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
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DOI：
10.1021/jm8010178
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发表时间：
2008-11-27
影响因子：
7.3
通讯作者：
Ulven, Trond
中科院分区：
文献类型：
--
作者：
Christiansen, Elisabeth;Urban, Christian;Ulven, Trond
已发现并探索了一系列游离脂肪酸受体1（FFA（1））的4-苯乙炔基二氢肉桂酸激动剂。优选的化合物20（TUG-424，EC 50 = 32 nM）在100 nM时显著增加葡萄糖刺激的胰岛素分泌，并可用于探索FFA（1）在代谢疾病如糖尿病或肥胖症中的作用。
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.