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Updated: Apr 23, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
New and under explored epigenetic modulators in search of new paradigms
Mohammad Abrar Alam1, Yeruva Suman Reddy, Mohamad Akbar Ali
1Department of Chemistry and Biochemistry Rowan University, Glassboro, NJ 08028, USA. alam@rowan.edu.
Abstract:
Aberrant regulation of epigenetic pathways causes many diseases including aging, cancer, diabetes, viral pathogenesis, drug addiction etc. and it has been estimated that epigenetic aberrations are at least ten to forty times more frequent in cancers than genetic mutations. Present epigenetic modulators hold great promise for a variety of diseases, and important tools for biological applications but these molecules have many dose limiting toxicities and existing paradigms lack desired efficacy. Synthesis and biological studies of epigenetic modulators have been attractive targets for medicinal and synthetic organic chemists in recent years. This review article provides deep insight into the new and under explored epigenetic modulators. These molecules have the potential to be used as unique template with novel pharmacophores.
Insights
Aberrant epigenetic regulation drives diseases like cancer and aging. This review explores novel epigenetic modulators offering potential therapeutic benefits with improved efficacy and reduced toxicity.
Area of Science:
- Epigenetics and Molecular Biology
- Medicinal Chemistry
- Drug Discovery
Background:
- Epigenetic pathway dysregulation is implicated in numerous diseases, including cancer, aging, and diabetes.
- Epigenetic aberrations are significantly more prevalent in cancers than genetic mutations.
- Current epigenetic modulators show promise but suffer from dose-limiting toxicities and suboptimal efficacy.
Purpose of the Study:
- To provide insights into novel and underexplored epigenetic modulators.
- To highlight the potential of these molecules as therapeutic agents.
- To discuss their utility as templates for new pharmacophores.
Main Methods:
- Literature review of recent advancements in epigenetic modulator synthesis and biological studies.
- Analysis of emerging epigenetic modulator classes.
- Exploration of structure-activity relationships and therapeutic potential.
Main Results:
- Identification of new classes of epigenetic modulators.
- Discussion of their unique chemical scaffolds and pharmacophore potential.
- Highlighting strategies to overcome limitations of existing therapies.
Conclusions:
- Novel epigenetic modulators represent a promising frontier in disease treatment.
- These molecules offer potential for improved therapeutic efficacy and safety profiles.
- Further research into their synthesis and biological activity is warranted for drug development.
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