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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Use of epigenetic drugs in disease: an overview
Sarah Heerboth1, Karolina Lapinska1, Nicole Snyder1
1Cancer Center, Department of Medicine, Boston University School of Medicine, Boston, MA, USA.
Abstract:
Epigenetic changes such as DNA methylation and histone methylation and acetylation alter gene expression at the level of transcription by upregulating, downregulating, or silencing genes completely. Dysregulation of epigenetic events can be pathological, leading to cardiovascular disease, neurological disorders, metabolic disorders, and cancer development. Therefore, identifying drugs that inhibit these epigenetic changes are of great clinical interest. In this review, we summarize the epigenetic events associated with different disorders and diseases including cardiovascular, neurological, and metabolic disorders, and cancer. Knowledge of the specific epigenetic changes associated with these types of diseases facilitates the development of specific inhibitors, which can be used as epigenetic drugs. In this review, we discuss the major classes of epigenetic drugs currently in use, such as DNA methylation inhibiting drugs, bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, protein methyltransferase inhibitors, and histone methylation inhibitors and their role in reversing epigenetic changes and treating disease.
Insights
Epigenetic drugs target DNA methylation and histone modifications to reverse pathological gene expression changes. This review covers epigenetic events in diseases and discusses key drug classes for therapeutic intervention.
Area of Science:
- Molecular Biology
- Pharmacology
- Genetics
Background:
- Epigenetic alterations like DNA methylation and histone modifications regulate gene expression.
- Dysregulation of these epigenetic events is linked to various diseases, including cancer, cardiovascular, neurological, and metabolic disorders.
- Targeting epigenetic modifications offers a promising therapeutic strategy.
Purpose of the Study:
- To review epigenetic events associated with major human diseases.
- To discuss the development and therapeutic potential of epigenetic drugs.
- To highlight key classes of epigenetic inhibitors.
Main Methods:
- Literature review of epigenetic mechanisms in disease.
- Analysis of current epigenetic drug classes and their targets.
- Discussion of therapeutic applications in cardiovascular, neurological, metabolic disorders, and cancer.
Main Results:
- Specific epigenetic changes are implicated in diverse pathologies.
- Epigenetic drugs, including DNA methylation inhibitors and histone-modifying enzyme inhibitors, show therapeutic promise.
- Bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, and protein methyltransferase inhibitors represent major classes.
Conclusions:
- Understanding disease-specific epigenetic alterations is crucial for developing targeted therapies.
- Epigenetic drugs offer a novel approach to reverse pathological gene expression and treat diseases.
- Further research into epigenetic drug development holds significant clinical potential.
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