DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells.

@article{Klaus2014DOT1LIE,
  title={DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells.},
  author={Christine R. Klaus and Dorothy Iwanowicz and Danielle Johnston and Carly A Campbell and Jesse J. Smith and Mikel P. Moyer and Robert A Copeland and Edward J. Olhava and Margaret Porter Scott and Roy M. Pollock and Scott R. Daigle and Alejandra Raimondi},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2014},
  volume={350 3},
  pages={646-56}
}
EPZ-5676 [(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol], a small-molecule inhibitor of the protein methyltransferase DOT1L, is currently under clinical investigation for acute leukemias bearing MLL-rearrangements (MLL-r). In this study, we evaluated EPZ-5676 in combination with standard of care (SOC) agents for acute leukemias as well as other chromatin-modifying drugs in… CONTINUE READING

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