Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

MST1R (Q04912) - Overview - Molecular Target Synopsis

Protein


MST1R, Macrophage-stimulating protein receptor
Enzyme Classification 2.7.10.1
UniProt Q04912

Also Known as RON_HUMAN, MST1R, PTK8, RON

Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to MST1 ligand. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces autophosphorylation of RON on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with the PI3-kinase subunit PIK3R1, PLCG1 or the adapter GAB1. Recruitment of these downstream effectors by RON leads to the activation of several signaling cascades including the RAS-ERK, PI3 kinase-AKT, or PLCgamma-PKC. RON signaling activates the wound healing response by promoting epithelial cell migration, proliferation as well as survival at the wound site. Plays also a role in the innate immune response by regulating the migration and phagocytic activity of macrophages. Alternatively, RON can also promote signals such as cell migration and proliferation in response to growth factors other than MST1 ligand. Heterodimer of an alpha chain and a beta chain which are disulfide linked. Binds PLXNB1. Associates with and is negatively regulated by HYAL2. Interacts when phosphorylated with downstream effectors including PIK3R1, PCLG1, GRB2 and GAB1. Interacts with integrin beta1/ITGB1 in a ligand-independent fashion.

4QT8
CRYSTAL STRUCTURE OF RON SEMA-PSI-IPT1 EXTRACELLULAR DOMAINS IN COMPLEX WITH MSP BETA-CHAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for MST1R

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MST1R is active in the following subcellular-locations: membrane.
GO terms: MST1R is active in the following subcellular-locations: cell surface, integral component of plasma membrane, plasma membrane, receptor complex, stress fiber, vacuole.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MST1R has gain in 0 cell-lines, loss in 7 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H322M, HT29, HCC_2998

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H2347, NCI-H1869, LS1034

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HMEC, K562, HeLa-S3

(see details)

RNA Interference


MST1R was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: BT474, CAL120. (see details)

3D Structures


For MST1R there are:
3 structures (4 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MST1R has been screened with 874 compounds (1463 bioactivities), 68 compounds have bioactivities that show binding affinity of <= 500nM (84 bioactivities). (see details)