Mutation in the ATP-binding pocket of the ABL kinase domain in an STI571-resistant BCR/ABL-positive cell line.

@article{Ricci2002MutationIT,
  title={Mutation in the ATP-binding pocket of the ABL kinase domain in an STI571-resistant BCR/ABL-positive cell line.},
  author={Clara Ricci and Barbara Scappini and Vladim{\'i}r Divok{\'y} and Simona Gatto and Francesco Onida and Srdan Verstovsek and Hagop M Kantarjian and Miloslav E Beran},
  journal={Cancer research},
  year={2002},
  volume={62 21},
  pages={5995-8}
}
The major mechanism of action of STI571 is a competitive interference with the ATP-binding site of the Bcr/Abl tyrosine kinase. In the BCR/ABL-positive cell line KBM5, we studied cellular events associated with the in vitro acquisition of resistance to STI571. The emergence of the STI571-resistant phenotype was accompanied by only a marginal increase in the number of copies of the BCR/ABL gene and its level of expression. The activity of the Bcr/Abl kinase (level of autophosphorylation) in… CONTINUE READING

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