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Chronic myelogenous leukemia

BCR-ABL tyrosine kinase

In vitro and mouse studies identified a pyrazolo[3,4-d]pyrimidine that could help treat CML with the T315I resistance mutation in BCR-ABL. In mouse myeloid cells that express T315I mutant Bcr-Abl, compared with cells expressing wild-type Bcr-Abl, the molecule showed increased cytotoxicity. In mice grafted with myeloid cells that expressed T315I mutant Bcr-Abl, the inhibitor decreased tumor volume by more than 50% compared with vehicle. Next steps could include testing the inhibitor in additional animal models for CML.

SciBX 6(27); doi:10.1038/scibx.2013.679
Published online July 18, 2013

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Radi, M. et al. J. Med. Chem.; published online June 7, 2013;
Contact: Maurizio Botta, University of Siena, Siena, Italy
Contact: Silvia Schenone, University of Genoa, Genoa, Italy