A combination of chemical and genetic approaches has established a proof of concept in mouse models—with strong mechanistic underpinning—indicating that targeting the aberrantly recruited histone methyltransferase activity of DOT1L has therapeutic potential in aggressive leukemias driven by MLL fusion genes.
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Acknowledgements
The authors wish to acknowledge B. Matijssen for assistance with Figure 1b.
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P.W. and J.B. are employees of and J.T. is a student of the Institute of Cancer Research. P.W. is also associated with Chroma Therapeutics and Nextech Invest Ltd.
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Travers, J., Blagg, J. & Workman, P. Targeting leukemia on the DOT. Nat Chem Biol 7, 663–665 (2011). https://doi.org/10.1038/nchembio.661
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DOI: https://doi.org/10.1038/nchembio.661
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