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c-KIT proto-oncogene receptor tyrosine kinase (KIT, CD117, or stem cell factor receptor (SCFR)) is a transmembrane protein that functions as a cell-surface receptor for stem cell factor (SCF). Upon SCF binding, c-KIT dimerizes, autophosphorylates, and activates downstream signaling pathways regulating cell survival, proliferation, differentiation, and migration. Dysregulation of c-KIT, particularly through activating mutations, is implicated in various cancers, including GISTs, melanoma, and AML. Therapeutic strategies involve small-molecule inhibitors targeting c-KIT’s kinase activity, but resistance can develop.
Small-molecule inhibitors targeting c-KIT’s kinase activity, blocking aberrant signaling from mutant forms of c-KIT
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