| Literature DB >> 22926069 |
Xiaohui Du1, Yong-Jae Kim, Sujen Lai, Xi Chen, Mike Lizarzaburu, Simon Turcotte, Zice Fu, Qingxiang Liu, Ying Zhang, Alykhan Motani, Kozo Oda, Ryo Okuyama, Futoshi Nara, Michiko Murakoshi, Angela Fu, Jeff D Reagan, Peter Fan, Yumei Xiong, Wang Shen, Leping Li, Jonathan Houze, Julio C Medina.
Abstract
GPR142 is a novel GPCR that is predominantly expressed in pancreatic β-cells. GPR142 agonists potentiate glucose-dependent insulin secretion, and therefore can reduce the risk of hypoglycemia. Optimization of our lead pyridinone-phenylalanine series led to a proof-of-concept compound 22, which showed in vivo efficacy in mice with dose-dependent increase in insulin secretion and a decrease in glucose levels.Entities:
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Year: 2012 PMID： 22926069 DOI： 10.1016/j.bmcl.2012.08.015
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823