GPCR

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All about GPCR specials thanks to KD Tripathi book

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Presentation Transcript

Slide 1:

The G-Protein-Coupled Receptors Toshit Sharma M.Pharm . (Pharmacology) 2 nd Sem .

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Mechanism Of Drugs Action

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GPCRs Introduction

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A large family of cell membrane receptors which are linked to the effector through one or more GTP- activated proteins for response effectuation. Found only in eukaryotes. Are the target of approximately 40% of all modern medicines. GPCRs also include Orphans.

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Their work was - “Crucial for understanding how G- protein–coupled receptors function.”

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GPCRs Structure

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Single polypeptide chain of up to 1100 residues.

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2 cysteine residues with disulfide bonds on EC loops.

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GPCRs Classification

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On behalf of The length of the EC- N terminus. The location of the agonist binding site.

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Three more families are mentioned Fungal mating pheromone receptors Cyclic AMP receptors Frizzled/Smoothened

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G-proteins and their role

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Membrane resident proteins. Called as G-proteins because of their interaction with the GTP and GDP . Represents the level of middle management as follows:

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Guanine nucleotides binds to the α subunit. α subunit also has intrinsic GTPase activity.

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All the three subunits attached to the membrane through Prenylation .

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Mechanism of Action

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GPCRs effector pathways

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Adenylyl Cyclase : cAMP pathway

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Phospholipase C: IP 3 - DAG Pathway

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Rho/Rho kinase pathway

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Ion channel regulation

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Major functional pathways of G-protein coupled receptor transduction

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GPCRs desensitization

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Involves two steps: 1. Receptor phosphorylation 2. Receptor internalization

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Some recent developments

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? Any query…

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Thank you…

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