Article
Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.
Molecular pharmacology - 1 Nov 2012
Lin Daniel C-H, Guo Qi, Luo Jian, Zhang Jane, Nguyen Kathy, Chen Michael, Tran Thanh, Dransfield Paul J, Brown Sean P, Houze Jonathan, Vimolratana Marc, Jiao Xian Yun, Wang Yingcai, Birdsall Nigel J M, Swaminath Gayathri
Abstract excerpt
Activation of FFA1 (GPR40), a member of G protein-coupling receptor family A, is mediated by medium- and long-chain fatty acids and leads to amplification of glucose-stimulated insulin secretion, suggesting a potential role for free fatty acid 1 (FFA1) as a target for type 2 diabetes. It was assumed previously that there is a single binding site for fatty acids and synthetic FFA1 agonists. However, using members...
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