Dasatinib-resistant KIT mutants

Stable Identifier
Homo sapiens
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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
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

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

Cancer Res. 2006
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
Participant Of
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
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