Plasminogen Activator Inhibitor-1
Plasminogen activator inhibitor-1 (PAI-1) is encoded by the SERPINE1 gene and is the primary regulator of the plasminogen activation system. High levels of this protein are a risk factor for thrombosis and atherosclerosis, and elevated blood levels are associated with poor clinical outcome and response to therapy in cancer patients.
Plasminogen Activator -1 Inhibitors |
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| Cat. No. | Product Name / Activity |
| 6187 | SK 216 |
| Plasminogen activator inhibitor-1 (PAI-1) inhibitor | |
| 5565 | Tiplaxtinin |
| Plasminogen activator inhibitor-1 (PAI-1) inhibitor | |
| 5769 | TM 5275 sodium salt |
| Plasminogen activator inhibitor-1 (PAI-1) inhibitor; orally bioavailable | |
| 6194 | TM 5441 |
| Plasminogen activator inhibitor-1 (PAI-1) inhibitor | |
Plasminogen activator inhibitor-1 (PAI-1) is a serine protease inhibitor, encoded by the SERPINE1 gene. High levels of this protein are a risk factor for thrombosis and atherosclerosis, and elevated blood levels are associated with poor clinical outcome and response to therapy in cancer patients.
PAI-1 is the primary regulator of the plasminogen activation system, through its inhibitory action on tissue plasminogen activator (tPA) and urokinase (uPA). Both tPA and uPA cleave plasminogen to give plasmin, activating the breakdown of fibrin and matrix metalloproteases (MPPs) which regulate extracellular matrix (ECM) turnover. PAI-1 therefore inhibits fibrinolysis, and regulates tissue homeostasis, wound healing and fibrosis through its inhibition of plasmin mediated MPP activation.
As well as tPA and uPA, PAI-1 binds to vitronectin, an ECM protein that promotes cell adhesion and stabilizes PAI-1 through its binding. It also binds to low-density lipoprotein receptor-related protein (LRP1), promoting cell migration.
Increased levels of PAI-1 are associated with various disease states including obesity, metabolic syndrome, cardiovascular disorders and some forms of cancer. In cancer, pro-tumorigenic factors such as tumor necrosis factor-α (TNFα), transforming growth factor-β (TGFβ) and interleukin-6 (IL-6) stimulate the production of PAI-1 by endothelial cells, fibroblasts and macrophages in the tumor microenvironment. PAI-1 is pro-angiogenic and inhibits spontaneous apoptosis in cancer cells, so is pro-tumorigenic.
External sources of pharmacological information for Plasminogen Activator Inhibitor-1 :
Literature for Plasminogen Activator Inhibitor-1
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Our Angiogenesis in Cancer poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
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