DESIGN OF A NEW SELECTIVE CYSTEINE PROTEASE INACTIVATOR AND ITS MECHANISTIC IMPLICATIONS

被引：16

作者：

ALBECK, A

PERSKY, R

KLIPER, S

机构：

[1] Department of Chemistry, Bar Ilan University, Ramat Gan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 16期

关键词：

D O I：

10.1016/0960-894X(95)00312-H

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cbz-Phe-epoxide was designed as a selective inactivator of cysteine proteases. It exhibits a time- and concentration-dependent inactivation of cysteine proteases, while showing no activity towards serine proteases. The inhibition is irreversible, correlated with loss of the free active-site thiol, and its rate is at least 10(4) faster than the rate of a model reaction in solution. These results support the proposed active-site directed, protonation-dependent, mechanism-based mode of inactivation of cysteine proteases by the new inhibitor.

引用

页码：1767 / 1772

页数：6

共 32 条

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