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Inhibitors of Bcr-abl... breaking new ground again

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The report of a new class of potent and highly selective inhibitors of Bcr-abl highlights the potential for a truly leukemia-specific drug with no expected off-target activity. GNF-2, as a representative compound of this class, may have inspired the identification of a region of Bcr-abl that is amenable to drug design, just as imatinib did almost a decade ago.

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Figure 1: Ribbon diagram of the kinase domain of the fusion protein Bcr-abl.

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Acknowledgements

The authors would like to thank Dick Leopold for his thoughtful review of the manuscript and Chris Faehnjle for his assistance in the preparation of the figure.

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Ohren, J., Sebolt-Leopold, J. Inhibitors of Bcr-abl... breaking new ground again. Nat Chem Biol 2, 63–64 (2006). https://doi.org/10.1038/nchembio0206-63

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