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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

Papers overview

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Highly Cited
2018
Highly Cited
2018
Pinometostat (EPZ-5676) is a first-in-class small-molecule inhibitor of the histone methyltransferase disrupter of telomeric… 
2017
2017
DOT1L is a protein methyltransferase involved in the development and maintenance of MLL-rearranged (MLL-r) leukemia through its… 
Review
2017
Review
2017
Epigenetic modifications are heritable changes in gene expression that do not directly alter DNA sequence. These modifications… 
Highly Cited
2016
Highly Cited
2016
Introduction: MLL-rearranged (MLL-r) acute leukemia in children is characterized by young age at presentation and a poor overall… 
2015
2015
Introduction: Aberrant fusion proteins involving the MLL histone methyltransferase (HMT) result in recruitment of another HMT… 
2015
2015
AbstractPurpose The metabolism and disposition of the first-in-class DOT1L inhibitor, EPZ-5676 (pinometostat), was investigated… 
Highly Cited
2014
Highly Cited
2014
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… 
Highly Cited
2014
Highly Cited
2014
(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… 
2014
2014
Introduction: Rearrangements of the MLL (mixed lineage leukemia) gene on chromosome 11q23 are present in 5-10% of either acute… 
Highly Cited
2013
Highly Cited
2013
Rearrangements of the MLL gene define a genetically distinct subset of acute leukemias with poor prognosis. Current treatment…