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In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)
Bioorganic & Medicinal Chemistry, 2021Chemical knockdown of therapeutic targets using proteolysis targeting chimeras (PROTACs) is a rapidly developing field in drug discovery, but PROTACs are bifunctional molecules that generally show poor bioavailability due to their relatively high molecular weight.
Shusuke Tomoshige, Minoru Ishikawa
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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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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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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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Future Medicinal Chemistry, 2022
Proteolysis-targeting chimera (PROTAC) is an emerging revolutionary technology that promotes degradation of target proteins by proteolysis. AR-targeting PROTACs marked many milestones in the history of PROTAC development. In this review, the author discusses the development of AR-targeting PROTACs over the last two decades.
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Proteolysis-targeting chimera (PROTAC) is an emerging revolutionary technology that promotes degradation of target proteins by proteolysis. AR-targeting PROTACs marked many milestones in the history of PROTAC development. In this review, the author discusses the development of AR-targeting PROTACs over the last two decades.
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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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Synthesis, Biochemical, and Cellular Evaluation of HDAC6 Targeting Proteolysis Targeting Chimeras
2022Histone deacetylases are considered promising epigenetic targets for chemical protein degradation due to their diverse roles in physiological cellular functions and in the diseased state. Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules that hijack the cell's ubiquitin-proteasome system (UPS).
Salma Darwish +8 more
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Proteolysis-Targeting Chimeras: A Kaleidoscope of Targeted Protein Degradation
Future Medicinal Chemistry, 2021Yi Mou +3 more
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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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