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Updated: Jun 11, 2026

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing
Published on: May 5, 2023
Targeting epigenetic enzymes for drug discovery
Robert A Copeland1, Edward J Olhava, Margaret Porter Scott
1Epizyme Inc., 840 Memorial Drive, Cambridge, MA 02139, United States. rcopeland@Epizyme.com
Abstract:
Epigenetic control of gene transcription is the result of enzyme-mediated covalent modifications of promoter-region DNA sites and of histone proteins around which chromosomal DNA is wound. Many of the enzymes that mediate these epigenetic reactions are dysregulated in human diseases. Small molecule inhibitors against two classes of these enzymes have been approved for use in patients: DNA methyltransferase (DNMT) inhibitors and histone deacetylase inhibitors. Other classes of epigenetic enzymes have been demonstrated to have strong disease association and are currently being targeted for small molecule inhibition. In this article we review these enzymes and chemical biology approaches aimed at discovering small molecule inhibitors against them for therapeutic use.
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