The inhibitory effects of squalene-derived triterpenes on protein phosphatase PP2A

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1261-4. doi: 10.1016/s0960-894x(03)00136-7.

Abstract

This paper reports testing 15 polyether triterpenes with a squalene carbon skeleton for inhibitory effects on type 2A protein phosphatase. Two compounds, 16-hydroxydehydrothyrsiferol 10 and thyrsenol B 14, exhibited significant inhibitory action at a concentration of 10 microM. Comparison with thyrsiferyl-23-acetate 1 showed that a similar spatial disposition for the hydroxy group around C-15 or C-16 was the structural feature shared by these metabolites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Okadaic Acid / pharmacology
  • Phosphoprotein Phosphatases / antagonists & inhibitors*
  • Rhodophyta / chemistry
  • Squalene / analogs & derivatives*
  • Squalene / isolation & purification
  • Squalene / pharmacology*
  • Structure-Activity Relationship
  • Triterpenes / isolation & purification
  • Triterpenes / pharmacology*

Substances

  • Enzyme Inhibitors
  • Triterpenes
  • Okadaic Acid
  • Squalene
  • Phosphoprotein Phosphatases