PROBING THE SPECIFICITY OF THE S-1 BINDING-SITE OF M222 MUTANTS OF SUBTILISIN B-LENTUS WITH BORONIC ACID INHIBITORS

Authors
STABILE MR LAI WG DESANTIS G GOLD M JONES JB
Citation
Mr. Stabile et al., PROBING THE SPECIFICITY OF THE S-1 BINDING-SITE OF M222 MUTANTS OF SUBTILISIN B-LENTUS WITH BORONIC ACID INHIBITORS, Bioorganic & medicinal chemistry letters, 6(21), 1996, pp. 2501-2506
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
21
Year of publication
1996
Pages
2501 - 2506
Database
ISI
SICI code
0960-894X(1996)6:21<2501:PTSOTS>2.0.ZU;2-P
Abstract
Specificity differences between the S-1-pockets of subtilisin B. lentu s (SBL), and its M222C/S mutants have been explored with boronic acid inhibitors. Similar binding trends were noted, with 2,4-dichlorophenyl boronic acid being the best overall inhibitor for each enzyme. In addi tion, a correlation between inhibitor binding and the electrophilicity of boron was found for both the M222C and M222S enzymes. Copyright (C ) 1996 Elsevier Science Ltd