From Inhibition to Degradation: Proteolysis-Targeting Chimeras for Epigenetic Enzymes in Modern Drug Discovery
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ID: 318506
2026
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Abstract
Abstract Epigenetic enzymes are important therapeutic targets in several diseases, including cancer. This review summarizes recent studies on proteolysis-targeting chimeras (PROTACs) for epigenetic enzymes, with a focus on HDAC8, G9a/GLP, and KDM5. These case studies highlight the transition from conventional inhibition to targeted degradation and demonstrate the potential of degraders to modulate both catalytic and non-catalytic functions. We also discuss current challenges and future perspectives in the development of selective epigenetic degraders.
| Reference Key |
openalex_W7165770859
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|---|---|
| Authors | Shengwang Yu, Yukihiro Itoh, Takayoshi Suzuki |
| Journal | phytochemistry letters |
| Year | 2026 |
| DOI |
10.1093/chemle/upag134
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| URL | |
| Keywords | Keywords not found |
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