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Target intelligence / Profile preview
Receptor Protein-Tyrosine Kinase (RTK)
- Target
- RTK
- Molecular classification
- Receptor, Enzyme, Protein Kinase, Transmembrane Receptor
01
Overview
Receptor protein-tyrosine kinases (RTKs) are a major class of transmembrane cell surface receptors that possess intrinsic enzymatic activity, specifically the ability to phosphorylate tyrosine residues on themselves and other proteins. They serve as high-affinity receptors for many polypeptide growth factors, cytokines, and hormones. Ligand binding induces dimerization and autophosphorylation, leading to activation of downstream signaling pathways such as Ras/MAPK and PI3K/Akt, regulating cell growth, differentiation, metabolism and motility. Dysregulation is frequently implicated in cancer.
- Other names
- Receptor Tyrosine KinaseTyrosine Kinase Receptor
02
Mechanism of action
Tyrosine kinase inhibition
03
Biological functions
Signal transductionCell growthCell differentiationMetabolismCell motilityCell proliferationCell survivalAngiogenesis
04
Disease associations
CancerDevelopmental disordersMetabolic disordersOther
05
Safety considerations
Drug resistanceOff-target effectsCardiotoxicity (some VEGFR inhibitors)Skin rash (EGFR inhibitors)
06
Interacting drugs
EGFR inhibitors (e.g., gefitinib, erlotinib)
3 more in the full profile.
07
Biomarkers
EGFR mutations (e.g., in lung cancer)HER2 amplification (e.g., in breast cancer)VEGF levelsFGFR mutations/fusions
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