Potent inhibition of DOT1L as treatment of MLL-fusion leukemia
Open Access
- 8 August 2013
- journal article
- Published by American Society of Hematology in Blood
- Vol. 122 (6), 1017-1025
- https://doi.org/10.1182/blood-2013-04-497644
Abstract
Key Points. EPZ-5676 is a potent DOT1L inhibitor that causes tumor regressions in a rat xenograft model of MLL-rearranged leukemia.This publication has 44 references indexed in Scilit:
- Selective Inhibitors of Histone Methyltransferase DOT1L: Design, Synthesis, and Crystallographic StudiesJournal of the American Chemical Society, 2011
- Function of leukemogenic mixed lineage leukemia 1 (MLL) fusion proteins through distinct partner protein complexesProceedings of the National Academy of Sciences of the United States of America, 2011
- MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1LCancer Cell, 2011
- MLL-AF9 and MLL-ENL alter the dynamic association of transcriptional regulators with genes critical for leukemiaExperimental Hematology, 2011
- Kinetics of Re-establishing H3K79 Methylation Marks in Global Human Chromatin*Published by Elsevier BV ,2010
- A Higher-Order Complex Containing AF4 and ENL Family Proteins with P-TEFb Facilitates Oncogenic and Physiologic MLL-Dependent TranscriptionCancer Cell, 2010
- MLL-AF9-Induced Leukemogenesis Requires Coexpression of the Wild-Type Mll AlleleCancer Cell, 2010
- In Vivo Residue-specific Histone Methylation Dynamics*Published by Elsevier BV ,2010
- H3K79 Methylation Profiles Define Murine and Human MLL-AF4 LeukemiasCancer Cell, 2008
- Dot1a-AF9 Complex Mediates Histone H3 Lys-79 Hypermethylation and Repression of ENaCα in an Aldosterone-sensitive MannerPublished by Elsevier BV ,2006