Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.
Basic Information
ID: ALA2163318
Journal: Bioorg Med Chem Lett
Title: Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.
Authors: Du X, Kim YJ, Lai S, Chen X, Lizarzaburu M, Turcotte S, Fu Z, Liu Q, Zhang Y, Motani A, Oda K, Okuyama R, Nara F, Murakoshi M, Fu A, Reagan JD, Fan P, Xiong Y, Shen W, Li L, Houze J, Medina JC.
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.
CiteXplore: 22926069
DOI: 10.1016/j.bmcl.2012.08.015
Patent ID: ┄