Evaluation of phosphorus-containing inhibitors of gamma-glutamyl hydrolase.
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.
Rodriguez
C E
CE
Department of Chemistry & Biochemistry, San Francisco State University, CA 94132, USA.
Holmes
H M
HM
Mlodnosky
K L
KL
Lam
V Q
VQ
Berkman
C E
CE
D004341:Drug Evaluation; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D010758:Phosphorus / Q000032:analysis*; D010766:Phosphorylation; D011623:gamma-Glutamyl Hydrolase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D004791:Enzyme Inhibitors; D010758:Phosphorus; D011623:gamma-Glutamyl Hydrolase