Laboratory for Therapeutic and Diagnostic Antibodies, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, B-3000 Leuven, Belgium.
Int J Mol Sci. 2021 Mar 8;22(5):2721. doi: 10.3390/ijms22052721.
Plasminogen activator inhibitor-1 (PAI-1) is the main physiological inhibitor of plasminogen activators (PAs) and is therefore an important inhibitor of the plasminogen/plasmin system. Being the fast-acting inhibitor of tissue-type PA (tPA), PAI-1 primarily attenuates fibrinolysis. Through inhibition of urokinase-type PA (uPA) and interaction with biological ligands such as vitronectin and cell-surface receptors, the function of PAI-1 extends to pericellular proteolysis, tissue remodeling and other processes including cell migration. This review aims at providing a general overview of the properties of PAI-1 and the role it plays in many biological processes and touches upon the possible use of PAI-1 inhibitors as therapeutics.
纤溶酶原激活物抑制剂-1（PAI-1）是纤溶酶原激活物（PAs）的主要生理性抑制剂，因此也是纤溶酶原/纤溶系统的重要抑制剂。作为组织型 PA（tPA）的快速作用抑制剂，PAI-1 主要减弱纤维蛋白溶解。通过抑制尿激酶型 PA（uPA）以及与生物配体如 vitronectin 和细胞表面受体相互作用，PAI-1 的功能扩展到细胞周蛋白水解、组织重塑和其他过程，包括细胞迁移。本综述旨在概述 PAI-1 的特性及其在许多生物学过程中的作用，并探讨 PAI-1 抑制剂作为治疗剂的可能用途。
