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Updated: Apr 27, 2026

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing
Published on: May 5, 2023
Epigenetic drugs that do not target enzyme activity
Dafydd R Owen1, John D Trzupek1
1Pfizer Worldwide Research and Development, 200 Cambridgepark Drive, Cambridge, MA 02140, USA.
Epigenetic reader proteins interpret cellular marks without direct enzymatic action. These non-enzymatic proteins are promising drug discovery targets due to their role in transcriptional regulation.
Area of Science:
- Molecular Biology
- Epigenetics
- Drug Discovery
Background:
- Epigenetic marks on DNA and histones are dynamically regulated by enzymes.
- Epigenetic reader proteins interpret these marks but do not catalyze modifications.
- Their role in transcriptional activity makes them significant biological players.
Purpose of the Study:
- To review the literature on non-enzymatic epigenetic reader proteins.
- To highlight their potential as drug targets.
- To summarize recent findings from publications, patents, and company disclosures (2009-present).
Main Methods:
- Literature review
- Analysis of patent literature
- Review of company disclosures
Main Results:
- Epigenetic reader proteins are a distinct class of epigenetic regulators.
- They possess druggable binding sites suitable for small molecule inhibition.
- Their function is intrinsically linked to gene transcription.
Conclusions:
- Non-enzymatic epigenetic reader proteins represent attractive targets for therapeutic intervention.
- Targeting these proteins offers a novel strategy in drug discovery for epigenetic-related diseases.
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