Lifting the lid on GPCRs:the role of extracellular loops


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.

Publication DOI:
Divisions: Life & Health Sciences > Biosciences
Life & Health Sciences > Chronic and Communicable Conditions
Life & Health Sciences
Life & Health Sciences > Pharmacy
Life & Health Sciences > Cellular and Molecular Biomedicine
Additional Information: © 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society.
Uncontrolled Keywords: G-protein coupled receptor,family A GPCR,family B GPCR,extracellular loop,receptor activation,ligand binding,Pharmacology
Full Text Link: https://www.ncb ... les/PMC3372823/
Related URLs: http://www.scop ... tnerID=8YFLogxK (Scopus URL)
http://onlineli ... 1629.x/abstract (Publisher URL)
PURE Output Type: Article
Published Date: 2012-03
Published Online Date: 2012-02-22
Authors: Wheatley, M.
Wootten, Denise
Conner, Matthew T.
Simms, John ( 0000-0002-4675-0902)
Kendrick, R.
Logan, R.T.
Poyner, David R. ( 0000-0003-1590-112X)
Barwell, James

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