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Target intelligence / Profile preview
c-kit protein tyrosine kinase (c-KIT)
- Target
- c-KIT
- Molecular classification
- Receptor, Tyrosine Kinase, Type III receptor tyrosine kinase
01
Overview
The c-kit protein tyrosine kinase, also known as CD117 or stem cell factor receptor (SCFR), is a type III receptor tyrosine kinase encoded by the KIT proto-oncogene. It plays essential roles in normal physiology and disease, particularly in hematopoiesis, pigmentation, gametogenesis, and cancer. Dysregulation of c-KIT occurs via overexpression or activating mutations. Inhibitors targeting the ATP-binding site of mutant/overactive Kit have shown clinical efficacy.
- Other names
- CD117Stem cell factor receptor (SCFR)Tyrosine-protein kinase KITMast/stem cell growth factor receptor
02
Mechanism of action
ATP-binding site inhibition of mutant/overactive Kit
03
Biological functions
HematopoiesisMelanogenesis/pigmentationGametogenesisCell proliferationCell survivalCell migrationCell differentiationSignal transduction
04
Disease associations
CancerGastrointestinal stromal tumors (GISTs)Acute myeloid leukemia (AML)Mastocytosis/mastocytomaMelanomaNasal T-cell lymphomas
05
Safety considerations
Resistance development (secondary mutations, alternative signaling pathway activation)Toxicity
06
Interacting drugs
Imatinib mesylate (STI571)
07
Biomarkers
KIT mutations (e.g., juxtamembrane domain mutations)KIT overexpression
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