Target intelligence / Profile preview

Mutant Receptor Tyrosine Kinase (Mutant RTK)

Target
Mutant RTK
Molecular classification
Receptor, Enzyme, Protein Kinase, Receptor Tyrosine Kinase
01

Overview

Mutant receptor tyrosine kinases (RTKs) are altered forms of cell surface receptors that exhibit constitutive or dysregulated tyrosine kinase activity. These mutations, which can be germline or somatic, often lead to uncontrolled cell growth, survival, and proliferation, contributing to developmental disorders and various cancers. They are major targets for anticancer drugs.

Other names
Mutated Receptor Tyrosine KinaseActivating RTK mutantsOncogenic RTKs
02

Mechanism of action

Inhibition of tyrosine kinase activity, blockade of ligand binding

03

Biological functions

Signal transductionCell proliferationCell differentiationCell survivalApoptosis regulationCell migrationCell-to-cell communicationMorphogenesisAutophagy
04

Disease associations

CancerDevelopmental disorders
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Safety considerations

Off-target effectsDrug resistanceDevelopment of secondary malignanciesSpecific toxicities related to individual RTK inhibitors
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Interacting drugs

Small molecule inhibitors

1 more in the full profile.

07

Biomarkers

Specific RTK mutation types (e.g., EGFR mutations in lung cancer, MET mutations in renal carcinoma)Phosphorylation status of RTK and downstream targets

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