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EPZ-5676

Known as: DOT1L Inhibitor EPZ-5676 
A small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Upon intravenous administration, EPZ-5676… 
National Institutes of Health

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Related topics

1 relation

Broader (1)

Benzimidazoles

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2017
2017
[Effects of DOT1L Inhibitor EPZ-5676 Combined with Chemotherapeutic Drugs on Prolifiration and Apoptosis of RS 4;11 Cells].
OBJECTIVE To investigate the synergistic antiproliferative and inducing-apoptotic effect of EPZ-5676 combined with… 
Review
2016
Review
2016
[Mechanism of A New DOT1L Inhibitor EPZ-5676 and Its Research Progress -Review].
Leukemia carring translocation at the 11q23 locus is referred to MLL-rearranged (MLL-r) leukemia, and the occurrence of this… 
2016
2016
COMBINING DOT1L INHIBITOR EPZ-5676 WITH SORAFENIB TO TREAT MLL-REARRANGED (MLL-R) PEDIATRIC ACUTE MYELOID LEUKEAMIA (AML)
Review
2016
Review
2016
Design , Synthesis and Characterization of Small Molecules Targeting MLL 1 Methyltransferase in Mixed-Lineage Leukemia
The rearrangements of the MLL located on the chromosome 11q23 are the major cause of mixed-lineage leukemia. The translocation… 
2015
2015
Abstract 2701: Characterization of acquired EPZ-5676 resistance in cell line models of MLL rearranged leukemia
DOT1L inhibitor EPZ-5676 is currently under Phase 1 clinical trial investigation in relapsed/refractory patients with acute… 
2015
2015
Abstract C12: Identification of biomarkers and pathways associated with response to the DOT1L inhibitor Pinometostat (EPZ-5676) in MLL-r leukemia
Pinometostat is a highly selective first in class DOT1L inhibitor currently in Phase 1 clinical trials in adult and pediatric… 
2015
2015
Abstract 5383: DOT1L inhibitor EPZ-5676 synergizes with cytarabine and azacitidine in preclinical models of MLL-rearranged leukemia
EPZ-5676 is a small molecule inhibitor of the histone methyltransferase DOT1L currently in clinical development and represents a… 
2014
2014
Pediatric Dose Determinations for the Phase I Study of the DOT1L Inhibitor, EPZ-5676, in MLL-r Acute Leukemia: Leveraging Early Clinical Data in Adults through Physiologically-Based Pharmacokinetic…
Introduction: Relapsed/refractory (R/R) MLL-r acute leukemia in children has a poor prognosis, with a reported 5 year overall… 
2013
2013
Myeloid Leukemia Cells With MLL partial Tandem Duplication Are Sensitive To Pharmacological Inhibition Of The H3K79 Methyltransferase DOT1L
Genetic alterations of the mixed-lineage leukemia ( MLL ) gene are commonly identified in acute leukemias. In acute myeloid… 
2012
2012
Preclinical Characterization of a Potent, Selective Inhibitor of the Protein Methyltransferase DOT1L for Use in the Treatment of MLL-Rearranged Leukemia.
Abstract 2379 The enzymatic activity of the protein methyltransferase (PMT) DOT1L has been shown to be a driver of cell… 
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