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Target intelligence / Profile preview
Receptor Tyrosine Kinase KIT (KIT)
- Target
- KIT
- Molecular classification
- Receptor, Tyrosine Kinase, Receptor Tyrosine Kinase
01
Overview
KIT, also known as c-KIT or CD117, is a receptor tyrosine kinase that functions as a cell-surface receptor for stem cell factor (SCF). This protein plays an essential role in regulating cell survival, proliferation, differentiation, and migration across various tissues. Gain-of-function mutations in KIT are implicated in several cancers, including gastrointestinal stromal tumors (GIST) and systemic mastocytosis. KIT is a therapeutic target, and small molecule inhibitors like imatinib mesylate are used to treat cancers with activating KIT mutations.
- Other names
- c-KITCD117Tyrosine-protein kinase KIT
02
Mechanism of action
Small molecule inhibitors that bind to the ATP-binding site of KIT, inhibiting its kinase activity.
03
Biological functions
Cell survivalCell proliferationCell differentiationCell migrationSignal transductionHematopoiesisMelanogenesis
04
Disease associations
Gastrointestinal stromal tumors (GIST)Systemic mastocytosisAcute myeloid leukemia (AML)MastocytomasNasal T-cell lymphomas
05
Safety considerations
Resistance to tyrosine kinase inhibitors (TKIs)Off-target effects of TKIsPotential for acquired mutations leading to resistance
06
Interacting drugs
Imatinib mesylate
07
Biomarkers
KIT mutations (e.g., D816V)KIT expression level
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