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Updated: Aug 9, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Epigenetic therapy--a new development in pharmacology
1Department of Pharmacology & Clinical Pharmacology, Christian Medical College, Vellore, India. jpeedi@cmcvellore.ac.in
Epigenetic therapy offers a novel approach to disease treatment by targeting abnormal DNA methylation and histone modifications. Drugs inhibiting DNA methyltransferases (DNMTs) and histone deacetylases (HDACs) show promise, particularly in cancer therapy.
Area of Science:
- Pharmacology
- Molecular Biology
- Genetics
Background:
- Epigenetics involves heritable gene expression changes without altering DNA sequence.
- Abnormal DNA methylation and histone modifications are implicated in various diseases.
- Epigenetic alterations contribute to disease pathogenesis, including cancer.
Purpose of the Study:
- To review the emerging field of epigenetic therapy.
- To describe current drug development targeting epigenetic modifications.
- To highlight the therapeutic potential of epigenetic drugs in disease treatment.
Main Methods:
- Review of current pharmacological developments in epigenetic therapy.
- Description of two main drug classes: DNA methyltransferase (DNMT) inhibitors and histone deacetylase (HDAC) inhibitors.
- Summary of findings from drug trials, particularly in oncology.
Main Results:
- DNMT inhibitors reduce DNA methylation, potentially reversing tumor suppressor gene silencing in cancer.
- HDAC inhibitors increase histone acetylation, associated with anticancer effects.
- Both drug classes have demonstrated promising results in clinical trials for cancer treatment.
Conclusions:
- Epigenetic therapy represents a significant advancement in treating diseases linked to epigenetic dysregulation.
- The scope of epigenetic therapy is expected to broaden beyond cancer to other diseases.
- Targeting epigenetic mechanisms offers a promising therapeutic strategy for a wide range of conditions.
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