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Updated: Feb 28, 2026
miRNA Expression Analyses in Prostate Cancer Clinical Tissues
Published on: September 8, 2015
Bromodomain-containing proteins in prostate cancer
Alfonso Urbanucci1, Ian G Mills2
1Centre for Molecular Medicine Norway, Nordic European Molecular Biology Laboratory Partnership, University of Oslo, Forskningsparken, Oslo, Norway; Department of Molecular Oncology, Institute for Cancer Research, Oslo University Hospital, Oslo, Norway.
Abstract:
Several oncogenic factors have been involved in prostate cancer progression. However, therapeutic approaches still focus on suppression of androgen receptor (AR) signaling. In fact, whereas the full-length AR incorporates a ligand-binding domain, which has become a drug target for competitive inhibitors, other transcription factors often do not have tractable binding pockets that aid drug development. Consequently drug development efforts have turned to transcription co-regulators, often chromatin-modifying enzymes or factors that bind to epigenetic modifications to chromatin. Bromodomain (BRD)-containing proteins fall into the latter category and significant progress has been made in developing small molecule inhibitors that target a particular subgroup of BRD-containing proteins known as the Bromodomain and extra-terminal (BET) family proteins. These inhibitors have proven particularly effective in inactivating c-Myc in lymphoma but more recently members of the BET family have also been identified as AR-interacting proteins raising the prospect of using these inhibitors as an alternative strategy for targeting AR-driven cancers. In this review we will provide an overview of BRD-containing proteins and the potential for exploiting them as biomarkers and drug targets in prostate cancer.
Insights
Bromodomain (BRD)-containing proteins, including BET family proteins, are emerging as promising therapeutic targets for prostate cancer. Targeting these proteins offers a new strategy beyond androgen receptor (AR) signaling suppression.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Prostate cancer progression involves multiple oncogenic factors, with current therapies primarily targeting androgen receptor (AR) signaling.
- Traditional drug development targeting transcription factors is challenging due to the lack of tractable binding pockets.
- Focus has shifted to transcription co-regulators, such as chromatin-modifying enzymes and epigenetic factors.
Purpose of the Study:
- To review bromodomain (BRD)-containing proteins as potential biomarkers and drug targets in prostate cancer.
- To explore the therapeutic potential of targeting BET family proteins in AR-driven cancers.
- To provide an overview of BRD-containing proteins and their role in prostate cancer.
Main Methods:
- Review of existing literature on BRD-containing proteins, BET family proteins, and their interaction with AR.
- Analysis of the role of BRD-containing proteins in chromatin modification and epigenetic regulation.
- Exploration of small molecule inhibitors targeting BET family proteins.
Main Results:
- Bromodomain (BRD)-containing proteins, particularly BET family proteins, are involved in epigenetic regulation and interact with the androgen receptor (AR).
- Small molecule inhibitors targeting BET proteins show efficacy in inactivating c-Myc in lymphoma and are being investigated for prostate cancer.
- BET family proteins represent a potential alternative strategy for targeting AR-driven prostate cancers.
Conclusions:
- BRD-containing proteins, especially BET family members, hold significant potential as novel biomarkers and therapeutic targets for prostate cancer.
- Targeting BET proteins offers a promising alternative or complementary strategy to AR signaling suppression in prostate cancer treatment.
- Further research into BRD-containing proteins could lead to the development of new drugs for AR-driven cancers.
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