INHIBITORS OF HUMAN NEUTROPHIL CATHEPSIN-G - STRUCTURAL AND BIOCHEMICAL-STUDIES

被引：22

作者：

GROUTAS, WC

BRUBAKER, MJ

VENKATARAMAN, R

EPP, JB

STANGA, MA

MCCLENAHAN, JJ

机构：

[1] Department of Chemistry, Wichita State University, Wichita

来源：

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS | 1992年 / 294卷 / 01期

关键词：

D O I：

10.1016/0003-9861(92)90148-P

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：

The interaction of a series of sulfonate and phosphate esters derived from N-hydroxysuccinimide with human leukocyte cathepsin G was investigated. The synthesized compounds were found to be time-dependent inhibitors of the enzyme. The composite interplay of steric and electronic effects leads to the formation of acyl enzymes of variable stability, ultimately resulting in partial or full recovery of enzymatic activity. Compounds acting via phosphorylation of the active site serine inactivated the enzyme rapidly and irreversibly. © 1992.

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页码：144 / 146

页数：3

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