A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice

@inproceedings{Zheng2015ANT,
  title={A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice},
  author={Chunbing Zheng and Wenbo Zhou and Tongtong Wang and Panpan You and Yongliang Zhao and Yiqing Yang and Xin Wang and Jian Luo and Yihua Chen and Mingyao Liu and Huaqing Chen and Bridget Wagner},
  booktitle={PloS one},
  year={2015}
}
The G protein-coupled receptor TGR5 is a membrane receptor for bile acids. Its agonism increases energy expenditure and controls blood glucose through secretion of glucagon-like peptide-1 in enteroendocrine cells. In this study, we explored the therapeutic potential of WB403, a small compound activating TGR5 which was identified by combining TGR5 targeted luciferase assay and active GLP-1 assay, in treating type 2 diabetes. After confirmation of TGR5 and GLP-1 stimulating activities in various… CONTINUE READING
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