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Association details:
| Biomarker: | BCR-ABL1 S417T |
|---|---|
| Cancer: | Chronic Myeloid Leukemia |
| Drug: | imatinib (c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, PDGFR inhibitor) |
| Direction: | Resistant |
Evidence:
Source:
Title:
Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis
Excerpt:
Amino acids 417, 459, and 486 are located at the C-terminal of the kinase domain distant to the imatinib binding site...It is possible that mutation at these sites causes conformational changes to the BCR-ABL protein that alters the equilibrium to the active conformation and impairs imatinib binding...Our data suggest that mutations beyond the activation loop are also implicated in imatinib resistance, and patients with these mutations may benefit from therapeutic intervention.
DOI:
https://doi.org/10.1182/blood-2002-09-2896
