Article
Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5H88Y Mutant Mice.
Journal of medicinal chemistry - 26 Aug 2021
Yun Ying, Zhang Chenlu, Guo Shimeng, Liang Xiaoying, Lan Yuan, Wang Min, Zhuo Ning, Yin Jianpeng, Liu Huanan, Gu Min, Li Jing, Xie Xin, Nan Fajun
Abstract excerpt
Takeda G protein-coupled receptor 5 (TGR5) is a promising target for treating metabolic syndrome and inflammatory diseases. Herein, we identified a new series of betulinic acid derivatives as potent TGR5 agonists, which show remarkable activity on human (h) and canine (c) TGR5 but exhibit unpromising activity on murine (m) TGR5. Species difference was also observed with many other reported TGR5 agonists....
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