ligand binding in g protein coupled receptors

LIGAND BINDING IN G-PROTEIN COUPLED RECEPTORS

BY MARIAM JAMIL

WHAT IS GPCR? 7TM RECEPTORS

G PROTEIN–LINKED RECEPTORS 

ACTIVATES INTERNAL SIGNAL TRANSDUCTION PATHWAYS BINDS TO HORMONES, NEUROTRANSMITTERS

PRISCILA Y. SATO, J. KURT CHUPRUN, MATHEW SCHWARTZ, WALTER J. KOCH

PHYSIOLOGICAL REVIEWS PUBLISHED 1 APRIL 2015 VOL. 95 NO. 2, 377-404 DOI: 10.1152/PHYSREV.00015.2014

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MOLECULAR STRUCTURE OF 7-TM RECEPTORS

NATURE REVIEWS DRUG DISCOVERY 4, 107-120 (2005

SHORT EXTRACELLULAR N-TERMINUS AND INTRACELLULAR C-TERMINUS

DISULPHIDE BOND JOINING THE FIRST AND SECOND EXTRACELLULAR LOOPS.

THE THIRD LOOP IS THE MAIN SITE OF G-PROTEIN INTERACTION,

THIRD INTRACELLULAR LOOP AND CARBOXYL TAIL ARE TARGETS FOR PHOSPHORYLATION BY KINASES RESPONSIBLE FOR INITIATING RECEPTOR DESENSITIZATION

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J Biol Chem 2006 281: 2543-.

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DIFFERENT TYPES OF LIGANDS

AGONIST- ACTIVATES THE RECEPTOR

PARTIAL AGONIST- INDUCS PARTIAL ACTIVATION

INVERSE AGONIST- INHIBITS THE ACTIVATION

ANTAGONIST- BLOCKS THE ACCESS TO OTHER LIGANDS

ACTIVATION OF THE G ALPHA SUBUNIT 

 2002 NATURE PUBLISHING GROUP LI, J. ET AL. THE MOLECULE PAGES DATABASE. NATURE 420, 716-717 (2002)

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TYPES OF G-ΑLPHA SUBUNITS

2010 NATURE EDUCATION

SIGNALING CASCADE TRIGGERED BY G-PROTEIN COUPLED RECEPTORS

THERE ARE TWO TYPES OF CAMP DEPENDENT PATHWAYS

GS CAMP DEPENDENT PATHWAY

GI CAMP DEPENDENT PATHWAY

THERE IS ONE TYPE OF PHOSPHOLIPASE MEDIATED PATHWAY

GQ PHOSPHOLIPASE DEPENDENT PATHWAY

GS CAMP DEPENDENT PATHWAY

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METH NEUROSCI. 1995;25:366–428

GI CAMP DEPENDENT PATHWAY

METH NEUROSCI. 1995;25:366–428

GQ PHOSPHOLIPASE DEPENDENT PATHWAY

PMCID: PMC1876727

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DESENSITIZATION

PHYSIOLOGICAL REVIEWS PUBLISHED 1 APRIL 2015 VOL. 95 NO. 2, 377-404 DOI: 10.1152/PHYSREV.00015.2014