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Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes
Published on: January 12, 2024
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Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)
Daniela Tomaselli1, Nicola Mautone1, Antonello Mai1
1Department of Chemistry and Technology of Drugs, "Sapienza" University of Rome, 00185, Rome, Italy.
European Journal of Medicinal Chemistry
|September 2, 2020
Summary
PROteolysis Targeting Chimeras (PROTACs) offer a novel approach to degrade epigenetic proteins, enabling new therapeutic strategies. This review highlights recent advancements in epi-PROTACs for cancer treatment.
Area of Science:
- Biochemistry
- Molecular Biology
- Medicinal Chemistry
Background:
- PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules that induce protein degradation via the ubiquitin-proteasome system.
- Epigenetic targets (e-POIs) represent a promising area for PROTAC applications, offering a more effective modality than traditional small molecules.
- Degrading epigenetic proteins offers a new therapeutic strategy, particularly for cancer treatment.
Purpose of the Study:
- To review recent progress in the application of PROTAC technology to epigenetic targets.
- To focus on the medicinal chemistry of epi-PROTAC design, synthesis, and optimization.
- To compare epi-PROTACs with small molecule epigenetic drugs for therapeutic potential.
Main Methods:
- Review of recent scientific literature (last two years) on epi-PROTACs.
- Analysis of PROTAC applications targeting epigenetic protein classes: 'writers', 'erasers', and 'readers'.
- Evaluation of medicinal chemistry strategies for epi-PROTAC development.
Main Results:
- Significant advancements have been made in applying PROTAC technology to epigenetic targets.
- Epi-PROTACs demonstrate potential for comprehensive inhibition of epigenetic protein functions.
- Medicinal chemistry efforts are optimizing epi-PROTACs for enhanced efficacy and drug-like properties.
Conclusions:
- Epi-PROTACs represent a powerful tool for epigenetic research and drug discovery.
- Targeting epigenetic modifiers with PROTACs offers a promising therapeutic avenue, especially for cancers.
- Further development and comparison with small molecule epi-drugs are crucial for clinical translation.
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