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Discovery of a novel potent GPR40 full agonist
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-01-12 , DOI: 10.1016/j.bmcl.2018.01.013 Sanath K. Meegalla , Hui Huang , Tonya Martin , June Xu , Shuyuan Zhao , Jianying Liu , Meghan Hall , Joe Gunnet , Yuanping Wang , Brian Rady , Jose Silva , Monicah Otieno , Eric Arnoult , S. Paul Lee , Alessandro Pocai , Mark R. Player
中文翻译：
发现新型强效GPR40全激动剂
更新日期：2018-01-12
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-01-12 , DOI: 10.1016/j.bmcl.2018.01.013 Sanath K. Meegalla , Hui Huang , Tonya Martin , June Xu , Shuyuan Zhao , Jianying Liu , Meghan Hall , Joe Gunnet , Yuanping Wang , Brian Rady , Jose Silva , Monicah Otieno , Eric Arnoult , S. Paul Lee , Alessandro Pocai , Mark R. Player
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Compound 12 is a GPR40 agonist that realizes the full magnitude of efficacy possible via GPR40 receptor agonism. In vitro and in vivo studies demonstrated superior glucose lowering by 12 compared to fasiglifam (TAK-875), in a glucose dependent manner. The enhanced efficacy observed with the full agonist 12 was associated with both direct and indirect stimulation of insulin secretion.
中文翻译：
发现新型强效GPR40全激动剂
化合物12是GPR40激动剂，可通过GPR40受体激动剂实现全部功效。体外和体内研究表明，与依法格胺（TAK-875）相比，葡萄糖依赖性葡萄糖的降低率高12倍。用完全激动剂12观察到的功效增强与胰岛素分泌的直接和间接刺激有关。
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