Receptor tyrosine-protein kinase KIT (KIT)

Receptor tyrosine-protein kinase KIT (KIT) is a type III receptor tyrosine kinase encoded by the KIT proto-oncogene. It is a transmembrane receptor expressed on the surface of hematopoietic stem cells, melanocytes, mast cells, germ cells, and interstitial cells of Cajal. KIT binds to its ligand, stem cell factor (SCF), leading to receptor dimerization, autophosphorylation, and activation of downstream signaling pathways involved in cellular survival, proliferation, and differentiation. Pathogenic mutations or overactivation are implicated in several human cancers, notably gastrointestinal stromal tumors, melanomas, and certain leukemias. Clinically, KIT is both a prognostic biomarker and a validated therapeutic target, especially in oncology, where it is inhibited by several approved tyrosine kinase inhibitors.

Other names

CD117c-KITMast/stem cell growth factor receptor (SCFR)Stem cell factor receptorPiebald traitSteel factor receptorProto-oncogene c-KITv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog

Competitive inhibition of ATP binding (tyrosine kinase inhibition); Inhibition of receptor autophosphorylation and downstream signaling; Blockade of KIT-mediated cell proliferation and survival pathways