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.
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页码：1767 / 1772
页数：6
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