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Plasminogen activator inhibitor-1 （PAI-1）, a member of the serine protease inhibitor （serpin） superfamily with antiprotease activity, is the main physiological inhibitor of tissue-type （tPA） and urokinase-type （uPA） plasminogen activators （PAs）. Apart from being crucially involved in fibrinolysis and wound healing, PAI-1 plays a pivotal role in various acute and chronic pathophysiological processes, including cardiovascular disease, tissue fibrosis, cancer, and age-related diseases.