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Target intelligence / Profile preview
KIT Proto-Oncogene Receptor Tyrosine Kinase D816 Isoforms (KIT D816V/D816Y)
- Target
- KIT D816V/D816Y
- Molecular classification
- Receptor Tyrosine Kinase
01
Overview
KIT D816 isoforms are receptor tyrosine kinase mutants, most commonly D816V and D816Y, characterized by constitutive ligand-independent kinase activity. These mutations occur within the activation loop, leading to uncontrolled downstream signaling that promotes cell proliferation and survival, and are implicated in several hematologic malignancies, notably systemic mastocytosis and AML. The presence of these mutations guides diagnosis and informs therapeutic decisions due to implications for drug resistance.
- Other names
- c-KIT D816V/D816YCD117 D816V/D816YKIT D816 mutants
02
Mechanism of action
Tyrosine kinase inhibition (some TKIs)
03
Biological functions
Cell proliferationCell survivalCell differentiationSignal transduction
04
Disease associations
Systemic MastocytosisAcute Myeloid Leukemia (AML)Germ Cell TumorsGastrointestinal Stromal Tumors (GISTs)Mucosal Melanoma
05
Safety considerations
Resistance to some tyrosine kinase inhibitors (e.g., imatinib)Need for alternative therapies targeting mutant forms
06
Interacting drugs
Imatinib Mesylate
07
Biomarkers
KIT D816VKIT D816Y
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