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Pharmaceuticals 2012, 5(5), 417-446;

Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors

Faculty of Pharmaceutical Sciences, Division of Pharmacology and Toxicology, The University of British Columbia, Vancouver, BC, V6T 1Z3, Canada
Author to whom correspondence should be addressed.
Received: 3 February 2012 / Revised: 18 April 2012 / Accepted: 19 April 2012 / Published: 27 April 2012
(This article belongs to the Special Issue GPCR Based Drug Discovery)
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G-protein coupled receptors (GPCRs) are cell surface proteins responsible for translating >80% of extracellular reception to intracellular signals. The extracellular information in the form of neurotransmitters, peptides, ions, odorants etc is converted to intracellular signals via a wide variety of effector molecules activating distinct downstream signaling pathways. All GPCRs share common structural features including an extracellular N-terminal, seven-transmembrane domains (TMs) linked by extracellular/intracellular loops and the C-terminal tail. Recent studies have shown that most GPCRs function as dimers (homo- and/or heterodimers) or even higher order of oligomers. Protein-protein interaction among GPCRs and other receptor proteins play a critical role in the modulation of receptor pharmacology and functions. Although ~50% of the current drugs available in the market target GPCRs, still many GPCRs remain unexplored as potential therapeutic targets, opening immense possibility to discover the role of GPCRs in pathophysiological conditions. This review explores the existing information and future possibilities of GPCRs as tools in clinical pharmacology and is specifically focused for the role of somatostatin receptors (SSTRs) in pathophysiology of diseases and as the potential candidate for drug discovery. View Full-Text
Keywords: somatostatin; somatostatin receptors; heterodimerization; G proteins; GPCRs; Pb-FRET somatostatin; somatostatin receptors; heterodimerization; G proteins; GPCRs; Pb-FRET

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Somvanshi, R.K.; Kumar, U. Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors. Pharmaceuticals 2012, 5, 417-446.

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