The document summarizes ion channels and ion channel receptors. It discusses several key points:
1) Ion channels transport specific ions across cell membranes and generate electrical signals. Voltage-gated and ligand-gated ion channels open and close in response to changes in membrane potential or ligand binding.
2) Common types of ion channels include voltage-gated sodium, potassium, and calcium channels, as well as ligand-gated channels like GABA, glycine, and glutamate receptors.
3) Ion channels play important physiological roles in nerve impulse conduction, muscle contraction, and other processes. Dysfunctions can lead to channelopathies and medical conditions. Many drugs target ion channels.
1. ION CHANNELS
2. ION CHANNEL RECEPTORS- PRINCIPLES
3. STRUCTURE OF ION CHANNEL RECEPTORS
4. VOLTAGE GATED ION CHANNELS
5. LIGAND GATED ION CHANNELS
6. THANKS
1. ION CHANNELS
2. ION CHANNEL RECEPTORS- PRINCIPLES
3. STRUCTURE OF ION CHANNEL RECEPTORS
4. VOLTAGE GATED ION CHANNELS
5. LIGAND GATED ION CHANNELS
6. THANKS
Definition
Classification and description of each class.
Description of individual receptor.
Forces affecting the drug receptor binding.
Binding of drug receptor affect drug action.
Agonist and antagonist.
Disease due to malfunctioning of receptors.
New drug design based on structure of receptors
Receptor as target for drug discovery.
Drug action not mediated by receptor.
GPCRs are the most dynamic and most abundant all the receptors. The G protein-coupled receptor (GPCR) superfamily comprises the largest and most diverse group of proteins in mammals. GPCRs are responsible for every aspect of human biology from vision, taste, sense of smell, sympathetic and parasympathetic nervous functions, metabolism, and immune regulation to reproduction. GPCRs interact with a number of ligands ranging from photons, ions, amino acids, odorants, pheromones, eicosanoids, neurotransmitters, peptides, proteins, and hormones.
Nevertheless, for the majority of GPCRs, the identity of their natural ligands is still unknown, hence remain orphan receptors.
The simple dogma that underpins much of our current understanding of GPCRs, namely,
one GPCR gene− one GPCR protein− one functional GPCR− one G protein −one response
is showing distinct signs of wear.
Neurotransmission (Latin: transmission "passage, crossing" from transmitter "send, let through"), is the process by which signalling molecules called neurotransmitters are released by the axon terminal of a neuron and bind to and react with the receptors on the dendrites of another neuron
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Ion channels, types and their importace in managment of diseasesFarazaJaved
This topic covers voltage gated type of ion channel, general structure and functioning of ion channels and involvement of different ion channel types in the pathogenesis as wella as a target for the development of various diseases.
Receptor types, mechanism, receptor pharmacology, drug receptor interactions, theories of receptor pharmacology, spare receptors and new concepts like biased agonism
Definition
Classification and description of each class.
Description of individual receptor.
Forces affecting the drug receptor binding.
Binding of drug receptor affect drug action.
Agonist and antagonist.
Disease due to malfunctioning of receptors.
New drug design based on structure of receptors
Receptor as target for drug discovery.
Drug action not mediated by receptor.
GPCRs are the most dynamic and most abundant all the receptors. The G protein-coupled receptor (GPCR) superfamily comprises the largest and most diverse group of proteins in mammals. GPCRs are responsible for every aspect of human biology from vision, taste, sense of smell, sympathetic and parasympathetic nervous functions, metabolism, and immune regulation to reproduction. GPCRs interact with a number of ligands ranging from photons, ions, amino acids, odorants, pheromones, eicosanoids, neurotransmitters, peptides, proteins, and hormones.
Nevertheless, for the majority of GPCRs, the identity of their natural ligands is still unknown, hence remain orphan receptors.
The simple dogma that underpins much of our current understanding of GPCRs, namely,
one GPCR gene− one GPCR protein− one functional GPCR− one G protein −one response
is showing distinct signs of wear.
Neurotransmission (Latin: transmission "passage, crossing" from transmitter "send, let through"), is the process by which signalling molecules called neurotransmitters are released by the axon terminal of a neuron and bind to and react with the receptors on the dendrites of another neuron
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Ion channels, types and their importace in managment of diseasesFarazaJaved
This topic covers voltage gated type of ion channel, general structure and functioning of ion channels and involvement of different ion channel types in the pathogenesis as wella as a target for the development of various diseases.
Receptor types, mechanism, receptor pharmacology, drug receptor interactions, theories of receptor pharmacology, spare receptors and new concepts like biased agonism
Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
Role of Ethnopharmacology in drug evaluation,
Reverse Pharmacology.
Instructions for Submissions thorugh G- Classroom.pptxJheel Barad
This presentation provides a briefing on how to upload submissions and documents in Google Classroom. It was prepared as part of an orientation for new Sainik School in-service teacher trainees. As a training officer, my goal is to ensure that you are comfortable and proficient with this essential tool for managing assignments and fostering student engagement.
We all have good and bad thoughts from time to time and situation to situation. We are bombarded daily with spiraling thoughts(both negative and positive) creating all-consuming feel , making us difficult to manage with associated suffering. Good thoughts are like our Mob Signal (Positive thought) amidst noise(negative thought) in the atmosphere. Negative thoughts like noise outweigh positive thoughts. These thoughts often create unwanted confusion, trouble, stress and frustration in our mind as well as chaos in our physical world. Negative thoughts are also known as “distorted thinking”.
Read| The latest issue of The Challenger is here! We are thrilled to announce that our school paper has qualified for the NATIONAL SCHOOLS PRESS CONFERENCE (NSPC) 2024. Thank you for your unwavering support and trust. Dive into the stories that made us stand out!
2024.06.01 Introducing a competency framework for languag learning materials ...Sandy Millin
http://sandymillin.wordpress.com/iateflwebinar2024
Published classroom materials form the basis of syllabuses, drive teacher professional development, and have a potentially huge influence on learners, teachers and education systems. All teachers also create their own materials, whether a few sentences on a blackboard, a highly-structured fully-realised online course, or anything in between. Despite this, the knowledge and skills needed to create effective language learning materials are rarely part of teacher training, and are mostly learnt by trial and error.
Knowledge and skills frameworks, generally called competency frameworks, for ELT teachers, trainers and managers have existed for a few years now. However, until I created one for my MA dissertation, there wasn’t one drawing together what we need to know and do to be able to effectively produce language learning materials.
This webinar will introduce you to my framework, highlighting the key competencies I identified from my research. It will also show how anybody involved in language teaching (any language, not just English!), teacher training, managing schools or developing language learning materials can benefit from using the framework.
Welcome to TechSoup New Member Orientation and Q&A (May 2024).pdfTechSoup
In this webinar you will learn how your organization can access TechSoup's wide variety of product discount and donation programs. From hardware to software, we'll give you a tour of the tools available to help your nonprofit with productivity, collaboration, financial management, donor tracking, security, and more.
The French Revolution, which began in 1789, was a period of radical social and political upheaval in France. It marked the decline of absolute monarchies, the rise of secular and democratic republics, and the eventual rise of Napoleon Bonaparte. This revolutionary period is crucial in understanding the transition from feudalism to modernity in Europe.
For more information, visit-www.vavaclasses.com
This is a presentation by Dada Robert in a Your Skill Boost masterclass organised by the Excellence Foundation for South Sudan (EFSS) on Saturday, the 25th and Sunday, the 26th of May 2024.
He discussed the concept of quality improvement, emphasizing its applicability to various aspects of life, including personal, project, and program improvements. He defined quality as doing the right thing at the right time in the right way to achieve the best possible results and discussed the concept of the "gap" between what we know and what we do, and how this gap represents the areas we need to improve. He explained the scientific approach to quality improvement, which involves systematic performance analysis, testing and learning, and implementing change ideas. He also highlighted the importance of client focus and a team approach to quality improvement.
2. Pore forming transmembrane proteins
associated with transport of specific ions in or
out of the cells.
Highly selective in type of ion transported
(exceptions are there).
Very high rate of ion transfer.
Ions are transported across electrochemical
gradient.
Passive mechanism.
3. Conductance of nerve impulse,generation of
action potential,synaptic ransmission.
Cardiac,skeletal and smooth muscle
contraction.
Epithelial Transport of Nutrients and ions.
T-cell activation (immune regulation).
Pancreatic β-cells insulin release.
4. On the basis
of gating.
Voltage Gated
ion channels
Ligand Gated
Ion Channels
Other Gating
5. 1.Voltage Gated Ion Channels
Open and close in response to membrane potential.
2.Ligand Gated Ion Channels
Open in response to specific ligand molecules binding
to the extracellular domain of the receptor protein.
3.Other Gatings
Indirect signaling,mechano-gated ion channels,light
gated channels
6. Voltage sensitive
Conformational change in response to the potential
gradient.
Generally ion specific.
Important for excitable cells like neurons.
Role in regulation of depolarization and polarization of
neuronal membrane during an action potential.
Distributed along the axon and soma of the neurons.
7. Voltage gated ion channels are made up of
three basic parts :
1.The transmembrane pores
2.Voltage Sensor
3.Selectivity Filter
Contains different subunits:
α subunit and other auxillary subunits
8.
9. Voltage Gated Sodium Channels
(9 membrane ,responsible for membrane depolarization in
action potential generation).
Voltage Gated Calcium Channels
(10 members ,play an important role in both linking muscle
excitation with contraction as well as neuronal excitation
with transmitter release).
Voltage Gated Potassium Channels
(40 members ,role in repolarisation of cell membrane after
action potential)
10. Transient receptor Potential Channels
(28 types ,some of them are voltage gated,named after their
role in Drosophila phototransduction).
Hyperpolarisation-activated cyclic nucleotide-gated
channels
(pacemaking channels in the heart,sensitive to cAMP, CGMP
that alter the voltage sensitivity of the channels)
Voltage Sensitive Proton Channels
(helps in acid extrusion from cell,phagocytosis,strongly PH
regulated)
16. Group of transmembrane ion channels that allow the passing
of several ions upon the binding of specific chemical
messenger like neurotransmitters.
Two domains :transmembrane domain including channel pore
,Extracellular domain including Ligand binding site.
Function:Conversion of presynaptic chemical signal quickly
and effectively into post-synaptic electrical signal.
Three super families:cys-Loop Receptors,Ionotropic
Glutamate Receptor,ATP Gated Channels.
17. Characteristic loop formed by a disulfide bond
between two cystine residues in the N terminal
extracellular domain.
Provides specificity for :
Acetylcholine,sertonin,glycine,glutamate and γ-
aminobutyric acid (GABA) in vertebrates.
Structural elements are well conserved,with a large
extracellular domain(ECD) haboring an alpha-helix
and 10 beta-strands.
18. Bind to NT glutamate.
Consists of a tetramer.
Each subunit consists of extracellular amino
terminal domain,an extracellular ligand binding
domain,a transmembrane domain.
Each subunit of the tetramer has a binding site
for glutamate.
19. Bind to ATP in order to open.
They form trimers with two transmembrane
helices per subunit and both the C and N
terminate on the intracellular side.
22. Plasma Membrane Channels
Examples- Voltage-Gated potassium
channels,Sodium Channels,Calcium
Channels and Chloride Channels.
Intracellular Channels
Example- ER Channels, Mitochondrial
Channels.
23. Ion channels are varied widely and play a wide range
of critical biological functions.
55 different medical conditions have been attributed to
ion channel dysfunction.
Owning to these conditions,13.4% of all drugs are
targeted to ion channels (second highest after
GPCRs).
Worldwide sale of ion channel drugs(estimate)>$12
billion.
24. 1. Tetrodotoxin
2. Ziconitide
3. Benzodiazepines
4. Conotoxin
5. Lidocaine
Other drugs
are:Verapamil,Diltiazem,Amlodipine,Nimod
ipine,Nifedipin,Lidocaine etc.
25. Channelopathies
Cystic fibrosis is caused by mutations in the
CFTR gene,which is a Chloride Channel.
Brugada syndrome is another ventricular
arrhythmia caused by voltage-gated sodium
channel gene mutations.
Shaker gene mutations, ataxia etc.
26.
27. 1. Which of the following statements is true about transmembrane electrical
potential?
a) The chemical gradient drives Cl– and K+ inwards
b) The electrical gradient drives Na+ and Ca+2 inwards
c) The chemical gradient drives Na+ and Ca+2 inwards and K+ outward
d) The chemical gradient drives Cl– and K+ outwards
Answer: c
Explanation: The chemical gradient drives Na+ and Ca+2 inwards and K+ outward,
electrical gradient drives Cl–.
2. The receptor channels for which of the following are gated by extracellular
ligands?
a) Glycine
b) IP3
c) cAMP
d) cGMP
Answer: a
Explanation: The receptor channels for glycine are gated by extracellular ligands.
28. 3. Voltage regulation means
a) Na+/K+ pumps controls potential
b) Unless the voltage is regular gates will not respond
c) Oscilloscope only can control potential
d) With changes in the membrane potential voltage gated ion channels open and
close
Answer: d
Explanation: With changes in the membrane potential voltage gated ion channels open and
close, this is regulation of voltage.
4. Which of the following statements is false about a ligand-gated ion channel
receptor?
a) They are present in the cell membrane
b) They consist of five glycoproteins
c) Differences in membrane potential affect whether the channel receptors are
open or close
d) Neurotransmitters can act as the chemical messengers for these channels
Answer: c
Explanation: Ligands affect whether the channel receptors are open or close in a ligand-
gated ion channel whereas voltage gated ion channels are controlled by the differences in
membrane potential affect.
29. 5. Nicotinic acetylcholine receptor is an example of
a) Ligated gated receptor channel
b) Serpentine receptors
c) Adhesion receptors
d) Receptor enzyme
Answer: a
Explanation: Nicotinic acetylcholine receptor is an example of ligated gated receptor
channel.