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

Sameem M. Abedin; Craig S. Boddy; Hidayatullah G. Munshi

doi:10.2147/OTT.S100515

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

Medicine, Hematology Oncology Division

Research output: Contribution to journal › Review article › peer-review

52 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 language	English (US)
Pages (from-to)	5943-5953
Number of pages	11
Journal	OncoTargets and Therapy
Volume	9
DOIs	https://doi.org/10.2147/OTT.S100515
State	Published - Sep 28 2016

Keywords

Leukemia
Lymphoma
Multiple myeloma
Resistance mechanisms
Toxicity

ASJC Scopus subject areas

Pharmacology (medical)
Oncology

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10.2147/OTT.S100515

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title = "BET inhibitors in the treatment of hematologic malignancies: Current insights and future prospects",

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.",

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T2 - Current insights and future prospects

AU - Abedin, Sameem M.

AU - Boddy, Craig S.

AU - Munshi, Hidayatullah G.

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AB - 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.

KW - Leukemia

KW - Lymphoma

KW - Multiple myeloma

KW - Resistance mechanisms

KW - Toxicity

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

Abstract

Keywords

ASJC Scopus subject areas

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