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Target intelligence / Profile preview
C-ros oncogene 1 receptor tyrosine kinase (ROS1)
- Target
- ROS1
- Molecular classification
- Receptor Tyrosine Kinase, RTK
01
Overview
ROS1 (C-ros oncogene 1 receptor tyrosine kinase) is a receptor tyrosine kinase involved in cell growth, differentiation, and survival. In cancer, ROS1 gene fusions or activating mutations lead to constitutive kinase activation, driving tumorigenesis. ROS1 fusions are therapeutically targetable with small-molecule tyrosine kinase inhibitors like crizotinib and lorlatinib.
- Other names
- c-ros oncogene 1, receptor tyrosine kinaseROS-1ROS
02
Mechanism of action
Small-molecule tyrosine kinase inhibitors that bind to and inhibit the kinase activity of ROS1 fusion proteins or mutated ROS1, blocking downstream signaling pathways.
03
Biological functions
Cell growthCell differentiationCell migrationCell survivalSignal transductionEpithelial cell differentiationRegionalization of tissues
04
Disease associations
CancerNon-small cell lung cancer (NSCLC)Gastric cancerColorectal cancerSpitzoid melanomaCholangiosarcomaGlioblastoma
05
Safety considerations
Resistance to tyrosine kinase inhibitors (TKIs) can develop over time.Off-target effects of TKIsSpecific toxicities associated with individual TKIs (e.g., visual disturbances, edema, hepatotoxicity)
06
Interacting drugs
Crizotinib
1 more in the full profile.
07
Biomarkers
ROS1 fusions (e.g., CD74-ROS1, SLC34A2-ROS1, EZR-ROS1, TPM3-ROS1, FIG-ROS1)ROS1 D2113N mutationPD-L1 expression
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