Dasatinib-resistant KIT mutants do not bind dasatinib

Stable Identifier
Reaction [transition]
Homo sapiens
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KIT receptors bearing mutations in the ATP-binding pocket are resistant to treatment with dasatinib (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
Normal reaction
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
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