Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.

@article{Genet2010StructureactivityRS,
  title={Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.},
  author={C{\'e}dric Genet and Axelle Strehle and C{\'e}line Schmidt and Geoffrey Boudjelal and Annelise Lobstein and Kristina Schoonjans and Michel Souchet and Johan Auwerx and R{\'e}gis Saladin and Alain Wagner},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 1},
  pages={178-90}
}
We describe here the biological screening of a collection of natural occurring triterpenoids against the G protein-coupled receptor TGR5, known to be activated by bile acids and which mediates some important cell functions. This work revealed that betulinic (1), oleanolic (2), and ursolic acid (3) exhibited TGR5 agonist activity in a selective manner compared to bile acids, which also activated FXR, the nuclear bile acid receptor. The most potent natural triterpenoid betulinic acid was chosen… CONTINUE READING

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