Lifting the lid on GPCRs: the role of extracellular loops.

Autor:	Wheatley M; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Wootten D; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Conner MT; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Simms J; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Kendrick R; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Logan RT; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Poyner DR; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK., Barwell J; School of Biosciences, University of Birmingham, Birmingham, UKDrug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, AustraliaDepartment of Pharmacology, Monash University, Parkville, Victoria, AustraliaSchool of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK.
Jazyk:	angličtina
Zdroj:	British journal of pharmacology [Br J Pharmacol] 2012 Mar; Vol. 165 (6), pp. 1688-1703.
DOI:	10.1111/j.1476-5381.2011.01629.x
Abstrakt:	GPCRs exhibit a common architecture of seven transmembrane helices (TMs) linked by intracellular loops and extracellular loops (ECLs). Given their peripheral location to the site of G-protein interaction, it might be assumed that ECL segments merely link the important TMs within the helical bundle of the receptor. However, compelling evidence has emerged in recent years revealing a critical role for ECLs in many fundamental aspects of GPCR function, which supported by recent GPCR crystal structures has provided mechanistic insights. This review will present current understanding of the key roles of ECLs in ligand binding, activation and regulation of both family A and family B GPCRs. (© 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society.)
Databáze:	MEDLINE
Externí odkaz:	Zobrazit plný text záznamu Plný text ve formátu PDF