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Updated: Jun 12, 2025
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Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes
Published on: January 12, 2024
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PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications
Narayanaperumal Pravin1, Krzysztof Jóźwiak1
1Department of Biopharmacy, Medical University of Lublin, Ul.W.Chodzki 4a, 20-093 Lublin, Poland.
European Journal of Medicinal Chemistry
|September 21, 2024
Summary
Proteolysis-Targeting Chimeras (PROTACs) offer a new way to treat diseases by degrading harmful proteins. This review covers PROTAC synthesis, applications in cancer and other diseases, and their clinical trial progress.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Drug Discovery
Background:
- Proteolysis-Targeting Chimeras (PROTACs) represent a groundbreaking therapeutic strategy.
- They leverage the cell's ubiquitin-proteasome system for targeted protein degradation.
- This approach offers a novel method for treating diverse diseases by eliminating disease-associated proteins.
Purpose of the Study:
- To provide a comprehensive overview of PROTACs.
- To detail synthetic methodologies for PROTAC construction.
- To review recent advancements and clinical applications of PROTACs.
Main Methods:
- Delineation of synthetic strategies for PROTAC building blocks.
- Analysis of ligand and protein-binding components.
- Review of linker-attached structural elements and final PROTAC molecules.
Main Results:
- Exploration of PROTAC applications in oncogenic, neurodegenerative, antiviral, and autoimmune diseases.
- Discussion of advancements in PROTAC-mediated degradation of specific disease proteins.
- Overview of the current PROTAC clinical trial landscape.
Conclusions:
- PROTACs demonstrate significant versatility in modulating key disease-related proteins.
- The review highlights the translational potential of PROTACs as an emerging therapeutic modality.
- PROTACs offer a promising avenue for developing novel treatments across various severe diseases.
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