Mechanistic Insight on the Mode of Action of Colletoic Acid

  title={Mechanistic Insight on the Mode of Action of Colletoic Acid},
  author={T. Ling and D. J. Miller and W. H. Lang and Elizabeth C. Griffith and A. Rodr{\'i}guez-Cort{\'e}s and I. E. Ayachi and G. Palacios and J. Min and Gustavo A Miranda-Carboni and R. Lee and F. Rivas},
  journal={Journal of Medicinal Chemistry},
  • T. Ling, D. J. Miller, +8 authors F. Rivas
  • Published 2019
  • Chemistry
  • Journal of Medicinal Chemistry
  • The natural product colletoic acid (CA) is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which primarily converts cortisone to the active glucocorticoid (GC) cortisol. Here, CA’s mode of action and its potential as a chemical tool to study intracellular GC signaling in adipogenesis are disclosed. 11β-HSD1 biochemical studies of CA indicated that its functional groups at C-1, C-4, and C-9 were important for enzymatic activity; an X-ray crystal structure of 11β-HSD1… CONTINUE READING