Preclinical Pharmacokinetics and Pharmacodynamics of Pinometostat (EPZ-5676), a First-in-Class, Small Molecule S-Adenosyl Methionine Competitive Inhibitor of DOT1L

DOT1L as a therapeutic target for the treatment of DNMT3A -mutant acute myeloid leukemia

(2016) Rachel E. Rau et al.   BLOOD

Mechanistic investigations into the species differences in pinometostat clearance: impact of binding to alpha-1-acid glycoprotein and permeability-limited hepatic uptake

(2016) Sherri A. Smith et al.   XENOBIOTICA

Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket

(2016) Clemens Scheufler et al.   ACS Medicinal Chemistry Letters

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach

(2016) Chao Chen et al.   ACS Medicinal Chemistry Letters

Targeting Chromatin Regulators Inhibits Leukemogenic Gene Expression in NPM1 Mutant Leukemia

(2016) M. W. M. Ku hn et al.   Cancer Discovery

Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human

(2015) Nigel J. Waters et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Exploring drug delivery for the DOT1L inhibitor pinometostat (EPZ-5676): Subcutaneous administration as an alternative to continuous IV infusion, in the pursuit of an epigenetic target

(2015) Nigel J. Waters et al.   JOURNAL OF CONTROLLED RELEASE

Abstract C12: Identification of biomarkers and pathways associated with response to the DOT1L inhibitor Pinometostat (EPZ-5676) in MLL-r leukemia

(2015) Scott Daigle et al.   MOLECULAR CANCER THERAPEUTICS

DOT1L: a new therapeutic target for aggressive breast cancer

(2015) Jeong-Yeon Lee et al.   Oncotarget

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor

(2014) Aravind Basavapathruni et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Vertical allometry: Fact or fiction?

(2014) Iftekhar Mahmood et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l

(2013) A. J. Deshpande et al.   BLOOD

Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response

(2012) H. Wong et al.   CLINICAL CANCER RESEARCH

Abrogation of MLL–AF10 and CALM–AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l

(2012) L Chen et al.   LEUKEMIA

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

The Pathogenesis of Mixed-Lineage Leukemia

(2011) Andrew G. Muntean et al.   Annual Review of Pathology-Mechanisms of Disease

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L

(2011) Kathrin M. Bernt et al.   CANCER CELL

Function of leukemogenic mixed lineage leukemia 1 (MLL) fusion proteins through distinct partner protein complexes

(2011) D. Biswas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Higher-Order Complex Containing AF4 and ENL Family Proteins with P-TEFb Facilitates Oncogenic and Physiologic MLL-Dependent Transcription

(2010) Akihiko Yokoyama et al.   CANCER CELL

Kinetics of Re-establishing H3K79 Methylation Marks in Global Human Chromatin

(2010) Steve M. M. Sweet et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Af9/Mllt3 interferes with Tbr1 expression through epigenetic modification of histone H3K79 during development of the cerebral cortex

(2010) N. Buttner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

In VivoResidue-specific Histone Methylation Dynamics

(2009) Barry M. Zee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

H3K79 Methylation Profiles Define Murine and Human MLL-AF4 Leukemias

(2008) Andrei V. Krivtsov et al.   CANCER CELL

CYP2C8- and CYP3A-Mediated C-Demethylation of (3- -phenoxy)-acetic Acid (CP-533,536), an EP2 Receptor-Selective Prostaglandin E2 Agonist: Characterization of Metabolites by High-Resolution Liquid Chromatography-Tandem Mass Spectrometry and Liquid Chromatography/Mass Spectrometry-Nuclear Magnetic Resonance

(2008) C. Prakash et al.   DRUG METABOLISM AND DISPOSITION