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Target intelligence / Profile preview
Plasminogen Activator Inhibitor 1 (PAI-1)
- Target
- PAI-1
- Molecular classification
- Serine Protease Inhibitor, Serpin
01
Overview
Plasminogen activator inhibitor 1 (PAI-1) is a serine protease inhibitor (serpin) that inhibits tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), key enzymes in fibrinolysis. By inhibiting these enzymes, PAI-1 prevents the conversion of plasminogen to plasmin, thus stabilizing blood clots. Elevated PAI-1 levels are associated with an increased risk of thrombosis, cardiovascular disease, cancer progression, and fibrosis, making it a potential therapeutic target. Conversely, PAI-1 deficiency leads to excessive fibrinolysis and bleeding disorders.
- Other names
- Serpin E1Endothelial Plasminogen Activator Inhibitor
02
Mechanism of action
Inhibition of tPA and uPA activity, preventing plasminogen activation and subsequent fibrinolysis.
03
Biological functions
Fibrinolysis inhibitionWound healingRegulation of cell migrationRegulation of tissue remodelingRegulation of pericellular proteolysisCell adhesion
04
Disease associations
ThrombosisCancerFibrosisMetabolic SyndromeCardiovascular diseaseAtherosclerosisHemorrhagic diathesisAging-related diseases
05
Safety considerations
Inhibition may increase bleeding riskPotential for off-target effects due to serpin family homologyLong-term effects of PAI-1 inhibition on wound healing and tissue remodeling need to be evaluated
06
Biomarkers
Elevated PAI-1 levels in plasma/serum as a marker of thrombotic riskPAI-1 expression levels in tumor tissue as a prognostic marker in cancer
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