Work

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

Year: 2016

Type: review

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.

Source: OncoTargets and Therapy

DOI: 10.2147/ott.s100515

Authors: Hidayatullah Munshi, Sameem Abedin, Craig Boddy

Institutions: Northwestern University, Jesse Brown VA Medical Center, Robert H. Lurie Comprehensive Cancer Center of Northwestern University

Language: English

Topic: Protein Degradation and Inhibitors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $2,836