INACTIVATION OF CALPAIN BY PEPTIDYL FLUOROMETHYL KETONES

被引：61

作者：

ANGLIKER, H ^{[1
]}

ANAGLI, J ^{[1
]}

SHAW, E ^{[1
]}

机构：

[1] FRIEDRICH MIESCHER INST, POB 2543, CH-4002 BASEL, SWITZERLAND

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 02期

关键词：

D O I：

10.1021/jm00080a003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The syntheses of Z-Leu-Leu-Tyr-CH2F (1) and Z-Tyr-Ala-CH2F (3) are described. The ability of Z-Leu-Leu-Tyr-CH2F (1) and Z-Leu-Tyr-CH2F (2) to inactivate in vitro calcium-activated proteinase from chicken gizzard are compared. Like the analogous diazomethyl ketones 4 and 5, these inhibitors were also found to inactivate cathepsin L in common with other inhibitors under current investigation. However, other specific inactivators for cathepsin L are available, for example, the fluoromethyl ketone 3 and diazomethyl ketone 6 of Z-Tyr-Ala-OH, which have no effect on the calcium-activated proteinase and therefore provide control inhibitors for observations made with Z-Leu-Leu-Tyr-CH2F (1).

引用

页码：216 / 220

页数：5

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