BET inhibitors in the treatment of hematologic malignancies: Current insights and future prospects

Sameem M. Abedin*, Craig S. Boddy, Hidayatullah G. Munshi

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

29 Scopus citations

Abstract

The bromodomain and extra-terminal (BET) family of proteins are important epigenetic regulators involved in promoting gene expression of critical oncogenes. BET inhibitors have been demonstrated to repress c-Myc expression, and were initially shown to have efficacy in a number of c-Myc-dependent hematologic malignancies. Recent studies have now revealed a broader role for BET inhibitors in hematologic malignancies. In this review, we summarize the efficacy of BET inhibitors in preclinical models of acute leukemia, lymphoma, and multiple myeloma. We also summarize recent results of clinical trials utilizing BET inhibitors in hematologic malignancies, characterize potential resistance mechanisms to BET inhibitors, and discuss potential combination therapies with BET inhibitors in patients with hematologic malignancies.

Original languageEnglish (US)
Pages (from-to)5943-5953
Number of pages11
JournalOncoTargets and Therapy
Volume9
DOIs
StatePublished - Sep 28 2016

Keywords

  • Leukemia
  • Lymphoma
  • Multiple myeloma
  • Resistance mechanisms
  • Toxicity

ASJC Scopus subject areas

  • Oncology
  • Pharmacology (medical)

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