Factor XIIIa inhibitors as potential novel drugs for venous thromboembolism.
Factor XIIIa inhibitors as potential novel drugs for venous thromboembolism.
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DOI：
10.1016/j.ejmech.2020.112442
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发表时间：
2020-08-15
影响因子：
6.7
通讯作者：
Kar S
中科院分区：
文献类型：
--
作者：
Al-Horani RA;Kar S
人因子XIIIa（FXIIIa）是一种多功能转谷氨酰胺酶，具有重要的止血作用。FXIIIa催化凝血过程的最后一步。它通过交联纤维蛋白的α链和γ链来稳定血栓。它还保护新形成的凝块免受纤溶酶介导的纤维蛋白溶解，主要是通过将α2-抗纤溶酶与纤维蛋白交联。此外，FXIIIa是凝块大小和凝块红细胞含量的主要决定因素。因此，靶向FXIIIa的抑制剂已被认为是开发新一代抗凝剂以预防和/或治疗静脉血栓栓塞。已经发现或设计了几种FXIIIa的抑制剂，包括活性位点和变构位点小分子抑制剂以及天然和修饰的多肽。这项工作回顾了FXIIIa抑制剂的结构，生物化学和药理学方面，以推进其分子设计，变得更加临床相关。
Human factor XIIIa (FXIIIa) is a multifunctional transglutaminase with a significant role in hemostasis. FXIIIa catalyzes the last step in the coagulation process. It stabilizes the blood clot by cross-linking the α- and γ-chains of fibrin. It also protects the newly formed clot from plasmin-mediated fibrinolysis, primarily by cross-linking α2-antiplasmin to fibrin. Furthermore, FXIIIa is a major determinant of clot size and clot’s red blood cells content. Therefore, inhibitors targeting FXIIIa have been considered to develop a new generation of anticoagulants to prevent and/or treat venous thromboembolism. Several inhibitors of FXIIIa have been discovered or designed including active site and allosteric site small molecule inhibitors as well as natural and modified polypeptides. This work reviews the structural, biochemical, and pharmacological aspects of FXIIIa inhibitors so as to advance their molecular design to become more clinically relevant.
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