Document Report Card

ID: ALA2057144

Journal: J Med Chem

Title: Discovery of a potent and selective GPR120 agonist.

Authors: Shimpukade B, Hudson BD, Hovgaard CK, Milligan G, Ulven T.

Abstract: GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.

CiteXplore: 22519963

DOI: 10.1021/jm300215x