Target intelligence / Profile preview

KIT Proto-Oncogene, Receptor Tyrosine Kinase (c-KIT)

Target
c-KIT
Molecular classification
Receptor Tyrosine Kinase, Type III Receptor Tyrosine Kinase
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Overview

c-KIT, also known as CD117 or stem cell factor receptor (SCFR), is a type III receptor tyrosine kinase that plays a crucial role in regulating cell proliferation, survival, migration, and differentiation. Dysregulation through overexpression or mutations can lead to oncogenic transformation, promoting tumorigenesis in several cancers. Targeting mutant or overactive c-KIT with small molecule inhibitors has become an important therapeutic strategy.

Other names
CD117SCFRMast/stem cell growth factor receptor
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Mechanism of action

Small molecule inhibitors targeting the tyrosine kinase activity of c-KIT

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Biological functions

Cell proliferationCell survivalCell differentiationCell migrationHematopoiesisMelanogenesisGametogenesisGastrointestinal motilitySignal transduction
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Disease associations

Gastrointestinal Stromal Tumors (GISTs)Acute Myeloid Leukemia (AML)MastocytosisMelanomaBreast CancerThyroid CancerColorectal CancerCancer
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Safety considerations

Drug resistanceOff-target effectsToxicity
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Interacting drugs

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Biomarkers

c-KIT expressionKIT mutations

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