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Progress on Small-Molecule Proteolysis-Targeting Chimeras
Future Medicinal Chemistry, 2019Proteolysis-targeting chimeras (PROTACs) have received much attention for their promising therapeutic intervention in recent years. These molecules, with the mechanism of simultaneous recruitment of target protein and an E3 ligase, can trigger the cellular ubiquitin-proteasome system to degrade the target proteins.
Wenhai, Huang +5 more
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Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors
Journal of the American Chemical Society, 2022Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which shows excellent advantages in targeting those so-called "undruggable" proteins. However, the potential systemic toxicity of PROTACs caused by undesired off-tissue protein degradation may limit the application of PROTACs in clinical practice.
Chunrong Yang +4 more
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Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery
Bioorganic Chemistry, 2022Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin-proteasome system (UPS) to induce different POIs degradation.
Jia-Yue, Xi +7 more
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Advances in Proteolysis Targeting Chimeras
Proceedings of Anticancer ResearchIn recent years, proteolysis-targeting chimeras (PROTACs) have gained widespread attention as an emerging therapeutic approach. PROTACs are bifunctional molecules composed of a target protein-binding ligand, an E3 ubiquitin ligase ligand, and a linker connecting these ligands.
Shili Liu, Yu Liu
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Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)
European Journal of Medicinal Chemistry, 2020PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules that trigger the poly-ubiquitination of the protein of interest (POI) inducing its degradation via the recruitment of the ubiquitin-proteasome system, thus suppressing the POI's intracellular levels and indirectly all its functions.
Tomaselli D. +3 more
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Proteolysis Targeting Chimera (PROTAC) Design
2023In this chapter, carefully selected examples have been elaborated to illustrate how proteolysis targeting chimeras (PROTACs) can be elegantly developed based upon pre-existing active site-directed inhibitors for different types of enzymatic reactions involved in various life processes and therapeutic areas.
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Proteolysis-targeting chimera (PROTAC): A promising senolytic strategy
Ageing Research ReviewsSenescent cells (SCs) accumulate with aging and contribute to the development of age-related pathologies. These cells evade apoptosis through upregulation of senescent cell anti-apoptotic pathways (SCAPs), making their selective elimination, a strategy termed senolysis, a promising therapeutic avenue.
Gang Fan +6 more
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Proteolysis-Targeting Chimeras in Breast Cancer Therapy
Future Medicinal Chemistry, 2020Jifa Zhang, Liang Ouyang
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Discovery of a proteolysis targeting chimera (PROTAC) as a potent regulator of FOXP3
Bioorganic & Medicinal Chemistry LettersRegulatory T (Treg) cells play a central role in immune homeostasis. Forkhead box P3 (Foxp3), a hallmark molecule in Treg cells, is a vital transcription factor for their development and function. Studies have shown that degradation of the Foxp3 could provide therapeutic benefits in achieving effective anti-tumor immunity.
Bowen, Yang +9 more
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Clinical application of proteolysis targeting chimeras
International Conference on Modern Medicine and Global Health (ICMMGH 2023), 2023Jinfeng Gao, Chuhan Meng, Vivian FT Yuan
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