Target intelligence / Profile preview

Recepteur d'origine nantais tyrosine kinase receptor (RON)

Target
RON
Molecular classification
Receptor tyrosine kinase, Receptor
01

Overview

Recepteur d'origine nantais tyrosine kinase receptor (RON, encoded by the *MST1R* gene) is a transmembrane receptor tyrosine kinase and a member of the MET proto-oncogene family. It is primarily expressed on epithelial cells, tissue-resident macrophages, and some immune cells. RON is activated by its ligand, macrophage-stimulating protein (MSP), and upon ligand binding mediates autophosphorylation, leading to downstream signaling cascades that control cell proliferation, survival, adhesion, migration, and inflammatory responses. RON plays a dual role: it restricts inflammation under normal physiologic conditions but is often overexpressed in various epithelial cancers, promoting oncogenesis, metastasis, and tumor immune evasion. Multiple structural domains confer ligand specificity and dimerization. Targeting RON with small molecule inhibitors and monoclonal antibodies is under investigation as an anti-cancer strategy, but no approved therapies exist yet. RON overexpression correlates with poor outcomes in several cancers, and ongoing research is focused on elucidating its precise roles in tumor biology and therapeutic response

Other names
MST1RMacrophage stimulating 1 receptorMST1R tyrosine kinaseRON receptor
02

Mechanism of action

Tyrosine kinase inhibition (kinase inhibitors block RON phosphorylation and downstream signaling); Antibody-mediated receptor blockade (prevents ligand binding and receptor activation); Promotion of receptor degradation or inhibition of dimerization

03

Biological functions

Signal transductionCell proliferationCell migrationCell invasionApoptosisRegulation of inflammation
04

Disease associations

CancerInflammationTumor progressionMetastasis
05

Safety considerations

Potential impairment of normal tissue homeostasis and innate immune response if RON signaling is excessively inhibitedChemoresistance in cancers with high RON activity, especially to drugs causing DNA double-strand breaksTumor microenvironment immune modulation raising risk of immune-related adverse events with some inhibitors
06

Interacting drugs

SU11274 (multi-kinase inhibitor, also targets c-MET)

2 more in the full profile.

07

Biomarkers

RON (MST1R) protein overexpression levels in tumor tissues (candidate biomarker for poor prognosis and therapy response in various cancers such as gastric, colon, breast, prostate, and others)

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