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Recent Advances in PROTAC Technology Toward New Therapeutic Modalities
Hidetomo Yokoo1,2, Miyako Naganuma2,3, Makoto Oba1
1Medical Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 1-5 Shimogamo Hangicho, Sakyo-ku, Kyoto, 606-0823, Japan.
Chemistry & Biodiversity
|September 20, 2022
Summary
Proteolysis targeting chimeras (PROTACs) degrade disease proteins using the cell's natural machinery. This review explores PROTACs, including those using peptides and nucleic acids for improved protein degradation strategies.
Area of Science:
- Biochemistry
- Molecular Biology
- Drug Discovery
Background:
- Proteolysis targeting chimeras (PROTACs) leverage the ubiquitin-proteasome system for targeted protein degradation.
- Bifunctional PROTACs utilize ligands binding to target proteins and E3 ligases.
Purpose of the Study:
- To review the mechanisms and behaviors of small-molecule PROTACs.
- To introduce targeted proteolysis techniques employing peptide and nucleic acid ligands.
- To highlight advancements in PROTAC technology for enhanced protein degradation.
Main Methods:
- Review of existing literature on PROTAC technology.
- Analysis of small-molecule, peptide, and nucleic acid-based PROTACs.
- Discussion of PROTAC characteristics, including binding modes and ligand types.
Main Results:
- PROTACs offer a versatile platform for targeted protein degradation.
- Ligand modalities (small molecules, peptides, nucleic acids) influence PROTAC properties like selectivity and delivery.
- Variations in PROTAC design, such as covalent binding and allosteric targeting, offer distinct advantages.
Conclusions:
- PROTAC technology is a powerful tool for degrading disease-related proteins.
- Exploring diverse targeting ligands can optimize PROTAC efficacy and overcome drug resistance.
- Peptide and nucleic acid-based PROTACs represent promising frontiers in targeted protein degradation.
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