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Protein tyrosine phosphatase receptor type B (PTPRB)

Target
PTPRB
Molecular classification
Enzyme (protein tyrosine phosphatase), Receptor (receptor-type protein tyrosine phosphatase), Cell adhesion molecule (contains fibronectin type III domains), Single-pass transmembrane protein
01

Overview

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].

Other names
VE-PTPReceptor-type tyrosine-protein phosphatase betaHPTP-BETAHPTPBPTPBR-PTP-BETAprotein tyrosine phosphatase, receptor type B
02

Mechanism of action

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)

03

Biological functions

Regulation of signal transduction (especially tyrosine phosphorylation)Blood vessel remodeling and angiogenesis (vasculature development and maintenance)Negative regulation of receptor tyrosine kinase signaling (e.g., TIE2, VEGFR-2 / KDR, Met)Maintenance of endothelial cell contact integrity and vascular permeabilityRegulation of cell adhesion, neurite growth, and neuronal differentiation
04

Disease associations

Cancer (e.g., angiosarcoma, breast angiosarcoma, colorectal cancer, carcinoma, sarcoma, CNS cancers)Cardiovascular disease (vascular development disorders)Embryonic lethality in knockout models (defective angiogenesis)Generalized epilepsy with febrile seizures plus, type 1Other (vascular permeability disorders)
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Safety considerations

Essential for vascular development; loss of function is embryonic lethal (suggesting risk of vascular side effects in inhibition)Possible impact on vascular permeability and endothelial barrier function if modulated therapeuticallyUnknown long-term impact of inhibition due to lack of marketed inhibitors
06

Interacting drugs

No approved drugs directly targeting PTPRB are listed in the retrieved sources

1 more in the full profile.

07

Biomarkers

PTPRB expression or mutation status in tumors (e.g., angiosarcoma with truncating mutations)Potential use in vascular tumor diagnostics and monitoring angiogenesis

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