Kinetic studies on rat liver 11 beta-hydroxysteroid dehydrogenase

Biochim Biophys Acta. 1991 Nov 14;1115(1):23-9. doi: 10.1016/0304-4165(91)90006-3.

Abstract

The kinetic behavior of homogeneous rat liver 11 beta-hydroxysteroid dehydrogenase (11-HSD) was investigated. The purified enzyme catalyzed oxidation of the 11 beta-hydroxy steroids, cortisol and corticosterone, to their 11-oxo products. The reverse 11-oxoreductase was not detected. Initial velocity studies of 11 beta-dehydrogenase were consistent with a sequential bireactant mechanism. Glycyrrhetinic acid, a competitive inhibitor of corticosterone oxidation, was uncompetitive with respect to NADP+. The observed inhibition patterns were consistent with an ordered sequential mechanism with NADP+ adding to the enzyme first. Analogs of NADP+ and NAD+ did not inhibit steroid oxidation by 11-HSD, nor did the products of the 11 beta-dehydrogenase reaction slow oxidation, or catalyze reduction. Ligand binding studies generated patterns that supported the ordered sequential mechanism derived from kinetic studies. The kinetic behavior of 11-HSD is therefore similar to other alcohol dehydrogenases. The basis for the apparent inability of homogeneous 11-HSD to catalyze reduction remains to be established.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenases
  • Animals
  • Binding, Competitive
  • Glycyrrhetinic Acid / pharmacology
  • Hydroxysteroid Dehydrogenases / antagonists & inhibitors
  • Hydroxysteroid Dehydrogenases / chemistry*
  • Kinetics
  • Liver / enzymology*
  • NAD / analogs & derivatives
  • NAD / pharmacology
  • NADP / analogs & derivatives
  • NADP / pharmacology
  • Protein Binding
  • Rats

Substances

  • NAD
  • NADP
  • Hydroxysteroid Dehydrogenases
  • 11-beta-Hydroxysteroid Dehydrogenases
  • Glycyrrhetinic Acid