Lifting the lid on GPCRs: the role of extracellular loops

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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
Pages (from-to)1688-1703
Number of pages16
JournalBritish Journal of Pharmacology
Issue number6
Early online date22 Feb 2012
Publication statusPublished - Mar 2012


  • G-protein coupled receptor, family A GPCR, family B GPCR, extracellular loop, receptor activation, ligand binding

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