Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes

  • J Med Chem. 2008 Nov 27;51(22):7061-4. doi: 10.1021/jm8010178.
Elisabeth Christiansen  1 ,  Christian Urban ,  Nicole Merten ,  Kathrin Liebscher ,  Kasper K Karlsen ,  Alexandra Hamacher ,  Andreas Spinrath ,  Andrew D Bond ,  Christel Drewke ,  Susanne Ullrich ,  Matthias U Kassack ,  Evi Kostenis ,  Trond Ulven
Affiliations
  • 1. Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
PMID: 18947221 DOI: 10.1021/jm8010178
Abstract

A series of 4-phenethynyldihydrocinnamic acid agonists of the Free Fatty Acid Receptor 1 (FFA(1)) has been discovered and explored. The preferred compound 20 (TUG-424, EC(50) = 32 nM) significantly increased glucose-stimulated Insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity.

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