Target intelligence / Profile preview

Proto-oncogene tyrosine-protein kinase Kit receptor (c-Kit)

Target
c-Kit
Molecular classification
Receptor, Receptor tyrosine kinase, Type III receptor tyrosine kinase, Transmembrane protein
01

Overview

Proto-oncogene tyrosine-protein kinase Kit receptor (commonly abbreviated as c-Kit, also known as CD117 or stem cell factor receptor) is a type III receptor tyrosine kinase found on the cell surface of hematopoietic stem cells, mast cells, melanocytes, germ cells, and interstitial cells of Cajal. It is essential for the regulation of cell proliferation, survival, migration, and differentiation in multiple lineages. c-Kit responds primarily to its ligand, stem cell factor (SCF), triggering dimerization, autophosphorylation, and activation of intracellular signaling pathways. Dysregulation, overexpression, or mutations in c-Kit have been implicated in several malignancies, especially gastrointestinal stromal tumors, mastocytosis, and certain leukemias. c-Kit is a major therapeutic target, particularly for tyrosine kinase inhibitors used in oncology. Its expression or mutation status serves as a key biomarker for diagnosis, prognosis, and drug selection in relevant cancers[1][2][3][4][5][6].

Other names
Stem cell factor receptorCD117KIT receptorSCF receptorTyrosine-protein kinase Kit
02

Mechanism of action

Small molecule inhibition of tyrosine kinase activity (competitive ATP binding); Blockade of downstream signaling (inhibition of phosphorylation and signal cascade); Suppression of cancer cell proliferation and survival

03

Biological functions

Signal transductionCell proliferationCell survivalCell migrationHematopoiesis (blood cell formation)Melanogenesis (melanin formation)Gametogenesis (oogenesis and spermatogenesis)Mast cell development and functionRegulation of gastrointestinal tract motility
04

Disease associations

CancerAcute myelogenous leukemiaGastrointestinal stromal tumorMastocytosisMelanomaOther tumor types (e.g. testicular cancer, seminoma)Pigment disordersInfertility
05

Safety considerations

Off-target effects on normal stem cells (hematopoietic, melanocyte, reproductive)Myelosuppression (due to impact on hematopoiesis)Skin pigmentation changesInfertility/reproductive toxicityGastrointestinal side effectsDrug resistance mutations
06

Interacting drugs

7 more in the full profile.

07

Biomarkers

CD117 immunohistochemistry (used in cancer diagnostics, especially gastrointestinal stromal tumors)KIT gene mutations (predictive for response to kinase inhibitors)Circulating KIT ligand levels (investigational)

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