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Updated: Mar 20, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Targeting Cancer with Epi-Drugs: A Precision Medicine Perspective
Lisa Gherardini, Ankush Sharma, Enrico Capobianco1
1Center for Computational Science (CCS), University of Miami, Miami, FL, USA. ecapobianco@med.miami.edu.
Abstract:
Recent pan-cancer studies have shown the importance of coupling DNA methylation patterns with transcriptome profiles to reveal tumor subgroups with clinically relevant distinct characteristics. While the coupling patterns remain in most cases matter for further study and/or interpretation, it is emerging that all associations between epigenetic changes and specific cancer histotypes can facilitate the development of novel epidrugs. In particular, together with chemotherapy and chemoprevention of cancer, these epidrugs will target specific enzymes involved in the complex regulation of gene expression. This perspective surveys recent cancer epigenetic findings on target drugs and therapeutic strategies, and focuses on the epigenetic modifications that can reverse a stable differentiated state of adult cell towards neoplastic phenotypes. The relevance of such developments may thus pave the way for patient's customized personalized therapies.
Insights
Coupling DNA methylation and transcriptome data reveals tumor subgroups. These epigenetic changes are key to developing novel epidrugs for personalized cancer therapies.
Area of Science:
- Oncology
- Epigenetics
- Genomics
Background:
- Pan-cancer studies highlight the significance of integrating DNA methylation and transcriptome profiles.
- Tumor subgroups with distinct clinical characteristics can be identified through coupled epigenetic and gene expression analyses.
- Associations between epigenetic alterations and cancer histotypes are crucial for developing novel therapeutic strategies.
Purpose of the Study:
- To survey recent findings in cancer epigenetics concerning targeted drugs and therapeutic strategies.
- To focus on epigenetic modifications that can revert adult cells from a differentiated to a neoplastic state.
- To explore the potential for patient-specific personalized therapies based on epigenetic insights.
Main Methods:
- Review of recent pan-cancer studies and epigenetic research.
- Analysis of associations between DNA methylation patterns and transcriptome profiles.
- Focus on epigenetic modifications driving cancer development and their therapeutic targeting.
Main Results:
- Emerging evidence suggests that epigenetic changes are linked to specific cancer types.
- Novel epidrugs targeting enzymes regulating gene expression are being developed.
- Epigenetic modifications can reverse cellular differentiation, contributing to neoplastic phenotypes.
Conclusions:
- Integrating epigenetic and transcriptomic data is vital for identifying clinically relevant tumor subgroups.
- Targeting epigenetic alterations holds promise for developing novel epidrugs and personalized cancer treatments.
- Understanding epigenetic reprogramming in cancer may lead to customized therapeutic strategies for patients.
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