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Target intelligence / Profile preview
Receptor tyrosine kinase c-ros oncogene 1 (ROS1)
- Target
- ROS1
- Molecular classification
- Receptor tyrosine kinase, Type I integral membrane protein, Insulin receptor family
01
Overview
Receptor tyrosine kinase c-ros oncogene 1 (ROS1) is a type I integral membrane protein with intrinsic tyrosine kinase activity. It functions as a growth or differentiation factor receptor, playing a role in epithelial cell differentiation. In cancer, chromosomal rearrangements can create fusion genes involving ROS1, leading to constitutive activation of its kinase function and driving oncogenesis. It is a therapeutic target in cancers such as non-small cell lung cancer (NSCLC), with several small-molecule inhibitors developed to target its aberrant activity.
02
Mechanism of action
Small-molecule inhibitors that target aberrant ROS1 kinase activity
03
Biological functions
Growth factor receptorDifferentiation factor receptorEpithelial cell differentiationEpithelial regionalizationSignal transductionCell proliferationCell survivalCell growth
04
Disease associations
CancerNon-small cell lung cancer (NSCLC)
05
Safety considerations
Resistance to first-generation inhibitors
06
Interacting drugs
Crizotinib
1 more in the full profile.
07
Biomarkers
ROS1 fusionsActivating ROS1 mutations
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