INHIBITION OF AMINOPEPTIDASES BY N-AMINOACYL-O-4-NITROBENZOYL HYDROXAMATES

被引：7

作者：

DEMUTH, HU

STOCKEL, A

SCHIERHORN, A

FITTKAU, S

KIRSCHKE, H

BROMME, D

机构：

[1] MARTIN LUTHER UNIV HALLE WITTENBERG,DEPT BIOCHEM & BIOTECHNOL,O-4010 HALLE,GERMANY

[2] MARTIN LUTHER UNIV HALLE WITTENBERG,INST BIOCHEM,O-4010 HALLE,GERMANY

[3] NATL RES COUNCIL CANADA,BIOTECHNOL RES INST,MOLEC BIOL SECT,MONTREAL,QUEBEC,CANADA

来源：

BIOCHIMICA ET BIOPHYSICA ACTA | 1993年 / 1202卷 / 02期

关键词：

AMINOPEPTIDASE; ENZYME INHIBITION; DIACYLHYDROXAMATE; HYDROXAMATE;

D O I：

10.1016/0167-4838(93)90014-I

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

10 N-aminoacyl-O-4-nitrobenzoyl hydroxamates were investigated as potential inhibitors of aminopeptidases. While the metal-depending enzymes aminopeptidase M, aminopeptidase P and leucine aminopeptidase were inhibited reversibly by the compounds, the thiol enzyme cathepsin H was inhibited efficently in time-dependent reactions according to its substrate specificity. N-phenylalanyl-O-4-nitrobenzoyl hydroxamate was shown to be most effective, exhibiting a second-order-rate constant of inhibitition of 31 766 M-1 s-1.

引用

页码：265 / 270

页数：6

共 15 条

[1]

BARRETT AJ, 1981, METHOD ENZYMOL, V80, P535

[2] POTENT AND SELECTIVE INACTIVATION OF CYSTEINE PROTEINASES WITH N-PEPTIDYL-O-ACYL HYDROXYLAMINES [J].