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 o...
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| Veröffentlicht in: | British journal of pharmacology 2012-03, Vol.165 (6), p.1688-1703 |
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| creator | Wheatley, M Wootten, D Conner, MT Simms, J Kendrick, R Logan, RT Poyner, DR Barwell, J |
| description | 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.
LINKED ARTICLES This article is part of a themed section on the Molecular Pharmacology of G Protein‐Coupled Receptors (GPCRs). To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2012.165.issue‐6. To view the 2010 themed section on the same topic visit http://onlinelibrary.wiley.com/doi/10.1111/bph.2010.159.issue‐5/issuetoc |
| doi_str_mv | 10.1111/j.1476-5381.2011.01629.x |
| format | Article |
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LINKED ARTICLES This article is part of a themed section on the Molecular Pharmacology of G Protein‐Coupled Receptors (GPCRs). To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2012.165.issue‐6. To view the 2010 themed section on the same topic visit http://onlinelibrary.wiley.com/doi/10.1111/bph.2010.159.issue‐5/issuetoc</description><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>extracellular loop</subject><subject>family A GPCR</subject><subject>family B GPCR</subject><subject>G‐protein coupled receptor</subject><subject>Humans</subject><subject>ligand binding</subject><subject>Ligands</subject><subject>Medical sciences</subject><subject>Pharmacology. 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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.
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| source | MEDLINE; Wiley Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Wiley Online Library (Open Access Collection); PubMed Central; Alma/SFX Local Collection |
| subjects | Binding Sites Biological and medical sciences extracellular loop family A GPCR family B GPCR G‐protein coupled receptor Humans ligand binding Ligands Medical sciences Pharmacology. Drug treatments Protein Conformation receptor activation Receptors, G-Protein-Coupled - chemistry Receptors, G-Protein-Coupled - metabolism Reviews |
| title | Lifting the lid on GPCRs: the role of extracellular loops |
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