Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors

被引:83
作者
Nar, H [1 ]
Bauer, M
Schmid, A
Stassen, JM
Wienen, W
Priepke, HWM
Kauffmann, IK
Ries, UJ
Hauel, NH
机构
[1] Boehringer Ingelheim KG, Dept Med Chem, D-88397 Biberach, Germany
[2] Boehringer Ingelheim KG, Dept Cardiovasc & Metab Dis, D-88397 Biberach, Germany
关键词
D O I
10.1016/S0969-2126(00)00551-7
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
Background: A major current focus of pharmaceutical research is the development of selective inhibitors of the blood coagulation enzymes thrombin or factor Xa to be used as orally bioavailable anticoagulant drugs in thromboembolic disorders and in the prevention of venous and arterial thrombosis. Simultaneous direct inhibition of thrombin and factor Xa by synthetic proteinase inhibitors as a novel approach to antithrombotic therapy could result in potent anticoagulants with improved pharmacological properties.
引用
收藏
页码:29 / 37
页数:9
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