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凝血因子Xa抑制剂:现状与未来。

Factor Xa inhibitors: today and beyond.

作者信息

Walenga Jeanine M, Jeske Walter P, Hoppensteadt Debra, Fareed Jawed

机构信息

Departments of Pathology and Thoracic-Cardiovascular Surgery, Loyola University Medical Center, 2160 S First Avenue, Maywood, IL 60153, USA.

出版信息

Curr Opin Investig Drugs. 2003 Mar;4(3):272-81.

Abstract

Serine proteases play an important role in thrombogenesis, the process that leads to blood clotting and conditions such as heart attack, stroke and other cardiovascular disorders. In the coagulation network, the activation of various serine proteases facilitates the formation of the serine protease Factor Xa, which plays a central role in the process of coagulation and platelet activation. Factor Xa is an essential component of the prothrombinase complex, from which thrombin is formed, which then directly leads to fibrin clot formation. Thus, the inhibition of Factor Xa and its generation is an important strategy in the development of new antithrombotic drugs.

摘要

丝氨酸蛋白酶在血栓形成过程中发挥着重要作用,血栓形成是导致血液凝固以及引发心脏病发作、中风和其他心血管疾病等状况的过程。在凝血网络中,各种丝氨酸蛋白酶的激活促进了丝氨酸蛋白酶Xa因子的形成,Xa因子在凝血和血小板激活过程中起着核心作用。Xa因子是凝血酶原酶复合物的重要组成部分,由该复合物形成凝血酶,进而直接导致纤维蛋白凝块的形成。因此,抑制Xa因子及其生成是开发新型抗血栓药物的一项重要策略。

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