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Updated: Oct 1, 2025

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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
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Recent progress on small molecules targeting epigenetic complexes.
Yukihiro Itoh1, Yuri Takada1, Yasunobu Yamashita1
1SANKEN, Osaka University, Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan.
Current Opinion in Chemical Biology
|March 3, 2022
Summary
New drug discovery efforts focus on epigenetic complexes like Polycomb Repressive Complex 2 (PRC2) and Polycomb Repressive Complex 1 (PRC1), moving beyond single enzymes to target gene expression regulation for disease treatment.
Area of Science:
- Epigenetics
- Molecular Biology
- Drug Discovery
Background:
- Historically, epigenetic drug discovery concentrated on enzymes like histone deacetylases (HDACs).
- Emerging research highlights the significance of multiprotein complexes in epigenetic regulation.
- Dysfunctional epigenetic complexes are implicated in various pathological conditions.
Purpose of the Study:
- To review small molecules targeting key epigenetic complexes.
- To focus on recent drug discovery endeavors.
- To examine complexes including Polycomb Repressive Complex 2 (PRC2), Polycomb Repressive Complex 1 (PRC1), and the CoREST complex.
Main Methods:
- Literature review of recent drug discovery studies.
- Analysis of small molecules modulating epigenetic complex function.
- Focus on PRC2, PRC1, and CoREST complex targeting strategies.
Main Results:
- Identification of emerging small molecules targeting epigenetic complexes.
- Overview of drug discovery approaches for PRC2, PRC1, and CoREST.
- Highlighting the shift towards targeting complex machinery in epigenetics.
Conclusions:
- Small molecules targeting epigenetic complexes represent a promising area in drug discovery.
- PRC2, PRC1, and CoREST complexes are key targets for therapeutic intervention.
- Further research into these complexes could yield novel treatments for epigenetic-related diseases.
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