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GPCR

GPCR

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Published by anaeshkl

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Published by: anaeshkl on May 06, 2009
Copyright:Attribution Non-commercial

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07/01/2010

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GPCR 
~ aka 7 tranmembrane receptors/heptahelical receptors/ 7 transmembrane domain receptors/ GProtein Linked Receptors protein family of TM receptors that sense molecules outside cell and activate inside signaltransduction pathways and ultimately cellular responsesLigand that bind include:Light sensitive compoundsOdoursPheromonesHormones Neurotransmitters
Classification
6 classes based on sequence homology and functional similarityClass A to Class FGRAFS (glutamate, Rhodopsin, Adhesion, Frizzled/Taste2, Secretin)
Physiological roles
-wide variety-visual sense; rhodopsin-smell: odorant/pheromones-behavioral and mood regulation: serotonin, dopa, GABA, glutamate-immune system activity and inflammation: histamine receptors-autonomic nervous system
Structure
-7 TM helices-extracellular parts of receptor can be glycosylated: extracellular loops contain 2 highlyconserved cysteine reidues that form disulphide bonds
Mechanism
-activated by ligand-conformational change
activation of G protein ( depending on type of G protein)Ligands-examples-3 types of ligands: agonist, inverse agonist, neutral antagonist

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