Dasatinib-resistant KIT mutants

Stable Identifier
R-HSA-9669914
Type
Pathway
Species
Homo sapiens
ReviewStatus
5/5
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Dasatinib is a type II tyrosine kinase inhibitor that is active against KIT receptors with mutations in the juxtamembrane and activation loop domains, but shows only partial activity against KIT receptors with mutations at residue V654 (Schittenhelm et al, 2006; Serrano et al, 2019).
Literature References
PubMed ID Title Journal Year
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
16397263 Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies

Shiraga, S, Schroeder, A, Bokemeyer, C, Deininger, MW, Heinrich, MC, Druker, BJ, Schittenhelm, MM, Lee, FY, Corbin, AS, Griffith, D

Cancer Res. 2006
Participants
Participates
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
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