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

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) i...

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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:	Animals Cinnamates - chemical synthesis Cinnamates - chemistry Cinnamates - pharmacology Crystallography, X-Ray Diabetes Mellitus, Type 2 - drug therapy Dose-Response Relationship, Drug Drug Discovery Glucose - antagonists & inhibitors Glucose - pharmacology Humans Insulin - metabolism Insulin Secretion Mice Models, Molecular Molecular Structure Rats Receptors, G-Protein-Coupled - agonists Stereoisomerism Structure-Activity Relationship Time Factors
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Zusammenfassung:	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.
ISSN:	1520-4804
DOI:	10.1021/jm8010178