New insights into small-molecule inhibitors of Bcr-Abl.

  title={New insights into small-molecule inhibitors of Bcr-Abl.},
  author={Silvia Schenone and O. A. Bruno and Marco Radi and Maurizio Botta},
  journal={Medicinal research reviews},
  volume={31 1},
Chronic myelogenous leukemia (CML) is a myeloproliferative disease associated with a defined genetic abnormality, the Bcr-Abl fusion gene on the Philadelphia chromosome that expresses the constitutively activated tyrosine kinase (TK) Bcr-Abl. This enzyme leads to the malignant transformation of primitive hematopoietic cells and to the consequent disease. The central role of Bcr-Abl in the pathogenesis of CML culminated in the discovery of imatinib (an ATP-competitive inhibitor), which is… CONTINUE READING
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