The GPCR & Kinase Targets conference held from April 13-15, 2011, in London, featured leading experts in pharmaceutical research discussing advancements in drug development related to G-protein coupled receptors (GPCRs) and kinases. Key topics included innovative drug discovery techniques, cellular assays, biophysical models, and the challenges of translating early research into clinical success. The event offered networking opportunities for decision-makers in the biotech and pharmaceutical sectors to collaborate on overcoming current industry obstacles.

1. GPCR & Kinase Targets
Advances in drug development from molecular to clinical
13th – 15th April 2011, London, UK BOOK NOW!
Key Speakers
Mark Bunnage, Executive Director, Medicinal Chemistry, Pfizer
Maria Flocco, Senior Director, Lead Discovery and Structural Biology & Biophysics, Pfizer
Guido Zaman, Senior Director GPCR and Kinases, Molecular Pharmacology Unit, Merck Sharp & Dohme
Ulrich Wendt, Director, Structural Biology,Sanofi-Aventis
Paul Bamborough, Section Head, Computational and Structural Chemistry, GlaxoSmithKline
Magalie Rocheville, Investigator, GlaxoSmithKline
Will Spooren, Project Leader, Drug Discovery, F. Hoffmann La Roche
Alexandre Trifilieff, Senior Investigator, Novartis
Leo Widler, Senior Investigator, Novartis
Lee Dawson, Director, Biopharmacology, Neurosciences Product Creation Unit, Eisai
Benny Bang-Andersen, Chief Scientist & Group Leader, Discovery Chemistry & DMPK, Lundbeck
Trevor Howe, Research Fellow, Head of Biophysics & Structural Biology, Janssen Pharmaceutica
Stefan Knapp, Principal Investigator, Oxford University Structural Genomics Consortium
Luda Diatchenko, Chief Scientific Officer, Algynomics
Scott DeWire, Senior Research Scientist & Co-Founder, Trevena
Pre-conference Workshop, Wednesday 13th April, 2011
Cell-based assays for GPCR and kinase monitoring
Led by: Julian Burke, Chief Scientific Officer, Genetix
Driving the Industry Forward | www.futurepharmaus.com
Organised By
Media Partners
To Book Call: +44 (0) 20 7336 6100 | www.visiongain.com/gpcrkt

2. Conference Introduction
GPCR & Kinase Targets
13th – 15th April 2011, London, UK
Media Partners:
Dear Colleague,
PharmiWeb.com is the leading industry-sponsored portal
omprising more than 60% of all therapeutic targets, G-protein coupled
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for the pharmaceutical sector. Supported by most of the
receptor and kinase targets are arguably the most exciting proteins in
leading pharmaceutical corporations, PharmiWeb.com provides dynamic
pharmacology today. Drugs acting via GPCRs alone have netted over $50bn
real-time news, features, events listings and international jobs to industry
in sales worldwide, for conditions ranging from diabetes, to hypertension
professionals across Europe and the US.
and pain. Yet, despite massive investment spanning decades, translating
For further information please email: corporate@pharmiweb.com
early research to clinical success remains frustratingly slow. New approaches
are needed that acknowledge and integrate structural, functional and BIOTECHNOLOGY EUROPE is owned by BIOTECHNOLOGY
systems components, to accelerate time-to-market. WORLD. It is based and located in Warsaw, Poland.
Biotechnology World was founded in 2007 to provide the world’s biotech
By attending Visiongain’s GPCR and Kinase Targets conference, you
and pharma information and market to make it universally accessible and
will engage with leading decision makers and thought leaders, useful for scientific and business processes. Its first step to fulfilling that
enabling you to: mission was building the BIOTECHNOLOGY EUROPE platform that will
• mprove the efficacy of assays to enhance 7 transmembrane and kinase
I allow a quick spread of information in different channels. BIOTECHNOLOGY
drug discovery EUROPE offers companies completed internet public relations, publication
• ncorporate improved computational models to evaluate drug-receptor
I and marketing solutions. One of the mains goals of BIOTECHNOLOGY
interactions and allosteric modulation of downstream signalling pathways EUROPE is to integrate the Biotech and Pharma Sector in Europe to global
biotechnology, pharmaceutical and life science activities.
• valuate gene splicing for μ-opiod drug development
E
For further information please visit: www.biotechnology-europe.com
• arget chemogenomic, Wnt and aneuploid-specific pathways for cancer
T
Future Pharmaceuticals has forged powerful relationships
Driving the Industry Forward | www.futurepharmaus.com
therapy
with key industry leaders to provide a platform for
• mploy more accurate siRNA screens to map signalling networks
E successful brand recognition, and for senior decision-makers to have the
• issect variability in chemotherapy through systems pharmacology
D means to procure and plan implementation strategies based on the topics
• tilise developments in HTS technology to improve patient stratification
U covered. Positioned to be an authoritative resource within top pharma
companies as well as small, specialty, and biotech, Future Pharmaceuticals
• mploy alternatives to mass spectrometry when undertaking research
E magazine is geared to create a deep penetration into a highly targeted and
• ntegrate cell-signalling and systems biology insights into treatments for
I responsive audience, bridging the gap between the industries’ top issues and
complex diseases the solutions top-tier vendors can provide.
• electively activate and quantify beta-arrestin biased ligands for analgesia
S For further information please visit: www.futurepharmaus.com
and heart disease InPharm is the online platform for exclusive
• etter modulate parathyroid hormone release to treat osteoporosis
B pharmaceutical news, comment, contracts, services, jobs
and events and is home to InPharmjobs.com, Pharmafile and Pharmafocus.
• ssess pharmacotherapies in clinical development for pulmonary,
A
neurodevelopmental and antipsychotic diseases For further information please visit: www.In-Pharm.com
I look forward to meeting you at the conference
Best regards
John Shah
Sponsorship and exhibition opportunities
Conference Producer
This event offers a unique opportunity to meet and do business with some
of the key players in the pharmaceutical and biotech industries. If you have a
Who should attend? service or product to promote, you can do so at this event by:
Presidents, Chief Executive Officers, VPs, Global Heads, Chief
Scientific Officers, Directors, Principal Scientists, Franchise Heads and • Hosting a networking drinks reception
Investigators in:
• GPCR/Kinase Research • Taking an exhibition space at the conference
• Molecular Pharmacology and Bioanalytical Development
• Cellular Assays • Advertising in the delegate documentation pack
• High-Throughput/High-Content Screening Operations
• Compound Profiling
• Providing branded bags, pens, gifts, etc.
• CNS, Neurodegenerative Disease, Diabetes, Arthritis, Pain, Oncology
• Lead Optimisation/Generation
If you would like more information on the range of sponsorship or exhibition
• In Vitro Sciences
• Pre-clinical Development
• Medicinal Chemistry possibilities for visiongain's GPCR & Kinase Targets Conference, please
• Computational Chemistry and Bioapplications
• Genomics contact us:
• Proteomics
• Bioinformatics Ronald Magali, +44 (0)20 7549 9934
• Systems Biology
• Pharmacovigilance and Safety Testing ronald.magali@visiongainglobal.com
• Personalised Medicine

3. Pre-Conference Interactive Workshop
GPCR & Kinase Targets
Wednesday 13th April 2011
Cell-based assays for GPCR and kinase monitoring
Led by: Julian Burke Timings: 9:30 - 10:00 Coffee & Registration
0
Chief Scientific Officer 10:00 - 15:00 Workshop
Genetix T
iming includes lunch and refreshment breaks
About the workshop: About your workshop leader:
Dr Julian F. Burke Ph.D
The workshop will address issues surrounding cell-based
Dr Julian F. Burke Ph.D. is Chief Scientific Officer at Genetix Limited and
GPCR and kinase screening. These will include the use of
a visiting Professor at the University of Southampton. He has previously
fluorescent protein reporters as read outs for activation, as held scientific and faculty positions at the University of Sussex where
well as label free techniques that can be used to monitor he also founded a university spin out company. He has worked for the
Medical Research Council, Cancer Research UK and the Roswell Park
and determine pathways of activation. A particular
Cancer Centre, New York, USA. He obtained his Ph.D. in Biochemistry
focus will be on the use of primary and iPS stem cells for
from the University of Aberdeen, has authored three books on
screening purposes and how these cells reflect current molecular biology and has over 80 publications in refereed journals. He
serves on several government funding committees.
models of pharmaceutical drug screening.
About the company
About visiongain:
Genetix Limited, now part of Leica Microssytems, currently employs
Visiongain is a specialist business information company focused on providing
cutting edge products and services across the Pharmaceutical/Biotech, 170 people and has been run as a consistently profitable business
Telecommunications, Defence and Finance sectors, which include reports,
developing reagents and instrumentation for the Biopharmaceutical
conferences, online daily news and offline news analysis and bespoke consultancy.
industry. The company played a major role in the Human Genome
With a commitment to innovation and excellence, visiongain offers flexible
solutions to meet our clients’ business intelligence needs, providing the right project supplying colony pickers to the major academic sequencing
information at the right time to facilitate the commercial decision-making
centres and commercial sequencing companies. The company has now
process. Our pharmaceutical products include Pharma Business Daily, the leading
evolved and focuses on its core strengths of imaging and analysis in
daily email newsletter for the pharmaceutical, biotech and healthcare industries,
and a range of independent, high-quality, in-depth reports covering focused and the field of cell biology. Genetix Limited develops systems for early
topical areas of concern. Our pharmaceutical conferences address the hottest
stage therapeutic antibody production, cell screening and cell based
commercial, regulatory and technical topics and provide an ideal forum for
diagnostics.
debate and networking for pharmaceutical professionals from around the world.
For further information, please visit: www.visiongain.com www.genetix.com

4. Day 1
GPCR & Kinase Targets
Thursday 14th April 2011
09:00 Registration and refreshments 14:00 A novel alternatively spliced isoform of the
mu-opioid receptor (MOR): functional antagonism
09:30 Opening address from the Chair • 7TM and 6TM MOR isoforms stimulate counteracting signalling pathways
Trevor Howe • Higher 6TM isoforms are linked to hyperalgesia/poor morphine response
Research Fellow, Head of Biophysics & Structural Biology
Janssen Pharmaceutica • There is clinical potential for developing selective 7TM/6TM compounds
Luda Diatchenko
09:40 Enabling structure-based drug discovery for GPCR Chief Scientific Officer
Algynomics
targets using conformationally thermostabilised
receptors (StaRs)
14:40 Targeting signalling networks
• StaRs enable production of functionally-relevant purified GPCRs
• Strategies for selective inhibitor design
• acilitates fragment screening by SPR and NMR to find high-quality hits
F
• Targeting kinases outside the active site
• Crystal structures of GPCRs support structure-based drug design
• Targeting complex cellular systems
Chris Langmead
Head of Pharmacology Stefan Knapp
Heptares Therapeutics Principal Investigator
Oxford University Structural Genomics Consortium
10:20 Drug design for G-protein coupled receptors by a
ligand based NMR method 15:20 Afternoon refreshments
• Development of ligand based NMR methods as a basis for drug design
15:40 Presentation to be announced
• Application to protein kinase and GPCR targets
Jürgen Moll
• Future perspectives for NMR in pharmaceutical research Director, Cell Biology Department
Nerviano Medical Sciences
Ulrich Wendt
Director, Structural Biology
Sanofi-Aventis
16:20 Panel discussion: Modelling the interactome
11:00 Morning refreshments T
opics covered will include ligand efficacy and quantitative and directional
protein interaction networks. Functional redundancy and the limitations of
11:20 Selecting and optimising screening assays for single target approaches for complex diseases will be critiqued, in addition
to methodological approaches. Please email your questions for the panel
7-transmembrane receptor signalling
to: john.shah@visiongainglobal.com.
• Label-free assays
Chair: Maria Flocco
• The importance of primary cells Senior Director, Lead Discovery and Structural Biology & Biophysics
Pfizer
• A holistic approach to cell signalling
Magalie Rocheville
Magalie Rocheville
Investigator
Investigator
GlaxoSmithKline
GlaxoSmithKline
Stefan Knapp
Principal Investigator, Structural Genomics Consortium
12:00 Chemogenomic analysis of protein kinases in
University of Oxford
Wnt/Frizzled signalling
• Importance of abnormal Wnt/ β-catenin in disease
• Development of a fast, reliable assay to measure intracellular signalling 17:00 Closing remarks from the chair
• Clinical applications
Guido Zaman
Senior Director GPCR and Kinases, Molecular Pharmacology Unit 17:10 Networking drinks
Merck Sharp & Dohme
Take your discussions further and build new
relationships in a relaxed and informal setting
12:40 Networking lunch
Due to unforeseen circumstances the programme may change and visiongain reserves the right to alter the venue and/or speakers c Copyright visiongain Ltd, 2011

5. Day 2
GPCR & Kinase Targets
Friday 15th April 2011
09:00 Registration and refreshments 12:40 Networking lunch
09:30 Opening address from the Chair 13:40 Bioactive peptides and orphan neuropeptides
Mark Bunnage
on known and orphan GPCRS using beta
Executive Director, Medicinal Chemistry arrestin technology
Pfizer • Multiple reporter assays
• Multiplex Tag-lite assays
09:40 GPCR biased ligand drug discovery: dissecting
receptor signaling pathways for better medicines • New internalisation assay based on FRET
• GPCRs signal through multiple, independent, intracellular pathways Xavier Leroy
Project Leader and Senior Lab Head, Drug Discovery
• These signaling pathways can be selectively targeted by biased ligands Actelion Pharmaceuticals
• Biased ligands elicit unique pharmacology targeting unmet medical needs
Scott DeWire
14:20 Therapeutic utility of neurokinin receptor
Senior Research Scientist, Co-founder antagonists in the treatment of schizophrenia
Trevena • Rationale for developing NK3 receptor antagonists for schizophrenia
• Preclinical evaluation of a number of molecules targeted at this receptor
10:20 Calcium-sensing receptor antagonists: a therapy
for established osteoporosis? • linical evaluation and potential utility of other neurokinin modulators
C
• Secretion of PTH is controlled by CaSRs Lee Dawson
Director, Biopharmacology, Neurosciences Product Creation Unit
• Clinical benefits in mild-to-moderate osteoporosis Eisai
• Prospects for the future
Leo Widler
15:00 Afternoon refreshments
Senior Investigator
Novartis 15:20 Drug targets in autism and neurodevelopmental
disorders
11:00 Morning refreshments Will Spooren
Project Leader, Drug Discovery
11:20 Discovery of PF-610,355, an inhaled once-daily F. Hoffmann La Roche
beta-2 adrenoceptor agonist for treatment of
asthma & COPD 16:00 Kinase drug discovery for chronic diseases, and
• otent, inhaled long-acting β2 agonist for treatment of
P
the discovery of Losmapimod
respiratory disease • Selectivity in kinase system-based drug discovery
• Long in vivo duration supporting once-daily dosing in humans • Case study: Losmapimod, a p38 kinase inhibitor
• Clinical POC achieved and compound in advanced phase II studies Paul Bamborough
Section Head, Computational and Structural Chemistry
Mark Bunnage
GlaxoSmithKline
Executive Director, Medicinal Chemistry
Pfizer
16:40 Chair’s closing remarks
12:00 Toward an understanding of the observed clinical
profile for Indacaterol, the first once-daily inhaled 16:50 End of conference
beta-2 adrenoceptor agonist
• Indacaterol combines fast onset and once daily dosing for COPD
• Long lasting action is believed to be due to its lipophilic properties
• Its fast onset is linked to its intermediate intrinsic efficacy
Alexandre Trifilieff
Senior Investigator
Novartis

6. Registration Form
GPCR & Kinase Targets
13th – 15th April 2011, London, UK
Conf. code
Standard Prices
Conference and workshop
Conference only
Fee: £1699
Fee: £1299
VAT: £339.80
VAT: £259.80
Total: £2038.80
Total: £1558.80
GPCR & Kinase Targets
Workshop only Fee: £599 VAT: £119.80 Total: £718.80 13th – 15th April 2011
Number of bookings: Total cost:
London, UK
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Distribution of your company’s promotional literature to all conference attendees
Fee: £999 VAT: £199.80 Total: £1198.80
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