XB-ART-19339
Pharm Acta Helv
1995 Sep 01;703:255-62. doi: 10.1016/0031-6865(95)00029-9.
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Towards understanding the role of the first extracellular loop for the binding of peptide hormones to G-protein coupled receptors.
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By a combination of molecular modelling and site-directed mutagenesis studies, we have recently identified a key residue in the first extracellular loop which determines agonist selectivity and high-affinity binding in the V1a vasopressin receptor. Based on primary sequence analysis and structure-activity relationship studies of other neuropeptides and their receptors, the corresponding amino acid in the first extracellular loop is proposed to play a homologous role in conferring affinity and selectivity. This would seem to be the case notably for angiotensin, cholecystokinin, neuropeptide Y and neurokinin receptors.
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Species referenced: Xenopus laevis
Genes referenced: atp6v1a avp cck