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

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...

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Detalles Bibliográficos
Autores principales: Somvanshi, Rishi K., Kumar, Ujendra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3763651/
https://www.ncbi.nlm.nih.gov/pubmed/24281555
http://dx.doi.org/10.3390/ph5050417
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author Somvanshi, Rishi K.
Kumar, Ujendra
author_facet Somvanshi, Rishi K.
Kumar, Ujendra
author_sort Somvanshi, Rishi K.
collection PubMed
description 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.
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spelling pubmed-37636512013-11-14 Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors Somvanshi, Rishi K. Kumar, Ujendra Pharmaceuticals (Basel) Review 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. MDPI 2012-04-27 /pmc/articles/PMC3763651/ /pubmed/24281555 http://dx.doi.org/10.3390/ph5050417 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Review
Somvanshi, Rishi K.
Kumar, Ujendra
Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
title Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
title_full Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
title_fullStr Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
title_full_unstemmed Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
title_short Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
title_sort pathophysiology of gpcr homo- and heterodimerization: special emphasis on somatostatin receptors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3763651/
https://www.ncbi.nlm.nih.gov/pubmed/24281555
http://dx.doi.org/10.3390/ph5050417
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