Inhibition of 3(17)alpha-hydroxysteroid Dehydrogenase (AKR1C21) by Aldose Reductase Inhibitors

Bioorg Med Chem. 2008 Mar 15;16(6):3245-54. doi: 10.1016/j.bmc.2007.12.016. Epub 2007 Dec 15.

Abstract

Mouse 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) is a member of the aldo-keto reductase superfamily that catalyses the oxido-reduction of steroid hormones such as estrogens, androgens and neurosteroids. Inhibitors of aldose reductase (AR), a member of the same superfamily, were evaluated against AKR1C21. Models of the enzyme-inhibitor complexes suggest that Tyr118 and Phe311 are important residues for inhibitor recognition and orientation in the active site of AKR1C21.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
  • 3-Hydroxysteroid Dehydrogenases / chemistry
  • Aldehyde Reductase / antagonists & inhibitors*
  • Aldehyde Reductase / chemistry
  • Animals
  • Binding Sites
  • Enzyme Inhibitors / chemistry*
  • Mice
  • Models, Molecular
  • Protein Binding
  • Substrate Specificity

Substances

  • Enzyme Inhibitors
  • 3-Hydroxysteroid Dehydrogenases
  • Aldehyde Reductase