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Target intelligence / Profile preview
c-KIT proto-oncogene receptor tyrosine kinase (KIT)
- Target
- KIT
- Molecular classification
- Receptor tyrosine kinase, RTK, Type III Receptor Tyrosine Kinase
01
Overview
c-KIT proto-oncogene receptor tyrosine kinase (KIT, CD117, or stem cell factor receptor (SCFR)) is a transmembrane protein that functions as a cell-surface receptor for stem cell factor (SCF). Upon SCF binding, c-KIT dimerizes, autophosphorylates, and activates downstream signaling pathways regulating cell survival, proliferation, differentiation, and migration. Dysregulation of c-KIT, particularly through activating mutations, is implicated in various cancers, including GISTs, melanoma, and AML. Therapeutic strategies involve small-molecule inhibitors targeting c-KIT’s kinase activity, but resistance can develop.
- Other names
- CD117SCFRStem Cell Factor ReceptorTyrosine-protein kinase KIT
02
Mechanism of action
Small-molecule inhibitors targeting c-KIT’s kinase activity, blocking aberrant signaling from mutant forms of c-KIT
03
Biological functions
Cell survivalProliferationDifferentiationMigrationHematopoiesisMelanogenesisGametogenesisMast cell development and functionSignal transduction
04
Disease associations
CancerGastrointestinal stromal tumors (GISTs)MelanomaAcute myeloid leukemia (AML)PiebaldismMastocytosis
05
Safety considerations
Acquired resistance mechanisms to kinase inhibitorsSecondary mutationsOff-target effects of kinase inhibitors
06
Interacting drugs
2 more in the full profile.
07
Biomarkers
Activating KIT mutations in GISTsKIT overexpression in melanomaKIT mutations in AML
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