Evaluation of phosphorus-containing inhibitors of gamma-glutamyl hydrolase

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1521-4. doi: 10.1016/s0960-894x(98)00253-4.

Abstract

Several putative, phosphorus-containing inhibitors of gamma-glutamyl hydrolase were synthesized and evaluated for inhibitory activity. The phosphonamidoic acids were shown to be weak competitive inhibitors while both a phosphoramidate diester and a phosphonamidate ester were shown to be potent time-dependent inactivators, presumably through irreversible phosphorylation of an active site nucleophile.

Publication types

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

MeSH terms

  • Drug Evaluation
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Kinetics
  • Phosphorus / analysis*
  • Phosphorylation
  • gamma-Glutamyl Hydrolase / antagonists & inhibitors*
  • gamma-Glutamyl Hydrolase / metabolism

Substances

  • Enzyme Inhibitors
  • Phosphorus
  • gamma-Glutamyl Hydrolase