1240521-70-3Relevant articles and documents
Phenylalanine derivatives as GPR142 agonists for the treatment of Type II diabetes
Du, Xiaohui,Kim, Yong-Jae,Lai, Sujen,Chen, Xi,Lizarzaburu, Mike,Turcotte, Simon,Fu, Zice,Liu, Qingxiang,Zhang, Ying,Motani, Alykhan,Oda, Kozo,Okuyama, Ryo,Nara, Futoshi,Murakoshi, Michiko,Fu, Angela,Reagan, Jeff D.,Fan, Peter,Xiong, Yumei,Shen, Wang,Li, Leping,Houze, Jonathan,Medina, Julio C.
, p. 6218 - 6223 (2012)
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.