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Epigenetics

Disrupting histone lysine methylation

A small molecule targeting the protein-protein interaction between a chromatin binding protein and an oncogenic transcription factor shows therapeutic potential in a subtype of acute myeloid leukemia.

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Figure 1: The small molecule OICR-9429 disrupts the interaction between the chromatin-binding protein WDR5 and a histone methyltransferase complex that is required for the oncogenic p30 isoform of the transcription factor C/EBPα to suppress differentiation and promote proliferation of leukemic cells.

Katie Vicari/Nature Publishing Group

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Correspondence to Patrick Trojer.

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Trojer, P. Disrupting histone lysine methylation. Nat Chem Biol 11, 552–554 (2015). https://doi.org/10.1038/nchembio.1861

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