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

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

A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA1) 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 FFA1 in meta...

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Veröffentlicht in:Journal of medicinal chemistry 2008-11, Vol.51 (22), p.7061-7064
Hauptverfasser: Christiansen, Elisabeth, Urban, Christian, Merten, Nicole, Liebscher, Kathrin, Karlsen, Kasper K, Hamacher, Alexandra, Spinrath, Andreas, Bond, Andrew D, Drewke, Christel, Ullrich, Susanne, Kassack, Matthias U, Kostenis, Evi, Ulven, Trond
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
General and cellular metabolism. Vitamins
Medical sciences
Pharmacology. Drug treatments
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Zusammenfassung:A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA1) 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 FFA1 in metabolic diseases such as diabetes or obesity.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm8010178