About KIT
The proto-oncogene KIT encodes a type 3 transmembrane receptor tyrosine kinase. The receptor is activated through dimerization and autophosphorylation upon binding by its ligand, stem cell factor (SCF) also known as mast cell growth factor (MGF) (PMID: 9438854). KIT activation results in increased intracellular signaling through several pathways including PI3K, MAPK and STAT, ultimately leading to cell proliferation and survival (PMID: 17546049, 11896121, 22089421). For patients with wildtype gastrointestinal stromal tumors (GIST; no KIT or PDGFRA mutations), NCCN recommends testing for germline succinate dehydrogenase (SDH) mutations. About 10-15% of GISTs are wildtype; thus, the absence of a mutation does not exclude the diagnosis of GIST. In patients without KIT mutations, a subset of those with advanced GISTs benefit from imatinib (0-45% of patients) (NCCN Soft Tissue Sarcoma v.2.2017). Activating KIT mutations occur in 80 - 90% of GISTs and are distributed over multiple exons with different frequencies (exons 11 (66.1%), exon 9 (13%), exon 13 (1.2%), and exon 17 (0.6%)) (PMID: 15365079, 17268243, 11719439). There are at least eight small molecule tyrosine kinase inhibitors (TKIs) targeting KIT that have been approved by the US Food and Drug Administration with the efficacy of each TKI strongly depending on the location of the activating KIT mutation (PMID: 2427414, 18955458, 19164557).