Ontology highlight
ABSTRACT:
SUBMITTER: Brown SP
PROVIDER: S-EPMC4025659 | biostudies-literature | 2012 Sep
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20120815 9
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activation of which elicits increased insulin secretion only in the presence of elevated glucose levels. A potent, orally bioavailable small molecule GPR40 agonist is hypothesized to be an effective antidiabetic posing little or no risk of hypoglycemia. We recently reported the discovery of AMG 837 (1), a potent partial agonist of GPR40. Herein, we present the optimization from the GPR40 partial agonist 1 ...[more]