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肽基重氮甲基酮和肽基锍盐对癌促凝剂的抑制作用。

Inhibition of cancer procoagulant by peptidyl diazomethyl ketones and peptidyl sulfonium salts.

作者信息

Falanga A, Shaw E, Donati M B, Consonni R, Barbui T, Gordon S

机构信息

Mario Negri Institute, Milan, Italy.

出版信息

Thromb Res. 1989 Jun 1;54(5):389-98. doi: 10.1016/0049-3848(89)90209-0.

Abstract

Cancer procoagulant (CP) is a cysteine proteinase from cancer cells that initiates blood coagulation. Members of two classes of unique and highly specific cysteine proteinase inhibitors, peptidyl diazomethyl ketones (PDK) and peptidyl sulfonium salts (PSS), were studied to determine whether or not they inhibited CP. The inhibitors did not impair the activity of the coagulation system. There was a differential inhibitory effect of the 6 PDK and 2 PSS inhibitors, influenced by the amino acid composition or sequence of the peptide moiety, that suggests differences in structural features of the active site of CP and papain. CP was inhibited by both classes of inhibitors.

摘要

癌促凝物质(CP)是一种来自癌细胞的半胱氨酸蛋白酶,可启动血液凝固。研究了两类独特且高度特异性的半胱氨酸蛋白酶抑制剂,即肽基重氮甲基酮(PDK)和肽基锍盐(PSS)的成员,以确定它们是否抑制CP。这些抑制剂不会损害凝血系统的活性。6种PDK和2种PSS抑制剂存在差异抑制作用,受肽部分的氨基酸组成或序列影响,这表明CP和木瓜蛋白酶活性位点的结构特征存在差异。两类抑制剂均能抑制CP。

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