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

被引：57

作者：

Abedin, Sameem M. ^{[1
]}

Boddy, Craig S. ^{[1
]}

Munshi, Hidayatullah G. ^{[1
,2
,3
]}

机构：

[1] Northwestern Univ, Feinberg Sch Med, Dept Med, 303 East Super Ave, Chicago, IL 60611 USA

[2] Northwestern Univ, Jesse Brown VA Med Ctr, Med Serv, Chicago, IL 60611 USA

[3] Northwestern Univ, Robert H Lurie Comprehens Canc Ctr, Chicago, IL 60611 USA

来源：

ONCOTARGETS AND THERAPY | 2016年 / 9卷

关键词：

leukemia; lymphoma; multiple myeloma; toxicity; resistance mechanisms; B-CELL LYMPHOMA; ACUTE LYMPHOBLASTIC-LEUKEMIA; BROMODOMAIN INHIBITION; MULTIPLE-MYELOMA; C-MYC; SELECTIVE-INHIBITION; SYNERGISTIC ACTIVITY; DOSE-ESCALATION; OPEN-LABEL; OTX015;

D O I：

10.2147/OTT.S100515

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 [微生物学]; 090105 [作物生产系统与生态工程];

摘要：

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.

引用

页码：5943 / 5953

页数：11

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