A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance.

@article{Gumireddy2005ANI,
  title={A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance.},
  author={Kiranmai Gumireddy and Stacey J. Baker and Stephen C. Cosenza and Premila Rozanne John and Anthony D. Kang and Kimberly A Robell and M. Venkat Ramana Reddy and E. P. Reddy},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2005},
  volume={102 6},
  pages={
          1992-7
        }
}
Imatinib, which is an inhibitor of the BCR-ABL tyrosine kinase, has been a remarkable success for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemias (CMLs). However, a significant proportion of patients chronically treated with imatinib develop resistance because of the acquisition of mutations in the kinase domain of BCR-ABL. Mutations occur at residues directly implicated in imatinib binding or, more commonly, at residues important for the ability of the… CONTINUE READING

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