2. Academic Validation
  3. 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

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

Affiliation

  • 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.

Figures
Products