ligand binding in g protein coupled receptors
TRANSCRIPT
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