Competitive inhibition of a glutamate carboxypeptidase by phosphonamidothionate derivatives of glutamic acid

Authors
Rodriguez, CE Lu, HY Dinh, TT Mlodnosky, KL Dastgah, A Lam, VQ Nichols, CB Berkman, CE
Citation
Ce. Rodriguez et al., Competitive inhibition of a glutamate carboxypeptidase by phosphonamidothionate derivatives of glutamic acid, BIOORG MED, 9(10), 1999, pp. 1415-1418
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
10
Year of publication
1999
Pages
1415 - 1418
Database
ISI
SICI code
0960-894X(19990517)9:10<1415:CIOAGC>2.0.ZU;2-A
Abstract
Several N-thiophosphonyl-glutamates were found to be potent competitive inh ibitors of a zinc-dependent glutamyl hydrolase, carboxypeptidase G (CPG). W eak inhibition exhibited by an analogous N-phosphonyl-glutamate suggests th at the enhanced potency of the phosphonamidothioates is due to the presence of their sulfur ligand and its favorable interactions with active site fea tures, presumably zinc(II). (C) 1999 Elsevier Science Ltd. All rights reser ved.