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Updated: Nov 5, 2025
Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Therapeutic targeting of chromatin: status and opportunities
Marton Siklos1, Stefan Kubicek1
1CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna, Austria.
Abstract:
The molecular characterization of mechanisms underlying transcriptional control and epigenetic inheritance since the 1990s has paved the way for the development of targeted therapies that modulate these pathways. In the past two decades, cancer genome sequencing approaches have uncovered a plethora of mutations in chromatin modifying enzymes across tumor types, and systematic genetic screens have identified many of these proteins as specific vulnerabilities in certain cancers. Now is the time when many of these basic and translational efforts start to bear fruit and more and more chromatin-targeting drugs are entering the clinic. At the same time, novel pharmacological approaches harbor the potential to modulate chromatin in unprecedented fashion, thus generating entirely novel opportunities. Here, we review the current status of chromatin targets in oncology and describe a vision for the epigenome-modulating drugs of the future.
Insights
Targeted therapies are emerging for cancer, leveraging decades of research into transcriptional control and epigenetic inheritance. New drugs modulating chromatin are entering clinical trials, offering novel treatment opportunities.
Area of Science:
- Molecular biology
- Genomics
- Oncology
Background:
- Advances in understanding transcriptional control and epigenetic inheritance since the 1990s.
- Cancer genome sequencing has revealed mutations in chromatin modifying enzymes.
- Genetic screens identified chromatin proteins as cancer vulnerabilities.
Purpose of the Study:
- To review the current status of chromatin targets in oncology.
- To describe future directions for epigenome-modulating drugs.
Main Methods:
- Review of molecular characterization studies.
- Analysis of cancer genome sequencing data.
- Evaluation of genetic screening results.
Main Results:
- Development of targeted therapies modulating transcriptional control and epigenetic pathways.
- Identification of numerous mutations in chromatin modifying enzymes across cancer types.
- Emergence of chromatin-targeting drugs in clinical settings.
Conclusions:
- Basic and translational research on chromatin is yielding clinical benefits.
- Novel pharmacological approaches offer new ways to modulate chromatin.
- Significant potential exists for future epigenome-modulating drugs in cancer treatment.
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