Target intelligence / Profile preview

Macrophage-stimulating 1 receptor (MST1R) (MST1R)

Target
MST1R
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

Macrophage-stimulating 1 receptor (MST1R), commonly known as RON (Récepteur d'Origine Nantais), is a transmembrane receptor tyrosine kinase and a member of the MET proto-oncogene family [1, 3]. It is primarily expressed on epithelial cells and macrophages, where it plays a critical role in regulating cell survival, migration, and the immune response upon binding its ligand, macrophage-stimulating protein (MSP) [1, 5]. In physiological conditions, MST1R signaling is involved in wound healing and the modulation of inflammatory pathways to maintain tissue homeostasis [1, 6]. However, the receptor is frequently overexpressed or dysregulated in various malignancies, such as pancreatic, breast, and colorectal cancers, where it promotes epithelial-mesenchymal transition, metastasis, and resistance to apoptosis [1, 2]. Because of its prominent role in tumor progression and the immune microenvironment, MST1R has become a significant therapeutic target [1, 4]. Current drug development efforts include small molecule kinase inhibitors, monoclonal antibodies, and antibody-drug conjugates designed to block its oncogenic signaling [1, 6]. Despite its potential, therapeutic challenges remain, including the emergence of constitutively active splice variants like short-form RON (sf-RON) and complex cross-talk with other receptors like MET and EGFR [1, 2].

Other names
RONRécepteur d'Origine NantaisCD136PTK8Macrophage-stimulating protein receptorc-Met-related tyrosine kinaseNPCA3SEA
02

Mechanism of action

Tyrosine kinase inhibition, Monoclonal antibody binding, Ligand sequestration

03

Biological functions

Signal transductionCell proliferationCell migrationCell survivalImmune responseInflammationWound healing
04

Disease associations

CancerInflammationOther (Fibrosis)
05

Safety considerations

HyperglycemiaNeutropeniaTherapeutic resistance due to isoformsOff-target toxicity
06

Interacting drugs

Narnatumab

6 more in the full profile.

07

Biomarkers

RON overexpression (IHC)MST1R gene amplification (FISH/qPCR)sf-RON expressionMST1 ligand levels

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