General features of the heparin-binding serpins antithrombin, heparin cofactor II and protein C inhibitor.

General features of the heparin-binding serpins antithrombin, heparin cofactor II and protein C inhibitor.
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肝素结合丝氨酸蛋白酶抑制剂抗凝血酶、肝素辅因子 II 和蛋白 C 抑制剂的一般特征。

DOI:
10.1097/00001721-199306000-00013
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发表时间:
1993
期刊:
Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis
影响因子:
--
通讯作者:
Church,FC
Church,FC
中科院分区:
--
文献类型:
--
作者:
Pratt,CW;Church,FC

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血浆丝氨酸蛋白酶抑制剂(丝氨酸蛋白酶抑制剂)是糖蛋白,其活性参与许多重要的稳态反应。肝素依赖性血浆丝氨酸蛋白酶抑制剂、抗凝血酶、肝素辅因子 II 和蛋白 C 抑制剂,调节凝血的蛋白酶。肝素和一些其他糖胺聚糖可增加这三种血浆丝氨酸蛋白酶抑制蛋白的蛋白酶抑制率。蛋白酶识别靠近丝氨酸蛋白酶抑制剂羧基末端的特定肽,称为反应位点(对于抗凝血酶和蛋白 C 抑制剂,这是 Arg-Ser,对于肝素辅因子 II,这是 Leu-Ser)。此外,这三种丝氨酸蛋白酶抑制剂含有赋予糖胺聚糖结合活性的独特结构元件。据信,糖胺聚糖肝素的治疗性抗凝作用部分取决于抗凝血酶对蛋白酶的肝素加速抑制。特定蛋白聚糖的生理重要性归因于它们对这些丝氨酸蛋白酶抑制剂的识别以及它们对这些蛋白酶抑制剂的生物“激活”。
The blood plasma serine proteinase inhibitors (serpins) are glycoproteins whose activities are involved in many important homeostatic reactions. The heparin-dependent plasma serpins, antithrombin, heparin cofactor II and protein C inhibitor, regulate the proteinases of blood coagulation. Heparin and some other glycosaminoglycans increase the rate of proteinase inhibition by these three plasma serpins. Proteinases recognize a specific peptide, termed the reactive site, near the carboxyl-terminus of serpins (for antithrombin and protein C inhibitor this is Arg-Ser and for heparin cofactor II this is Leu-Ser). Additionally, these three serpins contain unique structural elements that confer glycosaminoglycan binding activities. The therapeutic anticoagulant action of the glycosaminoglycan heparin is believed to depend partially on heparin-accelerated inhibition of proteinases by antithrombin. The physiological importance of specific proteogly-cans has been attributed to their recognition of these serpins and their biological'activation'of these proteinase inhibitors.