Evaluation of phosphorus-containing inhibitors of gamma-glutamyl hydrolase. 1998

C E Rodriguez, and H M Holmes, and K L Mlodnosky, and V Q Lam, and C E Berkman
Department of Chemistry & Biochemistry, San Francisco State University, CA 94132, USA.

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.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D010758 Phosphorus A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions. Black Phosphorus,Phosphorus-31,Red Phosphorus,White Phosphorus,Yellow Phosphorus,Phosphorus 31,Phosphorus, Black,Phosphorus, Red,Phosphorus, White,Phosphorus, Yellow
D010766 Phosphorylation The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety. Phosphorylations
D011623 gamma-Glutamyl Hydrolase Catalyzes the hydrolysis of pteroylpolyglutamic acids in gamma linkage to pterolylmonoglutamic acid and free glutamic acid. EC 3.4.19.9. Conjugase,Folate Conjugase,Folyl Conjugate Synthetase,Pteroyl Polyglutamate Hydrolase,Carboxypeptidase G,Carboxypeptidase G1,Carboxypeptidase G2,Folacin Conjugase,Folate Hydrolyzing Enzyme,Folyl Poly-gamma-Glutamate Carboxypeptidase,Folyl Polyglutamate Cleavage Enzyme,Folylpolyglutamate Hydrolase,gamma Glutamyl Hydrolase
D004341 Drug Evaluation Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals. Evaluation Studies, Drug,Drug Evaluation Studies,Drug Evaluation Study,Drug Evaluations,Evaluation Study, Drug,Evaluation, Drug,Evaluations, Drug,Studies, Drug Evaluation,Study, Drug Evaluation
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme

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