BET inhibitors in the treatment of hematologic malignancies: current insights and future prospects
Open accessAbstract
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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Four top-ranking hit molecules from the screen, JQ1, I-BET151, I-BET762, and PFI-1, are inhibitors of BET family proteins.
“four top ranking hit molecules (JQ1, I-BET151, I-BET762, and PFI-1) turned out to be inhibitors of bromodomain and extra-terminal (BET) family proteins21,23”
From A BET family protein degrader provokes senolysis by targeting NHEJ and autophagy in senescent cells (2020) · cites this paper as [23]
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- Authors
- Munshi, H., Abedin, S., & Boddy, C.
- Affiliations
- Northwestern University (US)
- Corresponding author
- Munshi, Hidayatullah
- Abedin, Sameem
- Venue
- OncoTargets and Therapy
- Publisher
- Informa UK Limited
- Published
- 2016-09
- Volume
- Volume 9
- Pages
- 5943-5953
- ISSN
- 1178-6930 (ISSN-L)
- PMC
- PMC5047722
- OpenAlex
- W2527196333
- Cited by
- 71
- References
- 56
- Citations by year
- 2026: 6 · 2025: 6 · 2024: 5 · 2023: 5 · 2022: 9 · 2021: 4 · 2020: 11 · 2019: 9 · 2018: 9 · 2017: 6 · 2012: 1
- FWCI
- 0.72
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- OncoTargets and Therapy (publishedVersion, cc-by-nc)
- PubMed Central (publishedVersion, cc-by-nc)
- PubMed (publishedVersion)
- Dove Medical Press (Taylor and Francis Group) (submittedVersion, cc-by-nc)
- Funders
- National Cancer Institute (R01CA186885)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
- Keywords
- BET inhibitors, BET proteins, hematologic malignancies, c-Myc, acute leukemia, lymphoma, multiple myeloma, epigenetic regulation, drug resistance mechanisms, combination therapy, clinical trials
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