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c-Kit is a cytokine receptor, a Type III receptor tyrosine kinase, expressed on hematopoietic stem cells and other cell types. Its main functions include regulating cell proliferation, survival, and migration, and it plays essential roles in hematopoiesis, melanogenesis, gametogenesis, and mast cell development/function. Upon binding its ligand SCF, c-Kit dimerizes, activates its intrinsic tyrosine kinase activity, and triggers downstream signaling pathways to regulate gene expression affecting proliferation/differentiation/survival. Dysregulation or mutation of KIT can lead to various pathologies including cancers and defects in pigmentation/fertility. Tyrosine kinase inhibitors targeting mutant/overactive c-KIT have been developed for GISTs and other malignancies.
ATP-binding site inhibition within the tyrosine kinase domain
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