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 of Medicinal Chemistry2008Vol. 51(22), pp. 7061–7064
Citations Over TimeTop 10% of 2008 papers
Elisabeth Christiansen, 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
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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