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Angiostatin K1-3 is a ~30 kDa protein fragment derived from plasminogen, specifically comprising its first three kringle domains. It functions as a potent anti-angiogenic agent, inhibiting the formation of new blood vessels, which is crucial for tumor growth. Its mechanism of action involves inhibiting the proliferation and migration of human endothelial cells and inducing their apoptosis. Angiostatin K1-3 interacts with several targets on endothelial cells, including Fas, integrin alpha(v)beta3, and ATP synthase. It also binds to angiomotin and annexin II. Furthermore, it increases the expression of p53 protein and enhances FasL-mediated signaling pathways, while decreasing the activation of AKT. These actions collectively lead to the suppression of tumor growth. It has been investigated in experimental studies for its potential in treating human gliomas and other solid tumors.
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