Bioorganic chemistryReceptorsG-Protein-CoupledAnimalsStructure-Activity RelationshipHypoglycemic Agents
Structure-guided discovery of cholic acid derivatives as potent and selective TGR5 allosteric agonists for the treatment of diabetes.
Xuemei Shao, Qirong Cao, Jingjing Sun, Jie Jin, Jisheng Li, Chentao Hua, Zhijie Luo, Shuai Zhao, Yanan Hou, Xin Chen, Mingcheng Qian
Published: 202610.1016/j.bioorg.2025.109384
Abstract
In this work, we designed and synthesized 48 new cholic acid (CA) derivatives as potential Takeda G protein coupled receptor 5 (TGR5) positive allosteric modulators (PAMs). The GloSensor cyclic adenosine monophosphate (cAMP) accumulation assay was us…
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