Medical College of Wisconsin
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BET inhibitors in the treatment of hematologic malignancies: current insights and future prospects. Onco Targets Ther 2016;9:5943-5953

Date

10/13/2016

Pubmed ID

27729803

Pubmed Central ID

PMC5047722

DOI

10.2147/OTT.S100515

Scopus ID

2-s2.0-84989325811   43 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.

Author List

Abedin SM, Boddy CS, Munshi HG

Author

Sameem Abedin MD Assistant Professor in the Medicine department at Medical College of Wisconsin