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Phenylalanine derivatives as GPR142 agonists for the treatment of Type II diabetes |
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| Authors: | Xiaohui Du 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 |
| Institution: | Amgen Inc, 1120 Veterans Blvd., South San Francisco, CA 94080, USA. Electronic address: xdu@amgen.com. |
| 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. |
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