4.7 Article

Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 22, Pages 7061-7064

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm8010178

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Funding

  1. Danish Natural Science Research Council
  2. Danish Medical Research Council
  3. DFG [UL140/7-1, GRK677]

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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, EC50 = 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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