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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

Related topics

Related topics

1 relation

Broader (1)

Benzimidazoles

Papers overview

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Highly Cited
2019
Highly Cited
2019
DOT1L inhibition reveals a distinct subset of enhancers dependent on H3K79 methylation
Enhancer elements are a key regulatory feature of many important genes. Several general features including the presence of… 
2018
2018
Investigation of the Relationship Between Susceptibility Loci for Hip Osteoarthritis and Dual X‐Ray Absorptiometry–Derived Hip Shape in a Population‐Based Cohort of Perimenopausal Women
To examine relationships between known osteoarthritis (OA) susceptibility loci and hip shape in a population‐based cohort of… 
Review
2018
Review
2018
Therapeutic targeting potential of chromatin-associated proteins in MLL-rearranged acute leukemia
Acute leukemias (AL) with a Mixed Lineage Leukemia (MLL) gene rearrangement (MLLr) represent a group of leukemic entities… 
Review
2017
Review
2017
Epigenetics of oropharyngeal squamous cell carcinoma: opportunities for novel chemotherapeutic targets
Epigenetic modifications are heritable changes in gene expression that do not directly alter DNA sequence. These modifications… 
Highly Cited
2016
Highly Cited
2016
Final Report of Phase 1 Study of the DOT1L Inhibitor, Pinometostat (EPZ-5676), in Children with Relapsed or Refractory MLL-r Acute Leukemia
Introduction: MLL-rearranged (MLL-r) acute leukemia in children is characterized by young age at presentation and a poor overall… 
2015
2015
Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human
AbstractPurpose The metabolism and disposition of the first-in-class DOT1L inhibitor, EPZ-5676 (pinometostat), was investigated… 
Review
2015
Review
2015
Mixed lineage rearranged leukaemia: pathogenesis and targeting DOT1L
Purpose of reviewThe purpose of this study is to explore the recent advances in understanding the pathogenesis of leukaemias with… 
Review
2015
Review
2015
Epigenetics of the failing heart
With the impressive advancement in high-throughput ‘omics’ technologies over the past two decades, epigenetic mechanisms have… 
Highly Cited
2014
Highly Cited
2014
DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs and Hypomethylating Agents in MLL-Rearranged Leukemia Cells
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
Nonclinical pharmacokinetics and metabolism of EPZ‐5676, a novel DOT1L histone methyltransferase inhibitor
(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… 
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