Dasatinib-resistant KIT mutants do not bind dasatinib

Stable Identifier
R-HSA-9669855
Type
Reaction [transition]
Species
Homo sapiens
Compartment
ReviewStatus
5/5
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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
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
Normal reaction
Functional status

Loss of function of dasatinib resistant KIT mutants [plasma membrane]

Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created
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