期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 4, 期 8, 页码 790-794出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml400186z
关键词
GPR142; agonist; insulin secretagogue; diabetes; glucose lowering
GPR142 is a G protein-coupled receptor that is predominantly expressed in pancreatic beta-cells. GPR142 agonists stimulate insulin secretion in the presence of high glucose concentration, so that they could be novel insulin secretagogues with reduced or no risk of hypoglycemia. We report here the optimization of HTS hit compound 1 toward a proof of concept compound 33, which showed potent glucose lowering effects during an oral glucose tolerance test in mice and monkeys.
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