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Protein tyrosine phosphatase receptor type B (PTPRB, also known as VE-PTP) is a single-pass transmembrane protein belonging to the receptor-type protein tyrosine phosphatase family, specifically expressed in endothelial cells. It features an extracellular region with multiple fibronectin type III repeats, a transmembrane domain, and one intracellular catalytic phosphatase domain. PTPRB plays a fundamental role in angiogenesis and the maintenance and remodeling of blood vessels by dephosphorylating key tyrosine kinase receptors (including VEGFR-2 and Tie2) and cell adhesion molecules, such as VE-cadherin. It acts as a critical negative regulator of tyrosine kinase signaling in vascular endothelial cells, ensuring vascular stability, inhibiting uncontrolled vessel growth, and regulating permeability. Mutations or dysregulation of PTPRB are implicated in various vascular tumors and other cancers. No approved drug targets PTPRB directly, but its essential role in vascular biology makes it a potential therapeutic target and biomarker for angiogenesis-related diseases[1][2][5][6].
Inhibition of phosphatase activity (e.g., by small molecule or metal ion inhibitors, such as zinc(II)) Modulation of receptor tyrosine kinase signaling through dephosphorylation of substrates (e.g., VEGFR-2, Tie2, Met)
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