Lifting The Lid On G-Protein-Coupled Receptors: The Role Of Extracellular Loops.

Mark Wheatley, Denise Wootten, Matthew Conner, John Simms, R Kendrick, Richard Logan, D Poyner, J Barwell

Research output: Contribution to journalArticle

165 Citations (Scopus)


G-protein-coupled receptors (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.
Original languageEnglish
JournalBritish Journal of Pharmacology
Publication statusPublished - 22 Aug 2011


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