Discovery of a potent and selective GPR120 agonist

  • J Med Chem. 2012 May 10;55(9):4511-5. doi: 10.1021/jm300215x.
Bharat Shimpukade  1 ,  Brian D Hudson ,  Christine Kiel Hovgaard ,  Graeme Milligan ,  Trond Ulven
Affiliations
  • 1. Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
PMID: 22519963 DOI: 10.1021/jm300215x
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.

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