Identification and Pharmacological Characterization of Multiple Allosteric Binding Sites on the Free Fatty Acid 1 Receptor

@article{Lin2012IdentificationAP,
  title={Identification and Pharmacological Characterization of Multiple Allosteric Binding Sites on the Free Fatty Acid 1 Receptor},
  author={Daniel C.-H. Lin and Qi Guo and Jian Luo and Jane Zhang and Kathy Nguyen and Michael Chen and T. D. Zoe Tran and Paul John Dransfield and Sean P. Brown and Jonathan B. Houze and Marc Vimolratana and Xianyun Jiao and Yingcai Wang and Nigel J.M. Birdsall and Gayathri Swaminath},
  journal={Molecular Pharmacology},
  year={2012},
  volume={82},
  pages={843 - 859}
}
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 of two chemical series of partial and full agonists that have been identified… 
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