Nilotinib-resistant KIT mutants

Stable Identifier
Homo sapiens
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Nilotinib is a type II tyrosine kinase inhibitor currently in clinical trials for treatment of KIT-mutant cancers, and shows variable effectiveness against mutations in exon 11, 13, 17 and 18. Nilotinib is ineffective against the gatekeeper mutation T670I (Kissova et al, 2016; Guo et al, 2007; Roberts et al, 2007; Serrano et al, 2019).
Literature References
PubMed ID Title Journal Year
17699867 Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor

Hom, G, Antonescu, CR, Guo, T, Agaram, NP, Veach, D, Singer, S, Schwartz, GK, Besmer, P, Maki, RG, Clarkson, BD, D'Adamo, D, Wong, GC, DeMatteo, RP

Clin. Cancer Res. 2007
17363509 Resistance to c-KIT kinase inhibitors conferred by V654A mutation

Griffith, R, Odell, AF, Roberts, KG, Baleato, RM, Lyons, AB, Ashman, LK, Byrnes, EM

Mol. Cancer Ther. 2007
28478525 Novel Insights into the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors

Morales-Barrera, R, Carles, J, Suárez, C, García-Valverde, A, Olivares, D, Valverde, C, George, S, Serrano, C

Target Oncol 2017
30792533 Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours

Heinrich, MC, Ketzer, J, Bauer, S, Zhu, M, Presnell, A, Raut, CP, George, S, Mannan, AM, Serrano, C, Yu, C, Sicinska, E, Tao, DL, Rubin, BP, Fletcher, JA, Mariño-Enríquez, A, Demetri, GD, Eilers, G, Czaplinski, JT, McKinley, A

Br. J. Cancer 2019
27527414 The human tyrosine kinase Kit and its gatekeeper mutant T670I, show different kinetic properties: Implications for drug design

Maga, G, Crespan, E, Kissova, M

Bioorg. Med. Chem. 2016
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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