| Literature DB >> 22217876 |
Jonathan B Houze1, Liusheng Zhu, Ying Sun, Michelle Akerman, Wei Qiu, Alex J Zhang, Rajiv Sharma, Michael Schmitt, Yingcai Wang, Jiwen Liu, Jinqian Liu, Julio C Medina, Jeff D Reagan, Jian Luo, George Tonn, Jane Zhang, Jenny Ying-Lin Lu, Michael Chen, Edwin Lopez, Kathy Nguyen, Li Yang, Liang Tang, Hui Tian, Steven J Shuttleworth, Daniel C-H Lin.
Abstract
The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest in GPR40 agonists as potential antidiabetic agents. Optimization of a series of β-substituted phenylpropanoic acids led to the identification of (S)-3-(4-((4'-(trifluoromethyl)biphenyl-3-yl)methoxy)phenyl)hex-4-ynoic acid (AMG 837) as a potent GPR40 agonist with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.Entities:
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Year: 2011 PMID： 22217876 DOI： 10.1016/j.bmcl.2011.10.118
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.940