Overriding imatinib resistance with a novel ABL kinase inhibitor.

@article{Shah2004OverridingIR,
  title={Overriding imatinib resistance with a novel ABL kinase inhibitor.},
  author={Neil Pravin Shah and Chris Tran and Francis Y. F. Lee and Ping Chen and Derek J Norris and Charles L Sawyers},
  journal={Science},
  year={2004},
  volume={305 5682},
  pages={399-401}
}
Resistance to the ABL kinase inhibitor imatinib (STI571 or Gleevec) in chronic myeloid leukemia (CML) occurs through selection for tumor cells harboring BCR-ABL kinase domain point mutations that interfere with drug binding. Crystallographic studies predict that most imatinib-resistant mutants should remain sensitive to inhibitors that bind ABL with less stringent conformational requirements. BMS-354825 is an orally bioavailable ABL kinase inhibitor with two-log increased potency relative to… CONTINUE READING
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