PAI-1 antagonists: the promise and the peril.
PAI-1 antagonists: the promise and the peril.
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发表时间：
2011
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通讯作者：
D. Vaughan
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作者：
D. Vaughan
纤溶酶原激活剂（即，纤溶系统是抗血管内血栓形成的关键内源性防御机制之一。血栓溶解剂代表了增强人体纤维蛋白溶解活性的唯一直接途径，并且已被证明在急性心肌梗死和中风的治疗中具有价值。虽然这些药物在急性环境中有效，但它们不是长期使用的可行选择。血浆中的净纤溶活性在很大程度上取决于组织型纤溶酶原激活物（t-PA）及其天然的快速作用抑制剂纤溶酶原激活物抑制剂-1（派-1）之间的平衡。特异性派-1拮抗剂的最新发展有望扩大对纤溶系统在人类疾病中的作用的理解的限制，并突破目前的治疗选择的限制，可以有效地恢复和增强纤溶系统的活性。
The plasminogen activator (i.e., fibrinolytic) system is one of the key endogenous defense mechanisms against intravascular thrombosis. Thrombolytic agents represent the only direct way of augmenting fibrinolytic activity in humans, and have proven to be of value in the treatment of acute myocardial infarction and stroke. Although these agents are efficacious in the acute setting, they are not a viable option for long-term use. Net fibrinolytic activity is plasma is largely determined by the balance between tissue-type plasminogen activator (t-PA) and its natural, fast-acting inhibitor, plasminogen activator inhibitor-1 (PAI-1). The recent development of specific PAI-1 antagonists promises to expand the limits of understanding of the role of the fibrinolytic system in human disease, and to break through the current confines of therapeutic options that can effectively restore and augment the activity of the fibrinolytic system.