Target intelligence / Profile preview

Receptor-type tyrosine-protein phosphatase T (PTPRT)

Target
PTPRT
Molecular classification
Enzyme (Protein tyrosine phosphatase), Receptor, Cell adhesion molecule, Signaling protein
01

Overview

Receptor-type tyrosine-protein phosphatase T (PTPRT) is a transmembrane enzyme belonging to the protein tyrosine phosphatase (PTP) family, primarily expressed in the central nervous system. It contains extracellular domains (MAM, Ig-like, fibronectin type III), a single transmembrane region, and two intracellular catalytic domains, the first of which is enzymatically active. PTPRT regulates cell signaling by dephosphorylating substrates involved in cell adhesion, growth, and differentiation—playing a critical role in neuronal development, synapse formation, and functioning as a tumor suppressor in various cancers. Mutation or loss of function in PTPRT is associated with enhanced STAT3 activity, disrupted cell-cell adhesion, impaired neuronal connectivity, and increased cancer risk.

Other names
Protein tyrosine phosphatase receptor type TPTPrhoPTPρRPTPrhoReceptor-type tyrosine-protein phosphatase rhoKIAA0283R-PTP-TRPTP-rho
02

Mechanism of action

Noted as a tumor suppressor that functions by dephosphorylating substrates such as STAT3 (affecting gene expression), paxillin (regulating tumorigenicity), and proteins involved in synapse formation. A drug targeting PTPRT would likely restore or enhance phosphatase activity, inhibit detrimental downstream signaling, or modulate cell adhesion, but no such drugs are in clinical use as of 2024.

03

Biological functions

Signal transductionCell adhesionRegulation of cell growth and differentiationCell cycle regulationRegulation of synapse formationTumor suppressionRegulation of STAT3 signalingDendritic arborization
04

Disease associations

Cancer (notably colon, lung, skin, and stomach cancers)Glioma susceptibilityHematologic malignanciesPotential role in neurodevelopmental disorders
05

Safety considerations

Potential impact on CNS function and neuronal development due to its role in synapse formation and neuronal adhesionTargeting PTPRT may affect normal cell signaling, raising concerns about off-target effects or neurodevelopmental toxicity
06

Interacting drugs

None identified in clinical use or late-stage development, as of 2024
07

Biomarkers

STAT3 phosphorylation statusPaxillin tyrosine 88 phosphorylationGenetic mutations in PTPRT (notably in tumor samples)

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