Nilotinib-resistant KIT mutants

Stable Identifier
R-HSA-9669926
Type
Pathway
Species
Homo sapiens
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Nilotinib-resistant KIT mutants
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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
17363509 Resistance to c-KIT kinase inhibitors conferred by V654A mutation

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

Mol. Cancer Ther. 2007
17699867 Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor

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

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

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

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

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

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

Kissova, M, Maga, G, Crespan, E

Bioorg. Med. Chem. 2016
Participants
Events
Participant Of
hasEvent
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Rothfels, K  (2020-04-01)
Reviewed
Serrano, C  (2020-03-13)
García-Valverde, A  (2020-03-13)
Pilco-Janeta, D  (2020-03-13)
Created
Rothfels, K  (2019-12-03)
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