Target intelligence / Profile preview

Receptor-type tyrosine-protein phosphatase sigma (PTPRS (or RPTPσ))

Target
PTPRS (or RPTPσ)
Molecular classification
Receptor, Enzyme, Receptor protein tyrosine phosphatase, Cell adhesion molecule
01

Overview

Receptor-type protein tyrosine phosphatase sigma (PTPRS or RPTPσ) is a transmembrane receptor belonging to the type IIB subfamily of receptor-type protein tyrosine phosphatases[2][4]. It consists of an extracellular region with immunoglobulin-like (Ig) and fibronectin type III (FNIII) domains that mediate cell adhesion and interactions with extracellular matrix proteins (including proteoglycans), a single transmembrane domain, and two intracellular phosphatase domains (D1 and D2) responsible for signal transduction via dephosphorylation of specific tyrosine residues[2][4][7]. RPTPσ plays a crucial role in neuronal development, particularly in axon growth, synaptogenesis, and in the response to neural injury by modulating the effects of chondroitin sulfate proteoglycans (CSPG) and heparan sulfate proteoglycans (HSPG)[2][8]. Altered function or expression of RPTPσ has been implicated in neuroregeneration failure, ocular diseases like glaucoma (via modulating trabecular meshwork cell matrix balance), and may be linked to tumorigenesis and other neurological disorders[2][4][7]. Currently, there are no clinically approved drugs specifically targeting RPTPσ, but research focuses on modulating its activity for neuroregenerative or anti-fibrotic therapies[7].

Other names
RPTP sigmaPTPσProtein tyrosine phosphatase sigmaLAR family receptor protein tyrosine phosphatase sigmaPTPRSCDw338
02

Mechanism of action

Inhibition of tyrosine phosphatase activity (for experimental inhibitors)[7] Regulation of extracellular matrix interaction (by modulating proteoglycans)[2][4][7]

03

Biological functions

Neural developmentSignal transductionSynaptogenesisCell adhesionRegulation of phosphorylationModulation of matrix metalloproteinase activity
04

Disease associations

Neurodegenerative diseaseNervous system injury/repairGlaucoma/eye diseasesCancer (role under investigation; evidence for tumor-suppressive and possibly oncogenic activity in different contexts)
05

Safety considerations

Potential effects on neural development and synapse formation (targeting may impact neurodevelopment or repair)[2][4]Potential effects on extracellular matrix remodeling and cell adhesion (modulation could influence tissue integrity or invasiveness)[2][7]
06

Interacting drugs

No approved drugs, but experimental inhibitors such as PTP-IV have been reported[7]
07

Biomarkers

Expression levels in neural tissue (potential, but not widely used clinically)[7]

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