Strategies for development of novel antithrombotics: modulating thrombin's procoagulant and anticoagulant properties

被引：7

作者：

Hall, SW ^{[1
]}

Gibbs, CS ^{[1
]}

Leung, LLK ^{[1
]}

机构：

[1] GILEAD SCI INC,FOSTER CITY,CA

来源：

CELLULAR AND MOLECULAR LIFE SCIENCES | 1997年 / 53卷 / 09期

关键词：

thrombin; structure; mutagenesis; protein C; allosteric;

D O I：

10.1007/s000180050092

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：

Thrombin is a serine proteinase that can interact with a large number of diverse macromolecular substrates, which results in either a procoagulant or anticoagulant effect. These divergent properties are physiologically regulated by the endogenous protein thrombomodulin. This review summarizes recent work on a variety of methods used to exploit the allosteric nature of the enzyme. The procoagulant and anticoagulant functions of thrombin can be modulated by sodium binding, site-directed mutagenesis, and a small synthetic molecule. Modulation of thrombin's intrinsic properties represents a novel approach to the development of unique antithrombotic agents.

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收藏

页码：731 / 736

页数：6

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