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Updated: Jun 29, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Chromatin-modifying enzymes as therapeutic targets--Part 2
Brian R Keppler1, Trevor K Archer
1National Institutes of Health, National Institute of Environmental Health Sciences, North Carolina 27709, USA. archer1@niehs.nih.gov
Beyond histone acetylation and methylation, other chromatin-modifying enzymes like those involved in phosphorylation and ubiquitylation are crucial for gene regulation and represent potential therapeutic targets.
Area of Science:
- Molecular Biology
- Epigenetics
- Gene Regulation
Background:
- Precise gene regulation involves more than histone acetylation and methylation.
- Histone phosphorylation, ubiquitylation, SUMOylation, and poly-ADP-ribosylation are critical.
- ATP-dependent nucleosome remodeling complexes also play key roles.
Purpose of the Study:
- To review the roles of diverse chromatin-modifying enzymes in gene regulation.
- To highlight the therapeutic potential of these enzymes.
Main Methods:
- Literature review of recent publications.
- Analysis of online resources.
Main Results:
- Enzymes responsible for histone phosphorylation, ubiquitylation, SUMOylation, and poly-ADP-ribosylation are vital for transcriptional fidelity.
- These enzymes, along with nucleosome remodelers, are implicated in various disease states.
Conclusions:
- This review emphasizes the significance of various histone and nucleosome modifying enzymes in gene transcription.
- These enzymes offer promising therapeutic avenues for diseases linked to their dysregulation.
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