De Meyer Simon F, De Maeyer Bauke, Deckmyn Hans, Vanhoorelbeke Karen
Laboratory for Thrombosis Research, IRC, KU Leuven Campus Kortrijk, E. Sabbelaan 53, 8500 Kortrijk, Belgium.
Cardiovasc Hematol Disord Drug Targets. 2009 Mar;9(1):9-20. doi: 10.2174/187152909787581327.
One of the key players in many thrombotic complications is von Willebrand factor (VWF), a large, multimeric glycoprotein that is present in plasma where it fulfils a crucial role in haemostasis. First, VWF recruits platelets to vascular lesions by acting as a linker molecule between the exposed collagen and free-flowing platelets in the circulation. Second, by serving as a carrier protein for the coagulation factor VIII, VWF protects this anti-haemophilic factor from rapid degradation. Quantitative or qualitative defects in VWF result in the most common bleeding disorder in man, known as von Willebrand disease, illustrating the central role of VWF in haemostasis. On the other hand, a thrombotic risk emerges when over-reactive VWF molecules can bind spontaneously to platelets. It is clear that because of its pivotal role in maintaining the fine balance between bleeding and thrombosis, VWF is an attractive but delicate drug target. This review focuses on the role of VWF in both haemostasis and thrombosis with special attention to the molecule as drug and drug target respectively.
在许多血栓形成并发症中,关键因素之一是血管性血友病因子(VWF),它是一种大型多聚体糖蛋白,存在于血浆中,在止血过程中发挥着关键作用。首先,VWF通过充当暴露的胶原蛋白与循环中自由流动的血小板之间的连接分子,将血小板募集到血管损伤部位。其次,作为凝血因子VIII的载体蛋白,VWF保护这种抗血友病因子不被快速降解。VWF的定量或定性缺陷会导致人类最常见的出血性疾病,即血管性血友病,这说明了VWF在止血中的核心作用。另一方面,当过度活跃的VWF分子能自发地与血小板结合时,就会出现血栓形成风险。很明显,由于VWF在维持出血和血栓形成之间的精细平衡中起着关键作用,它是一个有吸引力但又很微妙的药物靶点。本综述重点关注VWF在止血和血栓形成中的作用,特别分别关注该分子作为药物和药物靶点的情况。