Tyrosine-protein kinase KIT receptor (KIT)

Tyrosine-protein kinase KIT receptor (KIT, CD117) is a transmembrane receptor tyrosine kinase of the type III RTK family, encoded by the proto-oncogene KIT.[1][3][7] It acts as the cell-surface receptor for stem cell factor (SCF), and upon ligand binding, dimerizes to activate its intrinsic kinase activity, initiating signal transduction pathways that regulate cell survival, proliferation, differentiation, and migration in various cell types, notably hematopoietic stem cells, mast cells, melanocytes, germ cells, and interstitial cells of Cajal.[1][3][10] Activating mutations or overexpression of KIT are implicated in several human cancers—most prominently, gastrointestinal stromal tumors (GIST), acute myeloid leukemia (AML), mastocytosis, melanoma, and seminoma—making KIT an established therapeutic target.[1][2][6] Many small molecule tyrosine kinase inhibitors (TKIs)—such as imatinib and sunitinib—have been developed to inhibit abnormal KIT signaling, although resistance and toxicity pose therapeutic challenges.[2][4][6][8] Clinical diagnostics often include KIT (CD117) immunostaining or mutation testing to guide treatment.

Other names

CD117c-KitMast/stem cell growth factor receptor (SCFR)Proto-oncogene c-KitStem cell factor receptorPiebald trait proteinp145 c-kitTyrosine-protein kinase Kitv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog

Inhibition of receptor tyrosine kinase activity; Blockade of ATP binding sites; Antibody-mediated depletion or deactivation; Inhibition of downstream signaling pathways (RAS/MAPK, PI3K/AKT, PLCγ)