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

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

A Medicinal Chemistry Perspective for Targeting Histone H3 Lysine-79 Methyltransferase DOT1L

(2013) Justin L. Anglin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L

(2013) Lisheng Deng et al.   MedChemComm

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

(2012) Aravind Basavapathruni et al.   Chemical Biology & Drug Design

Mechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug design

(2012) Li Di et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 3: Comparative assessement of prediction methods of human clearance

(2011) Barbara J. Ring et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

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

Epigenetic modifications and human disease

(2010) Anna Portela et al.   NATURE BIOTECHNOLOGY

The Operational Multiple Dosing Half-life: A Key to Defining Drug Accumulation in Patients and to Designing Extended Release Dosage Forms

(2008) Selma Sahin et al.   PHARMACEUTICAL RESEARCH