Cysteinyl peptide inhibitors of Bacillus cereus zinc beta-lactamase

Authors
Bounaga, S Galleni, M Laws, AP Page, MI
Citation
S. Bounaga et al., Cysteinyl peptide inhibitors of Bacillus cereus zinc beta-lactamase, BIO MED CH, 9(2), 2001, pp. 503-510
Citations number
43
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
9
Issue
2
Year of publication
2001
Pages
503 - 510
Database
ISI
SICI code
0968-0896(200102)9:2<503:CPIOBC>2.0.ZU;2-P
Abstract
Several cysteinyl peptides have been synthesised and shown to be reversible competitive inhibitors of the Bacillus cereus metallo-beta -lactamase. The pH dependence of pK(i) indicates that the thiol anion displaces hydroxide ion from the active site zinc(II). D,D-Peptides bind to the enzyme better t han other diastereoisomers, which is compatible with the predicted stereoch emistry of the active site. (C) 2001 Elsevier Science Ltd. All rights reser ved.