goals and requirements of each phase of clinical trials: Phase I focuses on safety and dosing in healthy volunteers, Phase II evaluates efficacy and side effects in patients, Phase III tests efficacy versus existing treatments in hundreds to thousands of patients, and Phase IV monitors long-term safety and efficacy after approval and marketing. The overall process from discovery to approval takes 10-15 years and costs over $2 billion on average.
The document discusses lead identification in drug development. It defines a lead compound as one that shows desired pharmaceutical activity and could potentially be developed into a drug. The document outlines the content to be presented, including an introduction to lead identification, what a lead is, properties of leads, and methods for identifying leads. Key methods discussed are random screening, non-random screening, high-throughput screening, and structure-based drug design.
The document summarizes the principles of drug discovery, including the following key points:
1) Drug discovery is a lengthy, expensive, and inefficient process involving target identification, screening, preclinical testing, and clinical trials that can take over 10 years from initial compound to approved drug.
2) Natural products, especially from plants, microbes, and marine organisms, have historically been an important source of leads for drug discovery due to their chemical diversity.
3) The modern drug discovery process involves high-throughput screening of large libraries of synthetic compounds and natural products to identify initial hits, which are then optimized in the hit-to-lead phase through medicinal chemistry and further testing.
This document provides an overview of careers in drug discovery and development. It discusses the multi-stage process of discovering new drugs, from identifying drug targets through clinical trials and regulatory approval. The document notes that drug development is a highly time-intensive and costly process involving many disciplines. It also aims to dispel common myths about careers in the pharmaceutical industry, emphasizing that industry scientists have opportunities for publication, innovation, and interesting work.
The document summarizes the key events in the discovery and development of penicillin. Alexander Fleming first discovered penicillin in 1928 after noticing bacteria-killing properties of the Penicillium mold in one of his petri dishes. However, he was not able to purify or characterize penicillin at the time. In the 1940s, a team at Oxford led by Howard Florey and Ernst Chain managed to purify and mass produce penicillin, paving the way for clinical trials. The first successful human trials demonstrated penicillin's ability to cure bacterial infections. By the mid-1940s, large-scale production was established. Fleming, Florey and Chain received the 1945 Nobel Prize for their discoveries. Over time, resistance
This document discusses drug discovery and the process of identifying potential new drug targets. It outlines the need for drug discovery to develop treatments for diseases without existing therapies. The key steps in drug discovery include target identification using genomics and proteomics to study the genome and map protein-protein interactions, as well as target validation using techniques like RNA interference and transgenic animal models. Bioinformatics plays an important role in analyzing large datasets to aid in drug target discovery and validation.
This document discusses methods for drug discovery including extracting compounds from natural sources and rational drug design. It describes accidental discoveries like LSD and penicillin. Rational drug design uses structure-based and ligand-based approaches including determining biological targets, virtual screening, molecular docking, and optimization. High-throughput screening tests small molecules and virtual high-throughput screening uses computational methods. Chirality and absolute configuration can be determined through techniques like x-ray crystallography and vibrational circular dichroism. Future directions include continued computational and high-throughput approaches.
The stages of Drug Discovery and Development processA M O L D E O R E
Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regulatory status, such as via the United States Food and Drug Administration for an investigational new drug to initiate clinical trials on humans, and may include the step of obtaining regulatory approval with a new drug application to market the drug
The document discusses the drug development process from discovery to approval. It covers key stages including discovery research, preclinical testing, clinical trials, regulatory review and approval, and product launch. Key aspects addressed are screening compounds for drug candidates, assessing safety and efficacy in animal and human studies, developing formulations, and engaging regulatory agencies for approval to market a new drug. The overall goal is to discover, develop and launch new pharmaceutical products that treat diseases and conditions.
LEAD IDENTIFICATION BY SUHAS PATIL (S.K.)suhaspatil114
This document provides an overview of lead identification in drug discovery. It discusses various methods for identifying lead compounds, including combinatorial chemistry, high-throughput screening, and in silico lead discovery techniques. Combinatorial chemistry allows for the rapid production and screening of large compound libraries. High-throughput screening assays test large numbers of compounds against biological targets using automated technologies. In silico methods like molecular docking use computer simulations to predict how compounds may bind and interact with targets. The goal is to find initial "hit" compounds that can then be optimized into drug candidates.
Genetic discoveries can identify drug targets by finding loss-of-function mutations that mimic the desired effect of a drug. These "drug surrogate mutations" provide strong evidence of a target's validity. Two examples are given: 1) A mutation causing sclerosteosis identified SOST as a target for osteoporosis drugs. Antibodies blocking SOST are now in clinical trials. 2) Loss-of-function mutations in IL23 were linked to reduced Crohn's disease risk, identifying IL23 as a drug target before genetic mapping was available, and IL23 antagonists are now in clinical trials. Genetically identifying targets through drug surrogate mutations can significantly improve drug development success rates and lower costs.
Drug discovery process style 5 powerpoint presentation slides db ppt templatesSlideTeam.net
The document outlines the key stages in the drug discovery process, including target selection, lead discovery, drug development, preclinical testing, and clinical trials. Genetic and cellular targets are identified through genomics and proteomics. Combinatorial chemistry and high-throughput screening are used to develop compound libraries and identify potential drug candidates. Lead compounds are refined through medicinal chemistry and testing in cellular and animal disease models. Top candidates then progress to clinical trials in humans to test for safety and efficacy.
This document discusses ethnopharmacology, which is the scientific study of materials used as medicines by different cultural groups. It notes that ethnopharmacology is a branch of ethnobotany and involves multiple disciplines. The document outlines the historical development of ethnopharmacology and the process of drug discovery using its approach. This includes obtaining information from sources, scientific investigation through extraction, activity testing, and chemical examination. It also discusses some problems and questions regarding ethnopharmacology, such as reliability of information and intellectual property issues.
The document discusses preclinical development and whether changes are needed. It outlines the stages from target discovery to registration, noting the high costs and attrition rates. Exploratory toxicology aims to predict toxicities and select candidates, while regulatory toxicology provides safety margins for starting human trials. A variety of assays are used to evaluate general toxicity, genotoxicity, safety pharmacology and more. Challenges include poor translation between preclinical models and humans. Opportunities exist to improve prediction through new technologies and approaches. Overall, advances have been made but high attrition rates continue to motivate further improvements.
Target selection lead discovery medicinal drug discovery process design 5 pow...SlideTeam.net
The document outlines the key stages of the drug discovery process, including identifying genetic and cellular targets, synthesizing and isolating compounds through combinatorial chemistry and high-throughput screening, developing structure-activity relationships through in silico and in vitro studies, evaluating drug affinity and selectivity in cellular and disease models, testing lead candidates in animal models of disease states, and conducting clinical trials and therapeutics in humans.
The document provides an overview of requirements for an Investigational New Drug (IND) application to the FDA. It discusses key components of the IND including chemistry, manufacturing and controls (CMC), preclinical toxicology studies, and clinical trial protocols. The main points are:
1) An IND application is required to begin clinical testing of new drugs, drugs at new dosages, or drug combinations not previously approved.
2) Key sections of the IND include CMC data on drug manufacturing and quality controls, results of preclinical toxicology studies in animals, and protocols for proposed clinical trials.
3) Preclinical studies aim to identify safe starting doses for clinical trials and target organs of toxicity.
Teriparatide (Forteo) is an effective treatment for osteoporosis that works by stimulating new bone formation. It increases bone mineral density, improves bone microarchitecture, and reduces the risk of fractures. While other medications inhibit bone resorption, teriparatide has an anabolic effect through its similar structure to parathyroid hormone.
This document discusses the field of ethnopharmacology, which is the scientific study of medicinal substances used by different cultural groups. It provides examples of many plants and the indigenous medicinal uses of those plants, including yew, coca, willow, opium poppy, and ginseng. It also describes how some modern pharmaceuticals were developed from studying ethnopharmacological substances, such as aspirin from willow bark, quinine from cinchona, and taxol from yew trees.
Chronopharmacology is the study of variations in drug effects over biological times and circadian rhythms. It considers how drugs interact with living systems depending on the time of day they are administered. Biological rhythms like circadian (24-hour), ultradian (<20 hours), and infradian (>28 hours) rhythms influence physiological functions and drug pharmacokinetics and pharmacodynamics. Chronotherapy aims to increase drug efficacy and safety by timing drug administration according to biological rhythms. It has applications in treating cancers, asthma, hypertension, strokes, and other conditions. Recent advances include circadian-aligned drug delivery systems and future approaches may integrate chronopharmacology with systems biology and nanomedicine.
This document outlines reverse pharmacology, which involves starting drug discovery with clinically documented effects from traditional medicines and exploring the underlying mechanisms through laboratory and clinical research. It discusses the definition, scope, and phases of reverse pharmacology. It provides examples of drugs discovered through reverse pharmacology from India, including drugs for hypertension, amoebiasis, and Parkinson's disease. It also discusses some challenges to reverse pharmacology and promising future perspectives if more collaboration between academia and industry can help validate traditional knowledge through rigorous clinical research.
This document discusses reverse pharmacognosy, an approach that starts with a biologically active molecule and uses computational tools to identify potential plant sources of that molecule, rather than the conventional approach of screening many plant extracts. It describes Selenergy software that predicts molecule-protein interactions and identifies biological targets. Case studies are presented on identifying targets of ε-viniferin from grapes, meranzin from Limnocitrus, and tofisopam. Reverse pharmacognosy can accelerate drug discovery, allow drug repositioning, and decrease plant usage compared to conventional screening methods.
A review presentation by an authority - Dr Ashok Vaidya,
for drug design based on therapeutic efficacy of ayurvedic herbs carrying out reverse engineering ...
This document provides an overview of the scope of pharmacology. It discusses the history and evolution of pharmacology from materia medica and early pharmacy to its modern academic, industrial and research applications. Key areas of pharmacology discussed include drug development process, clinical pharmacology, special domains like pharmacovigilance, pharmacoeconomics and emerging areas like pharmacogenomics. The document outlines the past, present and future scope of pharmacology and how it aims to advance human health through rational and safe use of medicines.
Proteomics is the study of the structure and function of proteins. It involves identifying and quantifying the proteins expressed by a genome or cell type. Key aspects of proteomics include protein separation techniques like gel electrophoresis, mass spectrometry to identify proteins, and analyzing protein interactions and post-translational modifications. While genomes provide the blueprint, proteomics helps understand the diversity of proteins expressed and how they function together to direct cellular activities. It is a promising tool for disease diagnosis by identifying protein biomarkers.
Proteomics is the large-scale study of proteins, including their structures, functions, and interactions. It has become an important technology for understanding biological systems on a global scale. Mass spectrometry plays a key role in proteomic analysis by allowing researchers to identify and characterize proteins and their post-translational modifications like phosphorylation. There are challenges in analyzing post-translational modifications since proteins exist in multiple modified forms, but methods like affinity enrichment and tandem mass spectrometry are used to map modifications and locate them on protein sequences.
Data Mining and Big Data Analytics in Pharma Ankur Khanna
The document proposes software solutions for drug research, including text mining, data warehousing, data mining, database development, and big data analytics. It discusses common challenges in drug research like the high costs and low success rates. It then describes various solutions like text mining patents and research to help identify new research opportunities and reduce duplication of efforts. It provides examples of how various pharmaceutical companies use data mining and warehousing techniques. Overall, the document pitches different IT solutions that can help pharmaceutical and life sciences companies address their research challenges and make their processes more efficient.
This year's 3rd Annual TCGC: The Clinical Genome Conference, held June 10-12, 2014 in San Francisco, is a three-day event that weaves together the science of sequencing and the business of implementing genomics in the clinic. It uniquely illustrates the mutual influence of those areas and the need to therefore consider the needs, challenges and opportunities of both - from next-generation sequencing and variant interpretation to insurance reimbursement and electronic health records - throughout the entire research process.Learn more at http://www.clinicalgenomeconference.com
Discover new cases studies giving you unprecedented access to both the data and results of how RNA-Seq is being applied successfully from bench to bedside
Gain new insights into RNA-Seq for the study of toxicity, IO, host-viral interactions and more from companies such as BMS, Janssen, Pfizer, Merck, UCSC and Stanford
2nd CRISPR Congress Boston, 23-25 February 2016 Diane McKenna
The 2nd Annual CRISPR Congress will enhance the basic research, drug discovery and therapeutic applications of CRISPR technology by overcoming key specificity, efficiency and delivery challenges needed to improve the precise editing and repair of the genome.
CHI's Bioassays for Immuno-Oncology Symposium, Oct. 23, 2017 in Washington, DCJames Prudhomme
Biological assays demonstrating drug characteristics such as potency, mechanism-of-action, and stability, are one of the most critical components of an FDA biologic submission. However, with more complex mechanisms-of-action, immunotherapies add a layer of difficulty to bioassay selection and development. At Cambridge Healthtech Institute's Inaugural Bioassays for Immuno-Oncology symposium, experts in bioassays for immuno-oncology therapies will discuss selection, development, and standards for bioassays and immunoassays. Special attention will be given to understanding the mechanism-of-action for immunotherapies, whether they be antibody- or cell-based. Overall, this one-day immersive symposium will outline a product life cycle approach for developing and implementing biological assays from preclinical studies to clinical development. This symposium is part of the Immunogenicity & Bioassay Summit.
Jason C. Poole has 17 years of experience as a molecular biologist developing novel molecular and genetic assays. He has a PhD in molecular genetics and most recently worked at EMD Millipore developing qPCR and next generation sequencing assays that were commercialized. He is seeking a senior scientist or project leader position and has strong skills in areas like qPCR, sequencing, cloning, and assay development.
The document summarizes the 14th Annual PepTalk conference organized by Cambridge Healthtech Institute. The conference will be held from January 19-23, 2015 in San Diego, CA and will feature over 1,200 international participants from industry, academia and government. It will include 20 conferences, 13 short courses, 325 speaker presentations, 80 roundtable discussions, 100 exhibitors and 125 research posters on topics related to protein engineering, antibody therapeutics, formulation, production, analytics and purification. A keynote speech will be given by Dr. John Yates from The Scripps Research Institute on advances in proteomics. The conference provides numerous opportunities for education, innovation and networking in the protein science field.
Precision Medicine & Biomarkers Leaders Summit - Boston USA - 7th & 8th MayTony Couch
Global Engage is pleased to announce the 2018 Precision Medicine & Biomarkers Leaders Summit USA taking place on May 7-8th in Boston, MA. The event is part of our highly successful Drug Discovery Series which includes conferences on Biologics, Medicinal Chemistry, NASH, Pharmaceutical R&D IT and the Human Microbiome amongst others. It is also the sister meeting of the European Precision Medicine Summit which has run successfully since 2013.
The document summarizes a 2-day conference on qPCR and digital PCR taking place on July 11-12, 2016 in Philadelphia. Over 150 industry and academic experts will discuss the latest developments and applications of qPCR and dPCR across various fields such as healthcare, plant science, food science and environmental testing. The conference will feature keynote speakers, case study presentations, a poster session and interactive panels on topics including digital PCR applications, qPCR strategies, healthcare case studies, and plant/food/environmental case studies. Confirmed speakers include experts from academic institutions and companies.
The document discusses drug design, development, and delivery. It covers rational drug design using molecular properties and receptor modeling. Computer-assisted drug design uses molecular docking and QSAR methods. Neural networks are also used in drug design. Drug discovery involves identifying candidates and screening for efficacy. Drug development evaluates ADME, toxicity, and safety through preclinical and clinical studies. Drug delivery methods aim to effectively administer pharmaceutical compounds and improve drug release profiles.
Leveraging functional genomics analytics for target discoveryEnrico Ferrero
The document discusses how GSK is leveraging functional genomics analytics like RNA-seq, ChIP-seq, and DNase-seq to improve target discovery. It provides examples of projects analyzing disease progression in rheumatoid arthritis, responses to viral infection, and mechanisms of action of neurogenesis compounds. The goal is to better understand diseases, targets, and drugs to reduce late stage clinical trial failures and costs through more rigorous target validation early on. Partnerships with academic institutions are also highlighted.
This document provides an introduction to the field of bioinformatics. It defines bioinformatics as a branch of science that uses computer technology to analyze and integrate biological information that can be applied to gene-based drug discoveries. It discusses the emergence of bioinformatics due to the desire to understand how genetic structure affects traits. It also outlines some common applications of bioinformatics like drug design, gene therapy, and microbial genomic analysis. Finally, it provides examples of some bioinformatics tools, databases, and centers in India.
2nd CRISPR Congress Boston, 23-25 February 2016 Diane McKenna
The 2nd Annual CRISPR Congress will enhance the basic research, drug discovery and therapeutic applications of CRISPR technology by overcoming key specificity, efficiency and delivery challenges needed to improve the precise editing and repair of the genome.
PEGS Europe Protein & Antibody Engineering Summit 2014 AgendaNicole Proulx
PEGS Europe is the largest European event covering all aspects of protein and antibody engineering. With two consecutive years of 40% growth in attendance, and another year of expanded program coverage, this year’s event will feature:
•500 attendees
•150 technical presentations
•70+ scientific posters
•40+ sponsors & exhibitors
•Dedicated networking opportunities
•Exclusive exhibit & poster hours
•Interactive roundtable, breakout & panel discussions
Precision Medicine & Biomarkers Leaders Summit - Boston USA - 7th & 8th MayTony Couch
Tracks focus on R&D strategies, Biomarker development, Immuno-oncology, CDx development, AI and Big data analysis and approaches – Attending this Summit will provide you with the opportunity to mix and interact with experts working in all facets of Precision Medicine through the individual, panel and roundtable discussions on offer.
This document provides an introduction and overview of a refresher course in molecular biology and bioinformatics. The course aims to provide a solid introduction to molecular biology techniques and bioinformatics tools currently used to investigate molecular mechanisms and their application to disease diagnosis and treatment. It will introduce concepts like genomics, transcriptomics, proteomics, epigenetics, genome editing with CRISPR, molecular cloning, and genome-wide association studies. The course also discusses various molecular biology techniques like DNA sequencing, PCR, immunohistochemistry and their role in furthering our understanding of human disease at the molecular level to improve patient care through more accurate diagnosis and targeted therapies.
- Discover new methods for managing clinical next-gen data with insights from Pfizer, Boston Children’s Hospital and AstraZeneca
- Uncover and critique the latest technologies out there for you to use in clinical trials. Mayo Clinic, Merck and Harvard Medical School let you into their trade secrets
- Hear the genomics strategies that Roche, Millennium and Regeneron are using for discovery and validation of clinically actionable biomarkers
-Bristol-Myers Squibb, Takeda and Partners Healthcare the role that NGS can play when implementing an effective strategy in the lab to speed up CDx development
- Learn how to integrate molecular details into medical decision making, with fresh data from Washington University School of Medicine and Genzyme
Computer aided drug design (CADD) uses computer modeling to help design and discover new drug molecules. It involves designing molecules that are complementary in shape and charge to bind to a biomolecular target like a protein. This can help drugs activate or inhibit the target to produce therapeutic effects. CADD is not a direct route to new drugs but provides information to guide and coordinate drug discovery experiments in a more efficient manner. It is hoped CADD can help save time and money in the drug development process.
13th Annual World Pharma Congress [Full Agenda]Jaime Hodges
After spending 12 years in Philadelphia World Pharma Congress is moving to Boston, which is buzzing with new findings and technologies that can potentially revolutionize the way in which traditional preclinical drug discovery is done. World Pharma Congress 2014 will provide a forum for scientists and clinicians to meet to exchange ideas and launch collaborations. Coverage includes: Tumor Models for Targeted Therapy, Tumor Models for Cancer Immunotherapy, Imaging in Oncology, In Vitro Tumor Models, Preclinical Drug Safety, Epigenetics Screening, Formulation & Drug Delivery, Process Chemistry and Targeting Pain. For event updates and the full speaking faculty list, visit http://www.worldpharmacongress.com
Similar to Discovery on Target 2014 - The Industry's Preeminent Event on Novel Drug Targets (20)
CHI’s Thirteenth Annual High-Content Analysis meeting, the premier event showcasing the latest advancements in HCA applications and technologies, returns to San Diego with a new program. Over the years we have observed the technology mature and its adoption spread into many areas of compound screening/evaluation and functional analysis. The High-Content Analysis meeting will focus on the next steps of technology development, including screening of 3D and physiologically relevant complex models, ultra-high resolution and high-throughput imaging, more advanced image analysis and data management, and new assays and applications. The co-located Second Annual Phenotypic Screening meeting will address the advantages of phenotypic screening vs. target-based screening, and focus on assay development, selection of physiologically relevant models and subsequent target identification, as well as case studies of phenotypic screens from leading pharma. Join the original High-Content Analysis event and get access to two tracks featuring a cutting-edge scientific agenda, expanded exhibit hall and technology showcases, and an offering of technology demonstrations and dinner courses.
Seventh Annual Next Generation Dx SummitJaime Hodges
The Next Generation Dx Summit (www.nextgenerationdx.com), entering its seventh year, brings together more than 800 diagnostics professionals from across the world, providing comprehensive programming and valuable networking opportunities. Spanning from clinical diagnostics to business strategy, this year’s expanded program encompasses predictive cancer biomarkers, companion diagnostics, infectious disease, point-of-care, pharmacy-based diagnostics, cell-free DNA, commercialization, cancer immunotherapy, and reimbursement. With widespread coverage of all the most relevant diagnostics topics, the Next Generation Dx Summit promises to be a must-attend event to hear the latest announcements and developments in this rapidly evolving field.
Clinical Research Informatics World 2015Jaime Hodges
The document provides information about the "Clinical Research Informatics World 2015" conference to be held on May 6-7, 2015 in Boston, MA. It includes details about keynote speakers, sessions, sponsors and registration. The conference will focus on topics such as leveraging new technologies and analytics to advance clinical trials, using existing data sources to support trials, and cross-industry data sharing. Sessions will provide case studies and discuss strategies for areas like establishing big data strategies, bringing patient centricity to trials, and innovating clinical trial processes with new technologies.
The 2015 Bio-IT World Conference & Expo plans to unite 3,000+ life sciences, pharmaceutical, clinical, healthcare, and IT professionals from 32+ countries. The Expo provides the perfect venue to share information and discuss enabling technologies that are driving biomedical research and the drug development process.
Since its debut in 2002, the annual Bio-IT World Conference & Expo has established itself as a premier event showcasing the myriad applications of IT and informatics to biomedical research and the drug discovery enterprise. The 2015 program will feature compelling talks from industry and academia on new trends in data generation, knowledge management, and information technology in life sciences and drug development, including best practice case studies and joint partner presentations relevant to the technologies, research, and regulatory issues of life science, pharmaceutical, clinical and IT professionals.
Spanning three days, the meeting includes 12 parallel conference tracks and 17 pre-conference workshops. Learn more at http://www.bio-itworldexpo.com
Held each year in Boston, Medical Informatics World connects more than 400 healthcare, biomedical science, health informatics, and IT leaders to navigate emerging trends and opportunities in the evolving industry. The event responds to the challenges in collaborating and maximizing the benefit of enabling technologies with inspiring plenary keynotes combined with focused expert-led presentations and discussions. Coverage includes population health management, predictive analytics, payer-provider-pharma data collaborations, patient care and engagement, mobile and wearable technologies, care delivery models, enterprise hospital information systems, clinical decision support, error and readmission reduction, and healthcare data security. The 2015 program features six conference tracks, two interactive dinner workshops and six plenary keynote presentations, providing attendees with the connections, tools and strategies for taking their research and care delivery to the next level. Learn more at http://www.medicalinformaticsworld.com
Extracellular Biomarkers Summit, the newest addition to Cambridge Healthtech Institute's notable biomarker and diagnostics portfolio, merges the well-established microRNA as Biomarkers and Diagnostics Conference with focused discussions on three leading areas of research: the role of circulating microRNA, exosomes and microvesicles, long non-coding RNA and extracellular RNA in cancer and other diseases, as well as their potential to serve as biomarkers in drug and diagnostic development. Discussions will include the isolation and characterization of exosomes and exRNA, including expression profiling and sequencing of exRNA; understanding the role of miRNA, lncRNA, and exosomes in disease mechanism, tumor metastasis, and intracellular communication; their potential as biomarkers in drug development, drug toxicity assessment, and patient stratification; and finally, their role as circulating biomarkers for disease diagnosis and prognosis. Learn more at http://www.extracellularbiomarkers.com
Medical Informatics World 2014 [Full Agenda]Jaime Hodges
Cambridge Healthtech Institute and Bio-IT World’s Second Annual Medical Informatics World builds upon last year’s successful inaugural launch by delivering timely programming focused on the cross-industry connections and innovative solutions needed to take biomedical research and healthcare delivery to the next level.
The 2014 meeting will bring together more than 300 senior level executives and industry leaders from each side of the discussion - providers, payers and pharma - in the fields of healthcare, biomedical sciences, health informatics, and IT. Over two days of insightful discussions and engaging presentations, leading experts will share emerging trends and solutions in population health management, payer-provider-pharma data collaborations, optimizing patient care and engagement, leveraging mobile technologies, sustaining innovation within the rapidly changing care delivery models, enhancing clinical decision support, controlling costs and improving quality, and maintaining security-privacy in healthcare. Led by key decision makers and senior executives at the forefront of healthcare information technology, the conference is a must-attend for all involved in this evolving industry.
Co-located with CHI's flagship Bio-IT World Expo, a premier event showcasing the myriad applications of IT and informatics to the life sciences enterprise, Medical Informatics World completes the week of scientific content by bridging the healthcare and life science worlds. As Bio-IT World Expo attracts more than 2,500 delegates from dozens of countries as well as more than 130 exhibiting companies, networking opportunities abound at the two events. To learn more, visit http://www.medicalinformaticsworld.com
Clinical Genomics & Informatics Europe - ProgramJaime Hodges
Bio-IT World and Cambridge Healthtech Institute's Fifth International Clinical Genomics & Informatics Europe Conference will feature four main tracks on Clinical Exome Sequencing, High-Scale Computing, RNA Sequencing and Genome Informatics. In addition, two pre-conference Symposia on Clinical Epigenetics and Digital Detection Techniques and Applications will be provided. View the full program and details at http://www.clinicalgenomicsinformatics.com
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- Video recording of this lecture in English language: https://youtu.be/kqbnxVAZs-0
- Video recording of this lecture in Arabic language: https://youtu.be/SINlygW1Mpc
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Rasamanikya is a excellent preparation in the field of Rasashastra, it is used in various Kushtha Roga, Shwasa, Vicharchika, Bhagandara, Vatarakta, and Phiranga Roga. In this article Preparation& Comparative analytical profile for both Formulationon i.e Rasamanikya prepared by Kushmanda swarasa & Churnodhaka Shodita Haratala. The study aims to provide insights into the comparative efficacy and analytical aspects of these formulations for enhanced therapeutic outcomes.
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Oleg Kshivets
Overall life span (LS) was 1671.7±1721.6 days and cumulative 5YS reached 62.4%, 10 years – 50.4%, 20 years – 44.6%. 94 LCP lived more than 5 years without cancer (LS=2958.6±1723.6 days), 22 – more than 10 years (LS=5571±1841.8 days). 67 LCP died because of LC (LS=471.9±344 days). AT significantly improved 5YS (68% vs. 53.7%) (P=0.028 by log-rank test). Cox modeling displayed that 5YS of LCP significantly depended on: N0-N12, T3-4, blood cell circuit, cell ratio factors (ratio between cancer cells-CC and blood cells subpopulations), LC cell dynamics, recalcification time, heparin tolerance, prothrombin index, protein, AT, procedure type (P=0.000-0.031). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and N0-12 (rank=1), thrombocytes/CC (rank=2), segmented neutrophils/CC (3), eosinophils/CC (4), erythrocytes/CC (5), healthy cells/CC (6), lymphocytes/CC (7), stick neutrophils/CC (8), leucocytes/CC (9), monocytes/CC (10). Correct prediction of 5YS was 100% by neural networks computing (error=0.000; area under ROC curve=1.0).
Osteoporosis - Definition , Evaluation and Management .pdfJim Jacob Roy
Osteoporosis is an increasing cause of morbidity among the elderly.
In this document , a brief outline of osteoporosis is given , including the risk factors of osteoporosis fractures , the indications for testing bone mineral density and the management of osteoporosis
These lecture slides, by Dr Sidra Arshad, offer a quick overview of the physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar lead (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
6. Describe the flow of current around the heart during the cardiac cycle
7. Discuss the placement and polarity of the leads of electrocardiograph
8. Describe the normal electrocardiograms recorded from the limb leads and explain the physiological basis of the different records that are obtained
9. Define mean electrical vector (axis) of the heart and give the normal range
10. Define the mean QRS vector
11. Describe the axes of leads (hexagonal reference system)
12. Comprehend the vectorial analysis of the normal ECG
13. Determine the mean electrical axis of the ventricular QRS and appreciate the mean axis deviation
14. Explain the concepts of current of injury, J point, and their significance
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. Chapter 3, Cardiology Explained, https://www.ncbi.nlm.nih.gov/books/NBK2214/
7. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
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Part II - Body Grief: Losing parts of ourselves and our identity before, duri...
Discovery on Target 2014 - The Industry's Preeminent Event on Novel Drug Targets
1. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 1
REGISTER BY JUNE 13 AND SAVE UP TO $
600!
October 8 – 9
Targeting Epigenetic Readers and Chromatin Remodelers
Targeting the Ubiquitin Proteasome System
Big Data Analytics and Solutions – NEW!
GPCR-Based Drug Discovery
RNAi for Functional Genomics Screening - Part 1
Protein-Protein Interactions as Drug Targets – NEW!
Antibodies Against Membrane Protein Targets - Part 1
October 9 – 10
Targeting Histone Methyltransferases and Demethylases
Screening Drug Transporter Proteins – NEW!
Maximizing Efficiency in Discovery – NEW!
GPCR-Targeted Therapeutics
Genome Editing for Functional Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane Protein Targets - Part 2
12th
ANNUAL
OCTOBER 8 - 10, 2014 WESTIN BOSTON WATERFRONT | BOSTON MA
The Industry’s Preeminent Event on Novel Drug Targets
SYMPOSIUM
EIGHTH ANNUAL
Next Generation Histone
Deacetylase Inhibitors
EVENT FEATURES
14 Conferences
13 Short Courses
1 Symposium
40+ Exhibitors
50+ Posters
40+ Interactive Breakout Discussion Groups
Plenary Keynote Speakers
PREMIER
SPONSOR
2. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 2
Tuesday
October 7
Pre-Conference Short Courses* and 1-day Symposium: Next Generation Histone Deacetylase Inhibitors*
Wednesday
October 8
1A: Targeting
Epigenetic Readers
and Chromatin
Remodelers
2A: Targeting the
Ubiquitin Proteasome
System
3A: Big Data Analytics
& Solutions
4A: GPCR-Based Drug
Discovery
5A: RNAi for Functional
Genomics Screening –
Part 1
6A: Protein-Protein
Interactions as Drug
Targets
7A: Antibodies Against
Membrane Protein
Targets – Part 1
Thursday
October 9
1A: Targeting
Epigenetic Readers
and Chromatin
Remodelers
2A: Targeting the
Ubiquitin Proteasome
System
3A: Big Data Analytics
& Solutions
4A: GPCR-Based Drug
Discovery
5A: RNAi for Functional
Genomics Screening –
Part 1
6A: Protein-Protein
Interactions as Drug
Targets
7A: Antibodies Against
Membrane Protein
Targets – Part 1
1B: Targeting Histone
Methyltransferases and
Demethylases
2B: Screening Drug
Transporter Proteins
3B: Maximizing
Efficiency in Discovery
4B: GPCR-Targeted
Therapies
5B: Genome Editing for
Functional Genomics
Screens – Part 2
6B: Cancer Metabolism 7B: Antibodies Against
Membrane Protein
Targets – Part 2
Thursday
October 9
7:00–10:00 pm
Dinner Short Courses*
Friday
October 10
1B: Targeting Histone
Methyltransferases and
Demethylases
2B: Screening Drug
Transporter Proteins
3B: Maximizing
Efficiency in Discovery
4B: GPCR-Targeted
Therapies
5B: Genome Editing for
Functional Genomics
Screens – Part 2
6B: Cancer Metabolism 7B: Antibodies Against
Membrane Protein
Targets – Part 2
CONFERENCE-AT-A-GLANCE*
Cambridge Healthtech Institute will host its 12th
Annual Discovery onTarget event showcasing current and emerging “hot” targets for the pharmaceutical
industry October 8 – 10, 2014 in Boston, MA. Spanning three days, the meeting attracts 900+ attendees (from 24 countries), composed of scientists/
technologists, executives, directors, and managers from biopharma, academic, and healthcare organizations. In 2014 the event is comprised of 14 meeting
tracks which include Epigenetic Readers, Ubiquitin Proteasome, Big Data Discovery, GPCR Drug Discovery, RNAi-Screens-Functional-Genomics, PPI
Targets, Protein-Targets, Histone-Methyltransferases-Demethylases, DrugTransporters, Maximizing Efficiency, GPCRTherapeutics, Genomics Screening,
Cancer Metabolism and Membrane Production.The 2014 event offers 200+ scientific presentations across these 14 conference tracks, 1 Symposium and
13 conference short courses, 40+ interactive breakout discussion groups, an exhibit hall of 40+ companies, and dedicated poster viewing and networking
sessions.The 12th
Annual Discovery onTarget assembles an impressive group of 195+ distinguished speakers who look forward to sharing their
knowledge, best practices, and expertise with all attendees.
*Separate registration required for Short Courses and Symposium
PREMIER
SPONSOR
CORPORATE SPONSORS
Cambridge Healthtech Institute
250 First Avenue, Suite 300, Needham, MA 02494 | www.healthtech.com
3. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 3
SHORT COURSES*
* Separate registration required; see website for complete course details
TUESDAY, OCTOBER 7
Morning Courses | 8:00 am – 11:00 am
SC1: Designing Scalable Software Systems for Big Data Analytics
John Klein, Senior Member of the Technical Staff, Software Solutions
Division, Carnegie Mellon Software Engineering Institute
Scalable software systems that deliver the required functionality, along with
qualities such as performance, availability, and usability, are essential to data-
driven biomedical research.The design of these software systems includes
technology selection and a software architecture that spans data model, network
topology, and application design. Execution agility is critical in this rapidly
changing technology landscape.This course presents a method for rapidly
making technology selection decisions, discusses some underlying principles
that will help system designers cut through the hype surrounding scalable
solutions, and applications to identifying new targets for drug discovery.
Afternoon Courses | 12:00 pm – 3:00 pm
SC2: Approaches for Biologically-Relevant Chemical Diversity
Todd Wenderski, Ph.D., Research Fellow, Molecular Pharmacology &
Chemistry Program, Sloan-Kettering Institute for Cancer Research, Memorial
Sloan-Kettering Cancer Center
Additional Instructors to be Announced
Small bioactive molecules are the starting point for any discovery program,
yet despite the vast chemical space available for generation of novel chemical
matter, existing small-molecule drugs address only a very small subset
of protein targets.To address this disconnect, a resurgence of interest in
pharmacognosy, using “privileged” natural products along with the utilization
of diversity oriented synthesis (DOS), and DNA-templated organic synthesis
as a starting point for translation into chemical libraries are being recognized
as important strategies to guide design and generation of novel compound
collections.This workshop will discuss modern approaches for the synthesis of
novel, diverse, and biologically-relevant chemical collections.
SC3: Setting Up Effective RNAi Screens: From Design to
Data to Validation
Caroline Shamu, Ph.D., Director, ICCB-Longwood Screening Facility, Harvard
Medical School
Eugen Buehler, Ph.D., Group Leader, Informatics, National Center for
Advancing Translational Sciences, National Institutes of Health
John Doench, Ph.D., Research Scientist, Broad Institute of Harvard and MIT
Scott Martin, Ph.D., Team Leader, RNAi Screening, NIH Chemical Genomics
Center, National Center for Advancing Translational Sciences, National
Institutes for Health
The course is designed to provide in-depth information on how to go about
setting up RNAi screening experiments and how to design assays for getting
optimal results.The challenges working with siRNAs and shRNAs and the
delivery reagents needed to get them into the appropriate cells and tissues
will be discussed. The instructors will also provide their input on best
practices for the execution of experiments and interpretation of results when
dealing with complex biology and informatics.
SC4:Targeting Protein-Protein Interactions
Daniel A. Erlanson, Ph.D., Co-Founder and President, CarmotTherapeutics, Inc.
Edward R. Zartler, Ph.D., President & CSO, Quantum Tessera Consulting
Protein-protein interactions (PPIs) represent a large but largely untapped
class of biological targets covering virtually every therapeutic area. Despite
several success stories, many researchers still consider PPIs to be
“undruggable.” This course will provide attendees with an overview of how
to discover small-molecule inhibitors of PPIs. Attendees will also learn about
potential pitfalls and what not to do. Other topics covered will include how to
evaluate the feasibility of PPIs, what biophysical techniques to use, and how
fragment-based lead discovery can tackle particularly challenging PPIs.
SC5: GPCR Structure-Based Drug Discovery
Vsevolod (Seva) Katritch, Ph.D., Assistant Professor, Integrative Structural and
Computational Biology, The Scripps Research Institute
Jan Steyaert, Ph.D., Director, Structural Biology Brussels Research Center,
Vrije University Brussels
This course will review the new structural knowledge now available for many G
Protein-Coupled Receptors (GPCRs) based on their recently elucidated crystal
structures.The instructors will explore with participants, how new findings are
impacting rational drug design approaches for GPCRs.There will also be a focus on
tools now showing progress against GPCRs such as fragment-based approaches
and using antibodies to probe GPCR structure for extracting information that
enables the medicinal chemist to more efficiently design GPCR-targeted ligands.
Evening Courses | 3:45 pm – 6:45 pm
SC6: Advances in Metagenomic Drug Discovery for New Anti-
Infective Agents
Blaine Pfeifer, Ph.D., Associate Professor, Chemical and Biological
Engineering, University at Buffalo, The State University of New York
Mark R. Liles, Ph.D., Associate Professor, Biological Sciences, Auburn University
Metagenomic drug discovery is reliant on two components: viable
environmental DNA (eDNA) samples and a robust heterologous biosynthetic
platform. This workshop will present data and results focused on significant
modifications to each of these components and how they are now being
merged for advanced drug discovery potential. Specifically, unprecedented
large-insert eDNA constructs are being channeled through designer
heterologous host systems for a revamped antibiotic discovery scheme
that offers new possibilities for rapid, efficient, and scalable solutions to the
pressing need for new anti-infective agents.
SC7:Targeting of GPCRs with Monoclonal Antibodies
Barbara Swanson, Ph.D., Director, Research, SorrentoTherapeutics, Inc.
While GPCRs (G protein-coupled receptors) are important therapeutic targets,
it has been challenging to discover therapeutically relevant antibodies against
them.This course will examine different steps along the anti-GPCR antibody
discovery pathway and highlight various approaches to accomplishing each step.
4. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 4
SHORT COURSES*
* Separate registration required; see website for complete course details
The topics to be covered include: 1) Antibody discovery, including methods to
generate antibodies and antigen preparation; 2) Assays to measure antibody
binding, such as an EC50 using cells expressing the GPCR; 3) In vitro assays
to measure functional activity of the antibody, including antagonism (IC50) or
agonism using chemotaxis, calcium, cAMP or other cell-based assays; and 4)
Review of promising GPCR targets and antibodies in the clinic.
SC8: A Primer to Gene Editing:Tools and Applications
Neville Sanjana, Ph.D., Simons Postdoctoral Fellow, Laboratory of Dr. Feng
Zhang, Broad Institute and the Department of Brain and Cognitive Sciences,
Massachusetts Institute of Technology
John Doench, Ph.D., Research Scientist, Broad Institute of Harvard and MIT
Benjamin Housden, Ph.D., Postdoctoral Fellow, Laboratory of Dr. Norbert
Perrimon, Department of Genetics, Harvard Medical School
This course will help attendees understand the fundamentals of gene
editing and the various tools available. The instructors will compare and
contrast the use of CRISPR/Cas9 system with meganucleases, zinc-finger
nucleases, and transcription activator-like effector nucleases (TALENs)
highlighting the best use of each system for various applications. Tools and
methods for setting up CRISPR-based genetic screens using Drosophila and
mammalian cell systems will be discussed in great detail.
SC9: Introduction toTargeted Covalent Inhibitors
Mark Schnute, Ph.D., Associate Research Fellow, Biotherapeutics Chemistry
& Immunoscience Research, Pfizer Global R&D
Christoph Zapf, Ph.D., Principal Scientist, Worldwide Medicinal Chemistry,
Pfizer Research Labs
Covalent inhibitors of kinases have re-emerged as a drug design strategy
due to more examples of their safety and efficacy in patients. Covalent
inhibitors have the advantage of increased selectivity and longer action
of duration but there are still important issues about their design and
application that need to be better understood. This course will cover practical
as well as theoretical issues that a medicinal chemist needs to keep in mind
in developing covalent inhibitors.
THURSDAY, OCTOBER 9
Dinner Courses | 7:00 pm – 10:00 pm
SC10: Setting Up Effective Functional Screens Using 3D Cell Cultures
Lesley Mathews Griner, Ph.D., Investigator II, Lab Head in Molecular
Pharmacology at Novartis Institutes for BioMedical Research
Geoffrey A. Bartholomeusz, Ph.D., Assistant Professor and Director, siRNA
Core Facility, Department of Experimental Therapeutics, Division of Cancer
Medicine, The University of Texas M.D. Anderson Cancer Center
Arvind Rao, Ph.D., Assistant Professor, Department of Bioinformatics and
Computational Biology, The University of Texas MD Anderson Cancer Center
SC11: Integration of BDDCS and Extended Clearance Principles
for Understanding Disposition and ADME liabilities
Ayman El-Kattan, Ph.D., Associate Research Fellow, Department of
Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc.
Yurong Lai, Ph.D., Senior Principal Scientist, Pharmaceutical Candidate
Optimization, Bristol-Myers Squibb Company
The absorption and disposition of statins and ACE inhibitors is an outcome
of the interplay of metabolizing enzymes and transporters. Appropriate
understanding of principles of BDDCS and extended clearance concept
enable research scientists to put the ADME, drug-drug interactions (DDI) and
pharmacogenomics liabilities of such molcules in context and proactively
address them. This workshop will use statins and ACE inhibitors as a case
study to highlight these principles.
SC12: Introduction to Allosteric Modulators and Biased Ligands
of GPCRs
Michel Bouvier, Ph.D., Professeur, Department of Biochemistry, University
of Montréal
Stephan Schann, Ph.D., Head, Research, Domain Therapeutics SA
Allosteric modulators and biased ligands of G protein-coupled receptors
(GPCRs) represent new therapeutic paradigms for achieving more
selective activation of cellular responses. However the identification and
characterization of such GPCR-targeted compounds using standard functional
assays remain elusive due to the‘context-dependent phenomena’ of GPCRs.
This course will discuss important aspects of hit identification and validation of
allosteric modulators and biased ligands in GPCR research activity.
SC13: Introduction to Drug Metabolism
John Erve, Ph.D., DABT, Jerve Scientific Consulting, Inc.
This course is intended for chemists, biologists and scientists from related
disciplines who have an interest in furthering their understanding of drug
metabolism and its role in drug discovery and development. In addition to
some basic concepts, newer experimental approaches to drug metabolism
will be introduced such as hepatocyte models. In addition, the importance
of metabolism to drug toxicity will be explored through examining evidence
linking drug toxicity with bioactivation to reactive metabolites. Although
reactive metabolites and covalent binding has been considered a liability, there
has been a resurgence of interest in covalent modifiers and examples will
be provided.There is a growing recognition that transporters can play a role
in drug toxicity and examples will be provided. It is hoped that both novices
as well as those with more extensive exposure to drug metabolism will find
benefit in attending this course.
5. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 5
Eighth Annual October 7, 2014
Next Generation Histone Deacetylase Inhibitors Symposium*
Promising New Chemistries and Biological Strategies for Targeting HDACs
Histone deacetylases (HDACs) have proven to be a promising target for drug intervention and there are a number of HDAC inhibitors (HDACi) currently being
tested in pre-clinical and clinical stages. HDACi were primarily developed as anti-tumor agents for cancer, but many are now being explored for treating
neurodegenerative, immunologic, metabolic, inflammatory and cardiovascular disorders. However, much remains to be elucidated about the functional
implications of modulating HDACs and understanding the signaling pathways that can cause adverse cellular effects and unwanted toxicity. Cambridge
Healthtech Institute’s eighth annual event on Next Generation Histone Deacetylase Inhibitors, tracks both the scientific and clinical progress being made to
better understand the cellular function of this complex drug target family.
Suggested Event Package
October 7 Symposium: Next Generation Histone Deacetylase Inhibitors
October 8-9 Conference: Targeting Epigenetic Readers and
Chromatin Remodelers
October 9-10 Conference: Targeting Histone Methyltransferases
and Demethylases
New HDAC Chemistries and Screening Approaches
8:00 Chairperson’s Opening Remarks
Alan P. Kozikowski, Ph.D., Professor, College of Pharmacy Department of
Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago
8:10 HDAC6 Inhibitor Platform:Therapeutic Applications in
Charcot-Marie-Tooth (CMT) and Rett Syndrome
Alan P. Kozikowski, Ph.D., Professor, College of Pharmacy Department of
Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago
HDAC6 is one of the key enzymes that regulates the acetylation state of the
microtubule protein a-tubulin, and microtubule-dependent transport rates are
more efficient along acetylated a-tubulin than deacetylated a-tubulin. In addition to
facilitating anterograde transport of new cargo to synaptic zones, acetyl-tubulin also
increases the ability of damaged organelles or misfolded proteins to leave synaptic
zones.This may be very important for Rett Syndrome as well as other conditions, as
damaged mitochondria and elevated levels of improperly spliced mRNA transcripts
have been noted in MeCP2-deficient neurons.The design, synthesis, assay, and
application of HDAC6 inhibitors to various therapeutic areas will be covered.
8:40 Defining the Structural Requirements for the Design of Inter-
Class Selective HDAC Inhibitors
Edward Holson, Ph.D., Director, Medicinal Chemistry, Stanley Center for Psychiatric
Research and Director of Chemistry, Chemical Biology Platform, Broad Institute
I will describe the minimal structural requirements necessary for the potent
and selective inhibition of HDAC6 achieved through the careful choice of linker
element only. We extend these design considerations to the design of the first
inhibitors capable of potently and selectively inhibiting both HDAC6 and HDAC8
despite the fact that these isoforms belong to distinct phylogenetic classes
within the HDAC family of enzymes. Our biochemical and computational data
provide evidence that evolutionary relationships between HDACs cannot always
predict molecular recognition or ligand binding similarities.
9:10 Engaging Nuclear Receptors forTargeted Histone
Deacetylase Inhibition
Adeboyega “Yomi” Oyelere, Ph.D., Associate Professor, School of Chemistry
and Biochemistry, Georgia Institute of Technology
Histone deacetylase (HDAC) inhibition is a clinically validated strategy for
cancer treatment. Despite promises in preclinical studies, HDAC inhibitors
(HDACi) have been less efficacious in treating solid tumors. To address
this problem, my lab has designed HDACi equipped with secondary
pharmacophores to facilitate selective accumulation in malignant cells. In this
presentation, I will discuss the discovery and SAR studies on new class of
HDACi compounds targeted to breast and prostate tumors by equipping them
with the additional ability to bind to the estrogen receptor (ER) and androgen
receptor (AR) respectively.
9:40 Coffee break
10:00 Discovery of the First N-Hydroxycinnamamide-Based
Histone Deacetylase 1/3 Dual Inhibitors with Potent Oral
Antitumor Activity
Yingjie Zhang, Ph.D., Lecturer, Department of Medicinal Chemistry, School of
Pharmaceutical Sciences, Shandong University
A novel class of N-hydroxycinnamamide-based HDACs inhibitors was designed
and synthesized. In vitro activity evaluation of these compounds showed
excellent HDACs inhibition and potent growth inhibition in multiple tumor
cell lines. Relative to the approved HDACs inhibitor SAHA, our compound 11r
exhibited comparable even more potent oral anticancer activity in a human
leukemic monocyte lymphoma (U937) xenograft model. Most importantly,
our compounds exhibited marked dual HDAC1/3 selectivity over other Class I
isoforms (HDAC2 and HDAC8), Class IIa representative isoform HDAC4, Class
IIb representative isoform HDAC6 and Class IV isoform HDAC11.
10:30 Imaging HDAC Density and Drug Inhibition in the Human Brain
Jacob Hooker, Ph.D., Assistant Professor, Radiology, Harvard Medical School
Histone deacetylases have shown broad potential in treatments against
cancer and emerging data supports HDAC-targeting in the context of
cardiovascular disease and CNS dysfunction. Development of a radiotracer
for non-invasive imaging will elucidate the distribution and functional roles
of HDACs in human and accelerate medical research and drug discovery in
this domain. We have developed an HDAC imaging agent, [11C]Martinostat
for imaging HDACs in the brain, heart, kidney, pancreas and spleen to realize
these goals.
*Separate Registration Required for Next Generation Histone Deacetylase Inhibitors Symposium
6. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 6
Eighth Annual October 7, 2014
Next Generation Histone Deacetylase Inhibitors Symposium*
Promising New Chemistries and Biological Strategies for Targeting HDACs
11:00 Enjoy Lunch onYour Own
Exploring HDAC Biology
12:00 pm Chairperson’s Remarks
Wayne W. Hancock, M.D., Ph.D., Professor of Pathology and Chief of
Transplant Immunology, Children’s Hospital of Philadelphia and University of
Pennsylvania
12:10 Chemogenomic Approaches to Spatiotemporal Regulation
of HDAC Activity
Ralph Mazitschek, Ph.D., Assistant Professor, Center for Systems Biology,
Chemical Biology Platform, Massachusetts General Hospital
HDACs are master regulators of chromatin structure and function. Beyond
modulating histones acetylation they are recognized as regulators of non-histone
proteins. HDAC inhibitors have been used as tool compounds to study basic
biology and recognized as promising therapeutics. However, systemic exposure
is often not well tolerated, or does not provide the required resolution in biological
model systems.To address these shortcomings we have developed a new
approach to control HDAC activity with greater spatial and temporal resolution.
12:40 Characterization of HDAC Inhibitors: From Structural
Analysis to Cell Function
Pascal Steiner, Ph.D., Scientist, Department of Neuroscience, Genentech, Inc.
A detailed understanding of how HDAC inhibitors with different pharmacological
properties affect biological functions in vitro and in vivo is still missing. I will
present our recent findings showing the evaluation of HDAC inhibitors potency
in vitro using recombinant proteins and of their pharmacodynamic properties
as measured with histone acetylation are insufficient to predict their functional
consequences on biological activity such as gene expression and cell viability
and therefore might be misleading in identifying useful HDACi.
1:10 Immuno-Modulatory Function of HDAC6 andTubulinAcetylation
Tso-Pang Yao, Ph.D., Associate Professor, Department of Pharmacology and
Cancer Biology, Duke University
HDAC inhibitors show an anti-inflammatory activity. The underlying mechanism
is not well understood. The potential toxicity associated with pan-HDAC
inhibitors also presents a barrier for their chronic use in inflammatory disease.
We will discuss different anti-inflammatory phenotypes induced by HDAC
inhibitors and offer mechanistic basis for differential therapeutic effects and
opportunities for targeting selective HDAC members.
1:40 Coffee break
2:00The Roles of Class I HDACs in Alzheimer’s Disease
Li-Huei Tsai, Ph.D., Professor of Neuroscience, Department of Brain and
Cognitive Sciences and Director, Picower Institute for Learning and Memory,
Massachusetts Institute of Technology
Impaired genome integrity has been implicated in aging and in neurodegenerative
diseases such as Alzheimer’s disease (AD). Our work suggests that the
accumulation of DNA damage occurs early in AD pathophysiology, and that
this contributed to disease progression. In two separate studies, we found that
HDAC1 plays an important role in DNA damage repair and that its reduced activity
is correlated with neurodegeneration. Furthermore, HDAC1 may also directly
regulate the production and clearance of beta-amyloid.Thus targeting HDAC1 may
be beneficial for treatment of neurodegenerative disorders.
2:30 Discrete and Novel Immunologic Roles of Individual Class I
HDAC Enzymes
Wayne W. Hancock, M.D., Ph.D., Professor of Pathology and Chief ofTransplant
Immunology, Children’s Hospital of Philadelphia and University of Pennsylvania
In the same way that one size doesn’t fit all, it may not be desirable to try
and efficiently block all class I HDAC enzymes. I will present data comparing
the differing roles of class I enzymes in the immune system using genetic
and pharmacologic approaches. While there is some redundancy and ability
to compensate, HDAC1 and HDAC2 play distinct roles and their deletion has
differing effects, as does targeting of HDAC3 and HDAC8. Our data point to
the potential for major advances in therapeutics if, and as, the ability to target
individual class I isoforms is achieved.
3:00 Sponsored Presentation (Opportunity available)
3:30 Session Break
Evaluating Pan v/s Isoform-Specific Inhibitors
3:45 Chairperson’s Remarks
Simon Jones, Ph.D., Vice President, Biology and Preclinical Development,
Acetylon Pharmaceuticals
3:50 Clinical Potential of Isoform Selective HDAC Inhibitors
Simon Jones, Ph.D., Vice President, Biology and Preclinical Development,
Acetylon Pharmaceuticals, Inc.
There has been resurgence of activity in developing selective HDAC
inhibitors for the clinic. The use of selective inhibitors with genetic models
has substantially added to the basic biology of roles for HDACs regulating
acetylation states histone and non-histone protein substrates. The potential for
ricolinostat, a selective HDAC6 inhibitor, in multiple myeloma, highly selective
HDAC6 inhibitors for neurological indications, and targeting HDAC1,2 in
β-thalassemia and cellular differentiation in cancer will be discussed.
4:20 HDAC10 Controls Autophagy-Mediated Drug Resistance
Olaf Witt, M.D., Professor for Pediatric Oncology, Hematology and
Immunology Head, CCU Pediatric Oncology German Cancer Research Center
Head, Section Pediatric Brain Tumors, Department of Pediatric Oncology,
Hematology and Immunology, University Children’s Hospital
Pediatric neuronal cancers have been instructive in defining oncogenic functions
*Separate Registration Required for Next Generation Histone Deacetylase Inhibitors Symposium
7. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 7
Eighth Annual October 7, 2014
Next Generation Histone Deacetylase Inhibitors Symposium*
Promising New Chemistries and Biological Strategies for Targeting HDACs
of HDAC isoforms including HDACs 8, 5 and 9. Recently, we have identified a
novel non-epigenetic function of HDAC10 in controlling autophagy-mediated drug
resistance.Targeting of HDAC10 inhibits autophagic flux and restores sensitivity
of neuroblastoma to chemotherapy. Moreover, high level of HDAC10 expression is
associated with poor clinical outcome. We will discuss molecular mechanisms of
the HDAC10-autophagy-axis and potential options for isoform selective inhibition.
4:50 Coffee Break
5:10Targeting HDACs in Cardiovascular Disease
Timothy A. McKinsey, Ph.D., Associate Professor and Associate Division Head
for Translational Research, Department of Medicine, Division of Cardiology,
University of Colorado Denver
Efficacy of small molecule HDAC inhibitors has been demonstrated in animal
models of heart failure, where the compounds block cardiac hypertrophy and
fibrosis and improve systolic and diastolic function. Since the pharmacological
inhibitors used in the pre-clinical heart failure studies target 11 distinct HDAC
enzymes, the identity of the HDAC isoform(s) that controls pathological responses
of the heart unknown. I will present our recent data from studies of isoform-
selective HDAC inhibitors and HDAC knockout mice in models of cardiac disease.
5:40 Sponsored Presentation (Opportunity available)
»»5:55 FEATURED PRESENTATION: CHEMICAL
MODULATION OF CHROMATIN STRUCTURE AND
FUNCTION
James E. Bradner, M.D., Assistant Professor, Department of Medicine,
Harvard University Medical School and Staff Physician, Division of
Hematologic Malignancies, Dana-Farber Cancer Institute
With an interest in understanding chromatin-dependent signal transduction to
RNA polymerase in developmental and disease biology, we and others have
undertaken to discover and optimize small molecule modulators of chromatin
regulatory factors. These incisive chemical probes have availed new insights
into chromatin structure and function, and suggest plausible translational
opportunities for the targeted development of drug-like derivatives in cancer
and non-malignant indications. New biotechnologies have been created which
allow the rapid identification of critical regulatory regions underlying cell state
and which provide the first genome-wide maps of spatial localization of drug
molecules within the epigenome. Discussed in this lecture will be mechanistic
and translational efforts to modulate gene regulatory pathways of lysine
acetylation in cancer transcriptional signaling.
6:30 Close of Symposium
*Separate Registration Required for Next Generation Histone Deacetylase
Inhibitors Symposium
GET CONNECTED!
Maximize your experience on-site at
Discovery OnTarget 2014!
The Intro-Net offers you the opportunity to
set up meetings with selected attendees
before, during and after this conference,
allowing you to connect to the key people
you want to meet. This online system
was designed with your privacy in mind
and is available only to registered session
attendees of this event. Registered
conference attendees will receive more
information on accessing the Intro-Net in the
weeks leading up to the event!
Join the Discovery
On Target Group
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PRESENT A POSTER AND SAVE $50!
Cambridge Healthtech Institute encourages attendees
to gain further exposure by presenting their work in
the poster sessions. To secure a poster board and
inclusion in the conference materials, your abstract
must be submitted, approved and your registration
paid in full by August 8, 2014.
• Your poster will be available to 900+ delegates
• You’ll automatically be entered into our poster
competition where two winners each will receive
an American Express Gift Certificate
• $50 off your registration fee
• Your research will be seen by leaders from
pharmaceutical, biotech, academic and
government institutes
Discovery onTarget Student Fellowship
Full time graduate students and PhD Candidates
are encouraged to apply for the Discovery on Target
Student Fellowship. Interested students must
complete an online application for the 2014 Student
Fellowship. Applications are due by July 25, 2014.
How Students Benefit from Presenting a Poster:
1. ShowcaseYour Research to 900+ Attendees: Within
the expansive Exhibit Hall stand by your poster and
network with attendees. Distribute copies of journal
articles or papers you have authored or contributed to.
2. Start a Future Collaboration and Meet a Potential
Employer: Collect business cards and meet prospective
collaborators who may be actively pursuing work in
your field. Put together a short outline of the field(s)
in which you seek collaborators or new professional
challenges, and distribute those to the people
you meet.
3. Expand Your Network: When you return to school/
lab, add each person you meet to your LinkedIn
connections. Keep in touch to share new ideas that
may advance your own research or stature in the
scientific community.
8. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 8
Second Annual October 8 - 9, 2014
Targeting Epigenetic Readers and Chromatin Remodelers
Drugging the “Undruggable”
Operating at the interface of translating histone marks, reader domains that recognize the histone code written in acetyl and methyl marks have now emerged
as viable targets for therapeutic development. In particular, the BET bromodomain family of readers has gained significant attention for the treatment of human
cancers, with several inhibitors developed and clinical-stage programs now underway. Cambridge Healthtech Institute’s Second Annual Targeting Epigenetic
Readers and Chromatin Remodelers meeting will unite leading academic and industry researchers for the development of chemical probes and inhibitors to
further our understanding of the therapeutic opportunities associated with targeting reader domains and chromatin remodeling.
Suggested Event Package
October 7 Short Course: Targeting Protein-Protein Interactions
October 7 Short Course: Introduction to Targeted Covalent Inhibitors
October 8-9 Conference: Targeting Epigenetic Readers and
Chromatin Remodelers
October 9-10 Conference: Targeting Histone Methyltransferases
and Demethylases
WEDNESDAY, OCTOBER 8
7:00 am Registration and Morning Coffee
DEVELOPING NOVEL BROMODOMAIN INHIBITORS
8:05 Chairperson’s Opening Remarks
Ming-Ming Zhou, Ph.D., Harold and Golden Lamport Professor and Chairman,
Department of Structural & Chemical Biology; Co-Director, Experimental
Therapeutics Institute, Icahn School of Medicine at Mount Sinai
»»8:15 FEATURED PRESENTATION:TARGETING GENE
EXPRESSION: SELECTIVE VS. PROMISCUOUS
BROMODOMAIN INHIBITION
Panagis Filippakopoulos, Ph.D., Principal Investigator, Bromodomains, Structural
Genomics Consortium & Ludwig Institute for Cancer Research, Nuffield
Department of Clinical Medicine, University of Oxford
I will present our efforts to identify novel inhibitors of BRDs that are site
selective (in the case of BET bromodomains) as well as our efforts to destroy
selectivity while retaining affinity outside the BET family (i.e., promiscuous
inhibitors). I will be covering the development and characterization of these
tool compounds as well as their properties targeting gene expression in
diverse cellular systems, seeking to validate BRD function.
9:00 Selective Modulation of Bromodomains in Gene Activation
Ming-Ming Zhou, Ph.D., Harold and Golden Lamport Professor and Chairman,
Department of Structural & Chemical Biology; Co-Director, Experimental
Therapeutics Institute, Icahn School of Medicine at Mount Sinai
In this talk I will present my group’s latest study of structural mechanism
and function of bromodomain proteins in gene transcriptional activation
using newly designed, highly selective bromodomain inhibitors. I will discuss
the functional implications of their new findings of basic principles that
govern the molecular interactions and regulation in gene expression, and
a new strategy for developing targeted epigenetic therapy for cancer and
chronic inflammation.
9:30 Development and Utilities of BET Bromodomain Inhibitors
with High CNS Exposure
Claes Wahlestedt, M.D., Ph.D., Leonard M. Miller Professor & Associate Dean,
Therapeutic Innovation, Miller School of Medicine, University of Miami
Published bromodomain inhibitors show insufficient in vivo CNS exposure
due to a variety off issues. In collaboration with Epigenetix, Inc. we therefore
developed novel small molecules, such as EP11313, with characteristics
of CNS active drugs. These compounds have to date primarily been tested
in various models of glioblastoma. However, they have also been useful in
demonstrating a role for BET bromodomain proteins as novel epigenetic
regulators of cocaine-induced behavioral plasticity.
10:00 Grand Opening Coffee Break in the Exhibit Hall with Poster
Viewing
10:45 Discovery of Selective BRD4 Bromodomain Inhibitors by
Fragment-Based High-Throughput Docking
Dimitrios Spiliotopoulos, Ph.D., Senior Research Scientist, Biochemistry,
University of Zurich
Using a fragment-based in silico screening approach, we identified two small
molecules that selectively bind to the first bromodomain of BRD4 with low-
micromolar affinity and favorable ligand efficiency (0.37 kcal/mol per non-
hydrogen atom). Notably, the hit rate of the fragment-based in silico approach
is about 10% as only 24 putative inhibitors, from an initial library of about 10
million molecules, were tested in vitro.
11:15 Development and Application of BET and CREBBP
Bromodomain Ligands
Stuart Conway, Ph.D., Associate Professor, Chemistry, University of Oxford
I will present our work on the development of small molecule ligands for
the BET bromodomain. I will describe our understanding of the SAR for BET
bromodomain binding and our work to optimise the structure of our ligands
both for potency and metabolic stability for use in vivo. I will also present our
work on the development of a novel class of CREBBP ligands and describe
what these compounds have taught us about the requirements for CREBBP
bromodomain binding.
9. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 9
Second Annual October 8 - 9, 2014
Targeting Epigenetic Readers and Chromatin Remodelers
Drugging the “Undruggable”
11:45 A Novel Chemical Probe for Family VIII Bromodomains
Dafydd Owen, Ph.D., Associate Research Fellow, Medicinal Chemistry,
Biotherapeutics Worldwide R&D, Pfizer
BRG1 (SMARCA4) and BRM (SMARCA2) are the central ATPase components
of the multi-component complexes. BRG1 and BRM are multi-domain
proteins that contain a number of DNA and protein interaction modules.
These include C-terminal bromodomains. Through collaboration with the
SGC we have identified a chemical probe that interacts with just three of the
Family VIII bromodomains - BRG1, BRM and PB1(5). The discovery, binding
mode and phenotype derived from the use of PFI-3 will be discussed.
12:15 pm Sponsored Presentations (Opportunities Available)
12:45 Session Break
1:00 Luncheon Presentation (Sponsorship Opportunity Available) or
Lunch onYour Own
1:40 Session Break
MOLECULAR MECHANISMS IN CANCER
1:50 Chairperson’s Opening Remarks
Dafydd Owen, Ph.D., Associate Research Fellow, Medicinal Chemistry,
Biotherapeutics Worldwide R&D, Pfizer
2:00 Role of BRD4 and SWI/SNF in the Maintenance of Acute
Myeloid Leukemia
Chris Vakoc, M.D., Ph.D., Assistant Professor, Cold Spring Harbor Laboratory
Our lab has employed negative-selection shRNA screening to identify
chromatin regulator dependencies in a mouse model of acute
myeloidleukemia. These studies have identified Brd4 and SWI/SNF as
among the top dependencies in this disease, which exhibit several desirable
properties for therapeutic targeting. Recent work will be presented that
seeks to understand the molecular mechanism of these chromatin regulators
that underlies their role in cancer maintenance.
2:30Targeting Bromodomains in NUT Midline Carcinoma
Christopher A. French, M.D., Assistant Professor, Department of Pathology,
Harvard Medical School; Assistant Professor, Pathology, Brigham and
Women’s Hospital
I will first discuss the basic clinical aspects of NUT midline carcinoma. I will
then discuss three aspects of how BRD4-NUT blocks differentiation and
promotes growth of affected cancer cells. Next, I will present recent findings
that reveal the chromatin regions bound by BRD4-NUT, as well as NSD3,
which we recently found to be a variant fusion partner of NUT in a subset of
NUT midline carcinomas. Finally, I will discuss recent progress using BET
bromodomain inhibitors.
3:00 Sponsored Presentations (Opportunities Available)
3:30 Refreshment Break in the Exhibit Hall with PosterViewing
4:10Treating Genetically Diverse Glioblastoma with
Bromodomain Inhibitors
Jialiang Wang, Ph.D., Assistant Professor, Neurological Surgery, Vanderbilt
University
Glioblastoma is a genetically heterogeneous disease. Yet, a wide range of
glioblastoma tumors of diverse genotypes exhibited significant sensitivity
to BET bromodomain inhibitors. I will discuss in vitro and in vivo activities
of BET bromodomain inhibitors in glioblastoma primary samples. Molecular
mechanisms underlie the oncogenic activities of BET proteins in glioblastoma
will be discussed.
4:40 Betting on BETs for Advanced Prostate CancerTreatment
Irfan Asangani, Ph.D., Research Investigator, Pathology, Michigan Center for
Translational Pathology, University of Michigan
Maintenance of AR signaling is the most common resistance mechanism
that patients with advanced prostate cancer develop after conventional
hormonal treatments. Recently, selective small molecule inhibitors that
target the bromodomains of BET family proteins have been shown to exhibit
anti-proliferative effects in a range of malignancies. I will present our findings
offering a preclinical proof of principle for the use of BET-bromodomain
inhibitors that block AR signaling.
5:10 Interactive Breakout Discussion Groups (see website for
details)
6:10 Welcome Reception in the Exhibit Hall with Poster Viewing
7:15 Close of Day
THURSDAY, OCTOBER 9
7:30 am Registration and Morning Coffee
EVALUATINGTHERAPEUTIC POTENTIAL
8:00 Chairperson’s Opening Remarks
Claes Wahlestedt, M.D., Ph.D., Leonard M. Miller Professor & Associate
Dean, Therapeutic Innovation, Miller School of Medicine, University of Miami
10. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Second Annual October 8 - 9, 2014
Targeting Epigenetic Readers and Chromatin Remodelers
Drugging the “Undruggable”
8:10Targeting BET Bromodomains for CancerTreatment
Bernard Haendler, Ph.D., Senior Scientist, Global Drug Discovery, Bayer
Pharma AG
BRD4 belongs to the BET bromodomain family and represents an
interesting target for the treatment of various pathologies, including cancer.
Pharmacological in vitro and in vivo data on the activity of potent, selective
BET inhibitors in tumor cell lines and in xenografts will be presented. In
addition, the impact of individual point mutations in the BRD4 bromodomain
on inhibitor and acetylated histone peptide binding will be discussed.
8:40 Epigenetic Control ofT-Cell Biology
Jose M. Lora, Ph.D., Executive Director, Preclinical Sciences, Constellation
Pharmaceuticals
In my talk I will discuss some of our research, elucidating how chromatin
regulators and epigenetic factors are intimately involved in T-cell lineage
commitment and function, and how their functional inhibition could lead to
novel therapeutic opportunities.
9:10 Inhibition of BET Bromodomain Proteins as aTherapeutic
Approach in Prostate Cancer
Anastasia Wyce, Ph.D., Investigator, R&D Oncology, GlaxoSmithKline
9:40 Coffee Break in the Exhibit Hall with Poster Viewing
ASSESSINGTOXICITIES
10:30 Multifocal Defects in the Hematopoietic and Lymphoid
Compartments in Mice Dosed with a Broad BET Inhibitor
Dong Lee, Ph.D., Scientist, Safety Assessment, Genentech
The safety profile of BET inhibition is largely unknown. Our study shows
that mice treated with JQ1, a broad BET small molecule, at efficacious
concentrations develop multifocal defects in the lymphoid and immune cell
compartments. In addition JQ1 at higher concentrations are not tolerated.
This toxicity study establishes a baseline safety signal for JQ1 and begs
the question of whether these findings are related to specific BET isoform
inhibition or caused by secondary pharmacology from JQ1.
11:00 Bromodomain and ExtraTerminal (BET) Domain Inhibitors
Induce a Loss of Intestinal Stem Cells andVillous Atrophy
Peter Newham, Ph.D., Global Head, Discovery Safety, R&D Innovative
Medicines, AstraZeneca
The molecular and cellular mechanisms behind BET inhibitor gastrointestinal toxicity
have yet to be elucidated.We have found that BET inhibitors induce a dose-limiting
duodenal villous atrophy in vivo, accompanied by inappetance and weight loss. Ex
vivo cultures of intestinal organoids confirm that villous atrophy occurs with multiple
chemical classes of BET inhibitors and that toxicity is driven by their primary
pharmacology.We find instead inhibitors induce a loss of intestinal stem cells.
11:30 Enjoy Lunch onYour Own
1:00 pm Plenary Keynote Session (see website for details)
2:45 Refreshment Break in the Exhibit Hall with Poster Viewing
3:45 Close of Conference
Discovery on Target | 10
11. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 11
Second Annual October 8 - 9, 2014
Targeting the Ubiquitin Proteasome System
Exploring the Therapeutic Potential of Ubiquitin Ligases and Deubiquitinases (DUBs)
The ubiquitin proteasome system (UPS) is an essential and highly regulated mechanism operating to tightly control intracellular protein degradation and turnover.
It is therefore no surprise that emerging strategies in drug discovery moving away from single-target approaches are shifting toward targeting multicomponent
cellular machineries such as the UPS to elicit therapeutic response in complex disease. Following the approval of two proteasome inhibitors, significant progress
has been made in our understanding of ubiquitin biology along with the emergence of novel technologies and strategies enabling the development of small
molecules targeting specific UPS components. Thus, modulating ligases within the ubiquitination cascade and “rescue” deubiquitinases (DUBs) have gained
significant interest in drug discovery.
Suggested Event Package
October 7 Short Course: Targeting Protein-Protein Interactions
October 7 Short Course: Introduction to Targeted Covalent Inhibitors
October 8-9 Conference: Targeting the Ubiquitin Proteasome System
October 9-10 Conference: Maximizing Efficiency in Discovery
WEDNESDAY, OCTOBER 8
7:00am Registration and Morning Coffee
DIVERSE STRATEGIES MODULATINGTHE UPS &
PROTEIN DEGRADATION
8:05 Chairperson’s Opening Remarks
Ben Nicholson, Ph.D., Senior Director, R&D, Progenra, Inc.
»»8:15 FEATURED PRESENTATION: INDUCING PROTEIN
DEGRADATION AS ATHERAPEUTIC STRATEGY
Craig M. Crews, Ph.D., Lewis B. Cullman Professor of Molecular, Cellular, and
Developmental Biology; Professor Chemistry & Pharmacology, Yale University
Induced protein degradation offers a novel, catalytic mechanism to irreversibly
inhibit protein function, namely, the intracellular destruction of target proteins.
This is achieved via recruitment of target proteins to the cellular quality
control machinery, i.e., the Ubiquitin/Proteasome System (UPS). For the past
decade, we have focused on developing different strategies for inducing
selective protein degradation, including the Proteolytic Targeting Chimera and
Hydrophobic Tagging.
9:00 Pharmacological Activators ofTumor Suppressor PTEN
Alexander Statsyuk, Ph.D., Assistant Professor, Department of Chemistry,
Northwestern University
We developed a novel fragment-based drug discovery platform, and used it to
discover first in class mechanism based covalent inhibitor of Nedd4-1 ubiquitin
ligase, which degrades tumor suppressor PTEN. The developed drug discovery
platform is generally applicable to discover covalent drug leads for E1, E2, E3
enzymes and DUBs (~800 known enzymes). Our findings are conceptually
novel and will be of significant interest to the drug discovery community.
9:30 Substrate-Assisted Inhibition of Ubiquitin-Like Protein
Activation
Lawrence Dick, Ph.D., Director, Biochemistry, Oncology Drug Discovery Unit,
Takeda Pharmaceuticals International Co.
We have identified small molecule inhibitors of ubiquitin-like protein (Ubl)
activating enzymes (E1’s) that work by a novel form of mechanism-based
inhibition. These molecules serve as tools to probe the biological functions
of individual Ubl conjugation pathway. To date our efforts have yielded
two investigational drugs of this class that have entered into clinical trials;
MLN4924, an inhibitor of the Nedd8 conjugation pathway; and MLN7243, an
inhibitor of the ubiquitin conjugation pathway.
10:00 Grand Opening Coffee Break in the Exhibit Hall with Poster
Viewing
10:45Targeting Ring1B-Bmi1 E3 Ubiquitin Ligase Activity
Tomasz Cierpicki, Ph.D., Assistant Professor, Pathology, University of Michigan
Small molecule inhibitors of Ring1B-Bmi1 E3 ligase activity are highly desired
as potential agents targeting cancer stem cells. Targeting the Ring E3 ligases
with small molecules is a challenging task due to the lack of well-defined
substrate binding pocket and a complex biochemical assay required for
enzymatic activity studies. To identify small molecule inhibitors of Ring1B-
Bmi1 we performed fragment-based screening using NMR. I will present
development of potent Ring1B-Bmi1 inhibitors.
11:15 Discovery of a Selective p97 Inhibitor that Disrupts Protein
Homeostasis in vitro and Has Antitumor Activity in Vivo
Han-Jie Zhou, Ph.D., Director, Chemistry, Cleave BioSciences
Herein we reported the discovery of a selective and potent p97 inhibitor which
demonstrated effects on tumor cell markers of protein homeostasis related to
UPS inhibition and survival in vitro. After oral dosing this compound affected
pharmacodynamic markers of UPS activity in vivo as well as antitumor activity
in a xenograft model. Together these studies validate p97 as a druggable target
with potential antitumor activity.
12. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 12
Second Annual October 8 - 9, 2014
Targeting the Ubiquitin Proteasome System
Exploring the Therapeutic Potential of Ubiquitin Ligases and Deubiquitinases (DUBs)
11:45 Small MoleculesTargeting Integrity of the 26S Proteasome
Assembly
Pawel Osmulski, Ph.D., Assistant Research Professor, Molecular Medicine,
The University of Texas Health Science Center at San Antonio
Clinically recognized inhibitors used to treat aggressive blood cancers are
directly targeting catalytic sites of the core. We developed a set of small
molecules disabling the proteasome with an entirely different mechanism: by
targeting interactions between the catalytic core and its regulatory modules
and by allosterically inhibiting the core. In a proof-of principle studies one of
our compounds disables degradation of polyubiquitinylated substrates and
induces apoptosis in cancer cells.
12:15 pm Sponsored Presentations (Opportunities Available)
12:45 Session Break
1:00 Luncheon Presentation (Sponsorship Opportunity Available) or
Lunch onYour Own
1:40 Session Break
TARGETING DUBs: NOVEL APPROACHES, CHEMICAL
MATTER AND LEAD OPTIMIZATION
1:50 Chairperson’s Opening Remarks
Lawrence Dick, Ph.D., Director, Biochemistry, Oncology Drug Discovery Unit,
Takeda Pharmaceuticals International Co.
2:00Targeting DUBs by Chemoproteomic Inhibitor Profiling in
Cancer Cells
Benedikt Kessler, Ph.D., University Research Lecturer, Ubiquitin Proteolysis
Group, Target Discovery Institute, Nuffield Department of Medicine, University
of Oxford
We have utilized chemical proteomics and ubiquitin-based active site probes
to determine the potency and selectivity of deubiquitylating enzyme (DUB)
inhibitors in cell culture models. This approach is now being combined with
the application of unbiased molecular probes that allowed detection of
endogenous active nucleophile-dependent enzymatic activities in cell extracts
by direct isotope-label based mass spectrometric quantitation to discover a
broad range of small molecule cellular targets.
2:30 A Selective USP1/UAF1 Deubiquitinase Inhibitor Modulates
the DNA Damage Response In Humans
Zhihao Zhuang, Ph.D., Associate Professor, Department of Chemistry &
Biochemistry, University of Delaware
DUBs, as a promising therapeutic target class, have attracted increasing
interest in inhibitor discovery. We conducted a quantitative high-throughput
screening (qHTS) against USP1/UAF1 and a subsequent lead optimization.
We obtained a reversible inhibitor that displays nanomolar inhibition and
excellent selectivity towards USP1/UAF1. The USP1/UAF1 inhibitor disrupts
cellular DNA damage tolerance and repair pathways, i.e. Fanconi Anemia (FA)
and DNA translesion synthesis (TLS). Our study suggested a new strategy of
inhibiting deubiquitinases.
3:00 Sponsored Presentations (Opportunities Available)
3:30 Refreshment Break in the Exhibit Hall with Poster Viewing
4:10 Identification of Selective DUB InhibitorsTargeting DDR
DeficientTumors
Niall Martin, Ph.D., COO, MISSION Therapeutics Ltd.
In cancer cells, loss of one DDR pathway leads to dependency on the
remaining DDR pathways for survival. Inhibition of these remaining pathways
causes synthetic lethality (SL), a powerful mechanism for selectively targeting
cancer. By systematically knocking down all deubiquitylating enzymes (DUBs)
in isogenic models of DDR deficiencies, we identified SL interactions in
genetic backgrounds including ATM-, ATR- and BRCA2. These results have
been “phenocopied” using novel inhibitors identified.
4:40 Small Molecule Inhibitors of the Deubiquitinase USP7
Interfere with Ubiquitin Binding
Ingrid E. Wertz, Ph.D., Scientist & Project Team Leader, Department of Early
Discovery Biochemistry, Genentech
5:10 Interactive Breakout Discussion Groups (see website for
details)
6:10 Welcome Reception in the Exhibit Hall with Poster Viewing
7:15 Close of Day
THURSDAY, OCTOBER 9
7:30 am Registration and Morning Coffee
BEYOND ONCOLOGY: DISCOVERY OF BIOACTIVE
COMPOUNDS
8:00 Chairperson’s Opening Remarks
Niall Martin, Ph.D., COO, MISSION Therapeutics Ltd.
8:10 Selective Inhibition of the Proteasome-Associated
Deubiquitinating Enzyme USP14
Daniel Finley, Ph.D., Professor, Cell Biology, Harvard Medical School
Small-molecule inhibitors of the deubiquitinating enzyme Usp14 were obtained
via HTS. The compounds enhance degradation of various proteins and may
13. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Second Annual October 8 - 9, 2014
Targeting the Ubiquitin Proteasome System
Exploring the Therapeutic Potential of Ubiquitin Ligases and Deubiquitinases (DUBs)
have therapeutic applications for proteopathies. Proteasome substrates vary
dramatically in their susceptibility to Usp14 inhibition, and surprisingly Usp14
will not act on tested substrates when only a single ubiquitin chain is present
on the substrate. This principle of selectivity is to our knowledge novel for a
deubiquitinating enzyme.
8:40 Small-Molecule Inhibition of JAK-STAT Signaling through
the Deubiquitinase USP9X
Bridget Wagner, Ph.D., Director, Pancreatic Cell Biology, Center for the
Science of Therapeutics, Broad Institute
Using phenotypic screening, we identified a small-molecule suppressor of
beta-cell apoptosis. MOA studies revealed that our top compound binds
USP9X and interferes with JAK-STAT signaling induced by IFN-gamma
stimulation. Phenotypic screening, followed by comprehensive MOA efforts,
can provide novel mechanistic insights into ostensibly well-understood cell
signaling pathways. Furthermore, this study suggests USP9X as a novel
target for regulating JAK2 activity in cellular inflammation.
9:10 Idolizing Ubiquitin: NovelTherapies toTreat Cardiovascular
Disease
Ben Nicholson, Ph.D., Senior Director, R&D, Progenra, Inc.
Here we report that using our UbiProTM drug discovery platform we have
discovered novel inhibitors of the E3 ligase IDOL that modulate cellular
cholesterol homeostasis. The most promising compounds were used
as starting points to develop novel drug like molecules and the efficacy
of the lead compounds is being evaluated in translational models of
hypercholesterolemia. Data will be presented summarizing our progress to
date targeting IDOL for the treatment of hypercholesterolemia.
9:40 Coffee Break in the Exhibit Hall with Poster Viewing
DISRUPTING PPIs OF E3 LIGASES
10:30The Discovery of Small MoleculesTargeting the VHL E3
Ubiquitin Ligase and Disrupting its Protein-Protein Interaction
with HIF-alpha Subunit
Alessio Ciulli, Ph.D., Reader, Chemical & Structural Biology, College of Life
Sciences, University of Dundee
We have discovered drug-like small molecules that target the ubiquitin
proteosome system by disrupting, with nanomolar potencies, the key
interaction between the von Hippel-Lindau protein cullin ring E3 ligase and
with the Hypoxia Inducible Factor alpha subunit. Structure-based design
informed by co-crystal structures and biophysical binding assays guided the
medicinal chemistry optimization. Our efforts combined peptidomimetic
strategies with fragment-based deconstructive analyses.
11:00Targeting the MDM2-p53 Protein-Protein Interaction for
New CancerTherapeutics
Shaomeng Wang, Ph.D., Director, Center for Discovery of New Medicines;
Warner-Lambert/Parke-Davis Professor, Medicine, Pharmacology and
Medicinal Chemistry, University of Michigan Comprehensive Cancer Center
Blocking the MDM2-p53 protein-protein interaction is being pursued as a new
cancer therapeutic strategy. Our laboratory has designed and developed a class of
highly potent and specific small-molecule inhibitors to block the MDM2-p53 PPI
(MDM2 inhibitors). I will present our structure-based design and optimization of our
MDM2 inhibitors and extensive preclinical studies of SAR405838 (MI-77301), which
is now in phase I clinical development for the treatment of human cancers.
11:30 Enjoy Lunch onYour Own
1:00 pm Plenary Keynote Session (see website for details)
2:45 Refreshment Break in the Exhibit Hall with Poster Viewing
3:45 Close of Conference
Discovery on Target | 13
Interactive Breakout Discussion Groups
This interactive session provides conference delegates and speakers an opportunity to choose a specific roundtable discussion group to join. Each group has a
moderator to ensure focused discussions around key issues within the topic. This format allows participants to meet potential collaborators, share examples from
their work, vet ideas with peers, and be part of a group problem-solving endeavor. The discussions provide an informal exchange of ideas and are not meant to be a
corporate or specific product discussion. The Interactive Breakout Discussion Groups take place across all programs and will be held either on Wednesday, October
8 from 5:10-6:10 pm or Friday, October 10 from 8:00-9:00 am.
14. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 14
Inaugural October 8 - 9, 2014
Big Data Analytics and Solutions
Using Big Data to Identify New Targets for Drug Discovery
According to the McKinsey Global Institute, applying big-data strategies to better inform decision making could generate up to $100 billion in value annually
across the US health-care system, by optimizing innovation, improving the efficiency of research and clinical trials, and building new tools for physicians,
consumers, insurers, and regulators to meet the promise of more individualized approaches. Effectively utilizing big-data opportunities can help biopharma
companies better identify new potential drug candidates and develop them into effective, approved and reimbursed medicines more quickly. This potential
cannot be unlocked without addressing key issues including collection of low throughput, poor quality data; the ever-growing complex and disparate datasets;
scalability; bioinformatics tools not integrated; disparate analysis and visualization tools; revisiting analysis workflow; streamlining computational infrastructure;
and identifying multiple drug targets (not just single drug targets) to work together as a network.
Through lectures and panel discussions, Cambridge Healthtech Institute’s Big Data Analytics and Solutions Conference will bring together leading researchers
and thought leaders to discuss the significant role that big data has on drug design to identify biomarkers and discover targets for potential therapies.
Suggested Event Package
October 7 Short Course: Designing Scalable Software Systems for Big
Data Analytics
October 7 Short Course: Setting Up Effective RNAi Screens: From
Design to Data to Validation
October 7 Short Course: A Primer to Gene Editing: Tools
and Applications
October 8-9 Conference: Big Data Analytics and Solutions
October 9-10 Conference: Maximizing Efficiency in Discovery
WEDNESDAY, OCTOBER 8
7:00 am Registration and Morning Coffee
RIGHT DRUG, RIGHTTARGET: ROLE OF BIG DATA ON
DRUG DESIGNTO IDENTIFY POTENTIALTHERAPIES
8:05 Chairperson’s Opening Remarks
Michael Liebman, Ph.D., Managing Director, IPQ Analytics, LLC
8:15 Disease and Big (NGS) Data: Searching for Needles in
Needlestacks
Joseph D. Szustakowski, Ph.D., Senior Group Head, Novartis Institutes for
BioMedical Research
9:00 Big Data:We May Have the Right Drugs, but Do We Have the
RightTargets?
Michael Liebman, Ph.D., Managing Director, IPQ Analytics, LLC
Drug development targets the proposed molecular mechanism associated
with a disease but in much of medicine, accurate definition/diagnosis of the
disease or phenotype is lacking. We focus on applying big data to understand
the complexity of the disease to both improve clinical decision making/patient
care and drug development, particularly in complex diseases and syndromes.
Our approach uniquely starts with clinical need rather than data generation.
9:30 Rapid Drug Repositioning by Combining High-Throughput
Experiments and Publicly Available Datasets
Blake Borgeson, Co-Founder and CTO, Recursion Pharmaceuticals
This talk will describe integrating various sources of data from both data-
intensive high-throughput experiments and large public datasets such as
the Connectivity Map project. A practical evaluation of the ways in which
these sources can be integrated to support drug repositioning efforts will be
discussed. Additionally, the talk will describe relevant challenges and pitfalls of
combining public datasets with in-house experimental results.
10:00 Grand Opening Coffee Break in the Exhibit Hall with Poster
Viewing
BIG DATA APPROACHES ACROSS
MULTIPLE RESEARCH INITIATIVES
10:45 Cell-Based Assays for DrugTarget Discovery: Lessons from
Transcriptomic Studies With Human Lymphoblastoid Cell Lines
David Gurwitz, Ph.D., Director, National Laboratory for the Genetics of Israeli
Populations, Human Molecular Genetics and Biochemistry, Sackler Faculty of
Medicine, Tel-Aviv University
Genome-wide pharmacogenomic studies for developing targeted therapies
offer the advantage of hypothesis-free search for tentative drug response
biomarkers (efficacy and safety). However, they require large patient cohorts and
are therefore very costly.This talk presents our experience with an alternative
approach, based on genome-wide transcriptomic profiling of a panel of human
lymphoblastoid cell lines (LCLs) representing unrelated healthy donors.
11:15 Supporting Data and Development Strategy for ALZ-801:
Derisked, Close-to-Market Product for SymptomaticTreatment of
Alzheimer’s Disease
Martin Tolar, M.D., Ph.D., Founder, President & CEO, Alzheon, Inc.
This presentation describes data and development strategies that Alzheon is
using to build market leadership in Alzheimer’s disease with ALZ-801. ALZ-801
has the potential to be one of the first new treatments for Alzheimer’s in
over a decade. ALZ-801 is a prodrug of tramiprosate, an inhibitor of amyloid
aggregation and neurotoxicity, with demonstrated efficacy and safety in Phase
3 in the ApoE4 positive patient subgroup.
15. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 15
Inaugural October 8 - 9, 2014
Big Data Analytics and Solutions
Using Big Data to Identify New Targets for Drug Discovery
11:45 From Big Data to Smart Data: Using Quantitative Systems
Pharmacology for De-risking R&D Projects in CNS R&D
Hugo Geerts, Ph.D., CSO, Computational Neuropharmacology, In Silico
Biosciences
Mechanistic Disease Modeling is a completely new data analytic approach
for de-risking Drug Discovery and Development programs. The approach
has been recognized by the Institute of Medicine as an innovative platform
to reduce the limitations of preclinical animal models in CNS R&D, support
actively rationally designed multi-target drug discovery programs, and
significantly de-risk therapeutic projects for complex CNS disorders.
12:15 pm Sponsored Presentations (Opportunities Available)
12:45 Session Break
1:00 Luncheon Presentation (Sponsorship Opportunity Available) or
Lunch onYour Own
1:40 Session Break
1:50 Chairperson’s Opening Remarks
Deepak Rajpal, Ph.D., Senior Scientific Investigator, Computational Biology,
Medicines Discovery & Development, GlaxoSmithKline
2:00 Metabolic Diseases: Modulation of Microbiome
Deepak Rajpal, Ph.D., Senior Scientific Investigator, Computational Biology,
Medicines Discovery & Development, GlaxoSmithKline
We present a proof-of-concept study where modulation of gut microbiome
revealed novel associations with metabolic improvements in rodents.
This is an important step in evaluating the gut microbiome changes with
metabolic improvements.
2:30TalkTitle to be Announced
Chris Dwan, Assistant Director, Research Computing and Data Services,
Broad Institute of MIT and Harvard
DATA MODELING, SIMULATING
AND VISUALIZING IN NOVEL WAYS
3:00 Caleydo Entourage:Visualizing Relationships between
Biological Pathways
Alexander Lex, Ph.D., Researcher, Harvard School of Engineering & Applied
Sciences
This talk will introduce Entourage, a visualization technique for analyzing
interrelationships between multiple related biological pathways. This talk
demonstrates three case studies showing how Entourage can be used to
judge potential side-effects of compounds, to find potential targets for drug-
repositioning and how it can be combined with visualization of experimental
data to reason about varying effects of compounds on samples. Entourage is
part of Caleydo, an open-source visualization framework.
3:30 Refreshment Break in the Exhibit Hall with Poster Viewing
4:10The Secrets inTheir Landscapes: Using ‘Google Exacyle’ to
Elucidate Activation Mechanism of GPCRs for Selective Drug
Design
Diwakar Shukla, Ph.D., Simbios Distinguished Fellow, Laboratory of Vijay
Pande, Chemistry Department, Stanford University and soon to be Professor,
Chemical Engineering, University of Illinois at Urbana-Champaign
Mechanistic understanding of GPCR activation could be obtained via insilico
approaches, although this is very challenging due to the long activation
timescales. Here, we employ a novel computational paradigm that couples
cloud computing and Markov state model based sampling algorithms for
mapping the conformational landscape of β2-adrenergic receptor. These
computations provide the atomistic picture of activation and help identify key
structural intermediates for drug design.
4:40 Free Energies from a Molecular Printing Press
Kenneth M. Merz, Jr., Director, Institute for Cyber Enabled Research (iCER)
and Joseph Zichis Chair in Chemistry, Department of Chemistry, Department
of Biochemistry and Molecular Biology, Michigan State University
Docking calculations coupled with binding free energy estimates are a
mainstay of structure-based drug design. Docking and scoring methods have
steadily improved over the years, but remain challenging because of the
extensive sampling that is required, the need for accurate scoring functions
and challenges encountered in accurately estimating entropy effects. We
developed the Moveable Type (MT) method that combines knowledge-based
approaches with physics-based models to create molecular ensembles.
5:10 Interactive Breakout Discussion Groups (see website for
details)
6:10 Welcome Reception in the Exhibit Hall with Poster Viewing
7:15 Close of Day
16. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Inaugural October 8 - 9, 2014
Big Data Analytics and Solutions
Using Big Data to Identify New Targets for Drug Discovery
THURSDAY, OCTOBER 9
7:30 am Registration and Morning Coffee
DATA MODELING, SIMULATING AND VISUALIZING
IN NOVEL WAYS
8:00 Chairperson’s Opening Remarks
Peter Henstock, Ph.D., Senior Principal Scientist, Research Business
Technology Group, Pfizer, Inc.
8:10 CARD: A Web-Based Application for Statistical Analysis and
Interactive Visualization of RNAi Screen Data
Bhaskar Dutta, Ph.D., Staff Scientist, Laboratory of Systems Biology, National
Institute of Allergy and Infectious Diseases, National Institutes of Health
CARD is a web-based application for comprehensive analysis and interpretation
of RNAi-screen data. It uses client-server architecture and integrates multiple
types of genome-scale biological data. Different existing and novel data analysis
algorithms are implemented as back-end R modules.The results generated are
visualized using JavaScript libraries as interactive tables and figures. All the data
and results can be saved and securely shared between researchers.
8:40 Genome Wide Association Visual Analysis (GWAVA) Enabled
by a Scalable Data Pipeline
Peter Henstock, Ph.D., Senior Principal Scientist, Research Business
Technology Group, Pfizer, Inc.
Ami Khandeshi, Manager, Research Business Technology Group, Pfizer Inc.
GWAVA is our corporate standard software for interactively querying and
visualizing genome-wide association studies (GWAS) data loaded into the
tranSMART platform. Managing multiple genes and studies, it facilitates an
understanding of the relationship between SNP p-values and study endpoints
by providing and managing access to different views of the data. GWAVA
has recently been released as open source software available through the
tranSMART Foundation.
TRANSLATING DATA INTO KNOWLEDGE FOR
IMPROVED CLINICAL DECISION MAKING, PATIENT
CARE AND DRUG DEVELOPMENT
9:10 A Proven Platform for Diagnosis and Sponsored by
Discovery Using Massive WGS and Phenotypic
Data in RealTime
Jeffrey Gulcher, MD, PhD, Co-founder, President and CSO, NextCODE Health
NextCODE offers the world’s only road-tested solutions for rapidly analyzing
population-scale whole-genome and health data to detect disease-causing
mutations, enabling clinical diagnosis and the optimization of existing and
new treatments. Built to mine 350,000 whole genomes, our genome-
ordered relational (GOR) database architecture is uniquely powered to take
full advantage of the new WGS technology. Its SDL can query phenotypic
datasets to define cases and controls as well as drug response.
9:40 Coffee Break in the Exhibit Hall with Poster Viewing
10:30The Path to Establishing a Global Data Analysis
Infrastructure at AstraZeneca
Justin Johnson, Principal Translational Genomic Scientist, Oncology,
AstraZeneca
It is imperative that we build tools and methods to translate NGS data into
knowledge for target discovery, patient selection, and translational medicine
through a flexible, scalable and secure infrastructure. The hybrid cloud / local
solution and novel data warehousing strategies being built at AstraZeneca will
allow for a global streamlined ability to analyze, store and interpret NGS data.
11:00 Data and Computational Requirements for Implementing
the Department of Veterans Affairs Precision Oncology Program -
A Partnership Between Clinical Care and Clinical Research
Louis Fiore, M.D., MPH, Executive Director, Massachusetts Veterans
Epidemiology Research and Information Center (MAVERIC), Department of
Veterans Affairs; Associate Professor, Boston University School of Medicine,
Boston University School of Public Health
Precision Oncology is our current best chance to reduce the burden of disease
attributed to cancer. Information systems that capture longitudinal medical record
and genomic variant data and allow for real-time data analysis to recommend
individualized patient treatments is a necessary step in the process that must be
addressed by the medical informatics community.This presentation will discuss
the pilot project within VA to create such an integrated system.
11:30 Enjoy Lunch onYour Own
1:00 pm Plenary Keynote Session (see website for details)
2:45 Refreshment Break in the Exhibit Hall with Poster Viewing
3:45 Close of Conference
Discovery on Target | 16
17. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 17
Ninth Annual October 8 - 9, 2014
GPCR-Based Drug Discovery
New Approaches, Technologies and Assays
The renewed excitement in the field of GPCR drug discovery is due to technological progress which has enabled the collection of more structural data on GPCRs
and is allowing study of receptors in different conformational states. This meeting will focus on structural aspects of GPCRs and new assays and technologies
whose applications may enable the discovery of more selective and therefore therapeutically attractive modulators of GPCR signaling.
Suggested Event Package
October 7 Short Course: GPCR Structured-Based Drug Discovery
October 7 Short Course: Targeting of GPCRs with
Monoclonal Antibodies
October 8-9 Conference: GPCR-Based Drug Discovery
October 9-10 Conference: GPCR-Targeted Therapeutics
October 9 Dinner Course: Introduction to Allosteric Modulators and
Biased Ligands of GPCRs
WEDNESDAY, OCTOBER 8
7:00 am Registration and Morning Coffee
STRUCTURAL FEATURES OF GPCRS AND
IMPLICATIONS FOR DRUG DESIGN
8:05 Chairperson’s Opening Remarks
Xinjun Hou, Ph.D., Head, Computational Chemistry, Neuroscience
Department, Pfizer
»»8:15 FEATURED PRESENTATION: FUNCTION
AND PHARMACOLOGY OF CLASS A GPCR: NEW
STRUCTURAL AND COMPUTATIONAL INSIGHTS
Vsevolod (Seva) Katritch, Ph.D., Assistant Professor, Integrative Structural and
Computational Biology, The Scripps Research Institute
Class A G protein-coupled receptors represent the largest and the most
evolutionary dynamic branch of the GPCR tree.This talk will describe the
amazing diversity and the common features of Class A GPCR functional
mechanisms emerging from recent crystallographic, spectroscopic and
molecular modeling studies of the receptors. Direct applications of this atomic-
level knowledge to GPCR pharmacology and drug discovery will be discussed.
9:00 Structure and Ligand Binding Analysis of a Lipid Receptor
Michael Hanson, Ph.D., Director, Structural Biology, Receptos, Inc.
The Edg family of lipid binding receptors has been widely studied since the
discovery of its first member the S1P1 receptor. The structure of the S1P1
receptor has been used to understand the binding mode of pharmaceutical
agents for the treatment of relapsing multiple sclerosis. This structure can
also be used to understand pharmacological differences within the lipid
binding class of G protein coupled receptors.
9:30The Human Glucagon Receptor Structure
Fai Siu, Ph.D., Investigator II, Center for Proteomic Chemistry, Novartis
Institute for BioMedical Research
Binding of glucagon to the glucagon receptor (GCGR) triggers the release
of glucose from the liver during fasting; thus GCGR is important in glucose
homeostasis. I will present the crystal structure of the transmembrane domain
of human GCGR at 3.4 Å resolution, complemented by extensive site-specific
mutagenesis, and a hybrid model of glucagon bound.
10:00 Grand Opening Coffee Break in the Exhibit Hall with Poster
Viewing
10:45 Structure of a Class C GPCR 7TM Domain and Its Allosteric
Modulation
Huixian Wu, Ph.D., Raymond C. Stevens Lab, Department of Integrative
Structural and Computational Biology, The Scripps Research Institute
The metabotropic glutamate receptors (mGlus), which are class C GPCRs,
mediate the modulatory effects of the excitatory neurotransmitter, glutamate.
Allosteric modulators of mGlus are important drug candidates for many
diseases such as brain disorders. In this talk, the structure of mGlu1 seven-
transmembrane domain bound by a negative allosteric modulator will be
presented and the structural basis of the allosteric modulation will be discussed.
11:15 Computational Design of Water Soluble Variants of GPCRs
and other Membrane Proteins
Jeffrey G. Saven, Ph.D., Professor, Department of Chemistry, University of
Pennsylvania
Obtaining G-protein coupled receptors (GPCRs) in forms that retain native
structural and functional properties remains a core problem of membrane
protein science. Membrane proteins can be computationally redesigned,
however, to facilitate heterologous expression in E. coli and characterization.
We have developed and applied such methods to ion channels and to the
human mu opioid receptor, the GPCR target of many pain medications.
11:45 Impact and Gaps in Structural-Based GPCR Drug Discovery:
Q&A Panel Discussion
Moderator: Xinjun Hou, Ph.D., Head, Computational Chemistry, Neuroscience
Department, Pfizer
• Impact on computational chemistry
• Influence in collaborative culture: interactions between biologists, structural
biologists, computational chemists and medicinal chemists?
• Changing landscapes in assay techniques
• Evolving skill sets of computational chemists and modelers
18. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 18
Ninth Annual October 8 - 9, 2014
GPCR-Based Drug Discovery
New Approaches, Technologies and Assays
12:15 pm Sponsored Presentations (Opportunities Available)
12:45 Session Break
1:00 Luncheon Presentation Sponsored by
Speaker to be Announced
1:40 Session Break
SIMULATIONS AND BIG DATA
1:50 Chairperson’s Opening Remarks
Ron Dror, Ph.D., Associate Professor, Computer Science, Stanford University
2:00 Exploration of Drug Disease-Related Selectivity Using
Molecular Simulations of the Bioamine Receptor Family
Irina Tikhonova, Ph.D., Lecturer in Molecular Modeling, School of Pharmacy,
Queen’s University Belfast
Selective polypharmacology is when drugs act on multiple rather than single
molecular targets involved in a disease. We focus on bioamine receptors that
are targets for schizophrenia and depression. Among them, 5-HT2A, 5-HT6,
D2 and D3 receptors induce cognition-enhancing effects, while H1, 5-HT2C
and 5-HT2B receptors causes side effects. A computational dynamic structure-
based approach will be presented to identify drugs targeting preferably the
disease-active receptors.
2:30 Continuous Water Pathway Features GPCRs Ligand
Specificities and Activation States
Shuguang Yuan, Ph.D., Computational Chemist, Drug Discovery, Actelion
Internal water molecules are essential for the function of many membrane
proteins such as channel and GPCRs. We introduced the 32 microseconds
all-atom long time scale molecular dynamics on three different receptors
indicated that continuous water pathway can be features of family A GPCRs
ligand specificities and activation states.
3:00 Sponsored Presentations (Opportunities Available)
3:30 Refreshment Break in the Exhibit Hall with Poster Viewing
4:10The Secrets inTheir Landscapes: Using ‘Google Exacyle’ to
Elucidate Activation Mechanism of GPCRs for Selective Drug Design
Diwakar Shukla, Ph.D., Simbios Distinguished Fellow, Laboratory of Vijay
Pande, Chemistry Department, Stanford University and soon to be Professor,
Chemical Engineering, University of Illinois at Urbana-Champaign
Mechanistic understanding of GPCR activation could be obtained via in silico
approaches, although this is very challenging due to the long activation timescales.
Here, we employ a novel computational paradigm that couples cloud computing
and Markov state model based sampling algorithms for mapping the conformational
landscape of β2-adrenergic receptor.These computations provide the atomistic
picture of activation and help identify key structural intermediates for drug design.
4:40 Free Energies from a Molecular Printing Press
Kenneth M. Merz, Jr., Director, Institute for Cyber Enabled Research (iCER)
and Joseph Zichis Chair in Chemistry, Department of Chemistry, Department
of Biochemistry and Molecular Biology, Michigan State University
Docking calculations coupled with binding free energy estimates are a
mainstay of structure-based drug design. Docking and scoring methods have
steadily improved over the years, but remain challenging because of the
extensive sampling that is required, the need for accurate scoring functions
and challenges encountered in accurately estimating entropy effects. We
developed the Moveable Type (MT) method that combines knowledge-based
approaches with physics-based models to create molecular ensembles.
5:10 Interactive Breakout Discussion Groups (see website for
details)
6:10 Welcome Reception in the Exhibit Hall with Poster Viewing
7:15 Close of Day
THURSDAY, OCTOBER 9
7:30 am Registration and Morning Coffee
NEW APPROACHES FOR STUDYING GPCRS
8:00 Chairperson’s Opening Remarks
Michel Bouvier, Ph.D., Professeur, Department of Biochemistry, University of Montréal
8:10 Nanobody-Enabled Fragment Screening on Active-State
Constrained GPCRs
Jan Steyaert, Ph.D., Director, Structural Biology Brussels Research Center,
Vrije University Brussels
Nanobodies are effective tools for stabilizing agonist-bound active states
of GPCRs. Building on this technology, we have developed a nanobody-
enabled fragment screening approach to explore new chemical space for the
development of drugs targeting GPCRs. Our approach has the advantage
over other methods in that we can screen fragments that exclusively bind to
particular functional conformations of the receptor, allowing us to triage our
fragments according to efficacy profile and potency from a
19. Cover
Targeting Epigenetic Readers and
Chromatin Remodelers
Next Generation Histone Deacetylase
Inhibitors Symposium
Targeting the Ubiquitin
Proteasome System
Big Data Analytics and Solutions
GPCR-Based Drug Discovery
RNAi for Functional Genomics
Screening - Part 1
Protein-Protein Interactions
as Drug Targets
Antibodies Against Membrane
Protein Targets - Part 1
Sponsor & Exhibit Opportunities
Conference-at-a-Glance
Hotel & Travel Information
Short Courses
Registration Information
Click Here to
Register Online!
DiscoveryOnTarget.com
Targeting Histone Methyltransferases
and Demethylases
Screening Drug Transporter Proteins
Maximizing Efficiency in Discovery
GPCR-Targeted Therapeutics
Genome Editing for Functional
Genomics Screens - Part 2
Cancer Metabolism
Antibodies Against Membrane
Protein Targets - Part 2
Discovery on Target | 19
Ninth Annual October 8 - 9, 2014
GPCR-Based Drug Discovery
New Approaches, Technologies and Assays
8:40 BRET to Study Receptor Pharmacology
Kevin Pfleger, Ph.D., Harry Perkins Institute of Medical Research, Australia
Exciting advances have been made recently with respect to the development
of bioluminescence resonance energy transfer (BRET) for studying GPCRs.
This includes the validation of the latest BRET reagents and new BRET-based
approaches to study all facets of GPCR pharmacology, from ligand binding
and G protein-coupling to arrestin recruitment and intracellular trafficking,
particularly in terms of heteromeric complexes.
9:10 Sponsored Presentation
Sponsored by
Speaker to be Announced
9:40 Coffee Break in the Exhibit Hall with Poster Viewing
10:30 Designing Ligands that SpecificallyTarget Nuclear GPCRs
Terry Hébert, Ph.D., Professor, Department of Pharmacology and
Therapeutics,McGill University
An increasing number of GPCRs have been demonstrated to be targeted to
the endomembrane locations as have their associated signalling cascades.
What if half the drugs we deliver reach the wrong intracellular target? What
if the target is an intracellular GPCR rather than the better-characterized
cell surface version? Caging ligands may be an excellent means of further
stratifying the phenotypic effects of known pharmacophores.
11:00 High-Content Analysis to Study GPCR Internalization and
Trafficking
Marla Watt, Ph.D., Senior Research Investigator, Purdue Pharma, LP
11:30 Enjoy Lunch onYour Own
1:00 pm Plenary Keynote Session (see website for details)
2:45 Refreshment Break in the Exhibit Hall with Poster Viewing
3:45 Close of Conference
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