Novel inhibitors of the histone methyltransferase DOT1L show potent antileukemic activity in patient-derived xenografts

Blood. 2020 Oct 22;136(17):1983-1988. doi: 10.1182/blood.2020006113.

Abstract

Publisher's Note: There is a Blood Commentary on this article in this issue.

Publication types

  • Letter

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use
  • Benzimidazoles / pharmacokinetics
  • Benzimidazoles / therapeutic use*
  • Drugs, Investigational / pharmacokinetics
  • Drugs, Investigational / therapeutic use
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / therapeutic use*
  • Histone-Lysine N-Methyltransferase / antagonists & inhibitors*
  • Humans
  • Jurkat Cells
  • K562 Cells
  • Leukemia / drug therapy*
  • Leukemia / pathology
  • Mice
  • Treatment Outcome
  • Tumor Cells, Cultured
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Benzimidazoles
  • Drugs, Investigational
  • EPZ-5676
  • Enzyme Inhibitors
  • DOT1L protein, human
  • Histone-Lysine N-Methyltransferase