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BET bromodomains as novel epigenetic targets for brain health and disease
Mandakini B Singh1, Gregory C Sartor1
1Department of Pharmaceutical Sciences, University of Connecticut, Storrs, CT, 06269, USA.
Abstract:
Epigenetic pharmacotherapy for CNS-related diseases is a burgeoning area of research. In particular, members of the bromodomain and extra-terminal domain (BET) family of proteins have emerged as intriguing therapeutic targets due to their putative involvement in an array of brain diseases. With their ability to bind to acetylated histones and act as a scaffold for chromatin modifying complexes, BET proteins were originally thought of as passive epigenetic 'reader' proteins. However, new research depicts a more complex reality where BET proteins act as key nodes in lineage-specific and signal-dependent transcriptional mechanisms to influence disease-relevant functions. Amid a recent wave of drug development efforts from basic scientists and pharmaceutical companies, BET inhibitors are currently being studied in several CNS-related disease models, but safety and tolerability remain a concern. Here we review the progress in understanding the neurobiological mechanisms of BET proteins and the therapeutic potential of targeting BET proteins for brain health and disease.
Insights
Epigenetic drugs targeting bromodomain and extra-terminal domain (BET) proteins show promise for central nervous system (CNS) diseases. Research reveals BET proteins
Area of Science:
- Neuroscience
- Epigenetics
- Pharmacology
Background:
- Epigenetic pharmacotherapy is a rapidly advancing field for central nervous system (CNS) disorders.
- Bromodomain and extra-terminal domain (BET) proteins are implicated in various brain diseases.
- Initially viewed as passive epigenetic readers, BET proteins are now understood as crucial regulators of gene transcription.
Purpose of the Study:
- To review the neurobiological mechanisms of BET proteins in the context of CNS diseases.
- To explore the therapeutic potential of targeting BET proteins for brain health and disease.
- To discuss the progress and challenges in developing BET inhibitors for CNS applications.
Main Methods:
- Literature review of current research on BET proteins and their role in CNS diseases.
- Analysis of preclinical studies involving BET inhibitors in CNS disease models.
- Examination of safety and tolerability data from ongoing clinical investigations.
Main Results:
- BET proteins play complex roles in lineage-specific and signal-dependent transcriptional regulation relevant to brain function.
- BET inhibitors are under investigation in multiple CNS disease models, demonstrating potential therapeutic effects.
- Safety and tolerability of BET inhibitors in CNS applications remain a key area of concern and ongoing research.
Conclusions:
- BET proteins represent promising therapeutic targets for a range of CNS-related diseases.
- Further research is needed to optimize the safety and efficacy of BET inhibitors for neurological disorders.
- Understanding the intricate neurobiology of BET proteins is crucial for advancing epigenetic therapies for brain health.
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