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Association details:
| Biomarker: | BCR-ABL1 E255K |
|---|---|
| Cancer: | Chronic Myeloid Leukemia |
| Drug: | dasatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, Src kinase inhibitor, EphA2 receptor antagonist, PDGFR β antagonist) + imatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, PDGFR inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance
Excerpt:
To examine the potential role of conformational binding properties in drug resistance, we mapped the mutations in BCR-ABL capable of conferring resistance to BMS-354825....Of note, these three mutants were the most frequently recovered in our screen. L248R, E255K, F317L, and the previously uncharacterized mutant V299L show modest changes in IC50, increasing ≈10- to 15-fold from WT BCR-ABL....IC50 for growth of Ba/F3 stable lines grown in the presence of BMS-354825 and imatinib.
DOI:
10.1073/pnas.0409770102
