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Tissue Factor/Factor FVII Complex Inhibitors in Cardiovascular Disease. Are Things Going Well?

机译:心血管疾病中的组织因子/因子FVII复合抑制剂。事情进展顺利吗?

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摘要

Blood coagulation is a complex biological mechanism aimed to avoid bleeding in which a highly regulated and coordinated interplay of specific proteins and cellular components respond quickly to a vascular injury. However, when this mechanisms occurs in the coronary circulation, it has not a “protective” effect, but rather, it plays a pivotal role in determining acute coronary syndromes. Coagulation recognizes Tissue Factor (TF), the main physiological initiator of the extrinsic coagulation pathway, as its starter.Since TF:VIIa complex is the critical point of the blood coagulation cascade, it is a pharmacological attractive issue for the development of agents with anti thrombotic properties that can exert their activity by inhibiting complex formation and/or its catalytic activity. In fact, it is intuitive that an antithrombotic agent able to inhibit this initial step of the coagulation pathway has several theoretical, extremely important, advantages if compared with drugs active downstream the coagulation pathway, such as FXa or thrombin. The present report gives a brief overview of TF pathophysiology, highlighting the most recent advances in the field of inhibitors of the complex TF/VIIa potentially useful in cardiovascular disease.
机译:凝血是一种复杂的生物学机制,旨在避免出血,在出血中,高度调节和协调的特定蛋白质和细胞成分之间的相互作用会迅速响应血管损伤。但是,当这种机制发生在冠状动脉循环中时,它没有“保护”作用,而是在确定急性冠状动脉综合征中起着关键作用。凝血将外源性凝血途径的主要生理引发剂组织因子(TF)视为其起始剂。由于TF:VIIa复合物是凝血级联反应的关键点,因此对于开发具有抗凝血作用的药物而言,这是一个药理上的诱人问题可通过抑制复合物的形成和/或其催化活性发挥其活性的血栓形成特性。实际上,直觉上能够与凝血途径下游有活性的药物(例如FXa或凝血酶)相比,能够抑制凝血途径这一初始步骤的抗血栓形成剂具有若干理论上极其重要的优势。本报告简要概述了TF的病理生理,重点介绍了可能在心血管疾病中有用的复杂TF / VIIa抑制剂领域的最新进展。

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