Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

Volume: 24, Issue: 7, Pages: 570 - 577
Published: Jun 5, 2017
Abstract
Clinical studies indicate that partial agonists of the G-protein-coupled, free fatty acid receptor 1 GPR40 enhance glucose-dependent insulin secretion and represent a potential mechanism for the treatment of type 2 diabetes mellitus. Full allosteric agonists (AgoPAMs) of GPR40 bind to a site distinct from partial agonists and can provide additional efficacy. We report the 3.2-A crystal structure of human GPR40 (hGPR40) in complex with both the...
Paper Details
Title
Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40
Published Date
Jun 5, 2017
Volume
24
Issue
7
Pages
570 - 577
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