Target intelligence / Profile preview

KIT (Stem Cell Growth Factor Receptor) (KIT)

Target
KIT
Molecular classification
Receptor Tyrosine Kinase, Receptor
01

Overview

KIT, also known as the stem cell growth factor receptor or CD117, is a receptor tyrosine kinase that plays a crucial role in cell proliferation, survival, migration, and differentiation. It is essential for the development and function of hematopoietic stem cells, germ cells, mast cells, interstitial cells of Cajal, and melanocytes. Gain-of-function mutations in KIT are associated with several human cancers, including gastrointestinal stromal tumors, acute myelogenous leukemia, and mastocytomas. KIT serves as an important drug target, especially in oncology, for small molecule inhibitors like imatinib, which are effective against certain activating mutations.

Other names
Stem Cell Growth Factor ReceptorCD117c-KIT
02

Mechanism of action

Small molecule inhibitor that binds inactive conformation at ATP-binding site of mutant Kit proteins.

03

Biological functions

Cell proliferationSurvivalMigrationDifferentiationHematopoiesisGametogenesisMelanogenesisSignal transduction
04

Disease associations

CancerGastrointestinal stromal tumors (GISTs)Acute myelogenous leukemiaMastocytomas
05

Safety considerations

Resistance to imatinib due to secondary mutationsOff-target effects of kinase inhibitors
06

Interacting drugs

1 more in the full profile.

07

Biomarkers

KIT mutations (e.g., V559D, T670I, L576P, D816V, A829P)

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