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Localization matters in targeted protein degradation
Cell Chemical Biology, 2022Many factors influence the efficiency of targeted protein degradation induced by proteolysis targeting chimeras (PROTACs). In this issue of Cell Chemical Biology,Simpson et al. (2022) highlight the impact of subcellular localization. Their study elucidates that the protein of interest exhibits different amenability to PROTAC-mediated degradation at ...
Varun Jayeshkumar, Shah, Ivan, Đikić
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Targeted protein degradation by PROTACs
Pharmacology & Therapeutics, 2017Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases driven by the aberrant expression of a disease-causing protein. PROTAC molecules are bifunctional small molecules that simultaneously bind a target protein and an E3-ubiquitin ligase, thus causing ubiquitination and degradation of the ...
Taavi K, Neklesa +2 more
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Current Opinion in Chemical Biology, 2005
The ubiquitin-proteasome pathway plays a major role in cellular protein destruction and regulates fundamental cellular processes such as the cell cycle, cell signaling, and development. By altering the substrate recognition of ubiquitin-protein ligases, their robust proteolytic activity can be re-directed to recruit and accelerate the degradation of ...
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The ubiquitin-proteasome pathway plays a major role in cellular protein destruction and regulates fundamental cellular processes such as the cell cycle, cell signaling, and development. By altering the substrate recognition of ubiquitin-protein ligases, their robust proteolytic activity can be re-directed to recruit and accelerate the degradation of ...
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Targeted protein degradation and the enzymology of degraders
Current Opinion in Chemical Biology, 2018Targeted protein degradation is an emerging strategy for drug discovery that employs small molecules to catalyze the ubiquitination of target proteins, ultimately causing their degradation by the proteasome. Current degrader designs employ hetero-bivalent molecules to recruit E3 ubiquitin ligases such as VHL, Cereblon, and the IAPs to the target ...
Stewart L, Fisher, Andrew J, Phillips
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Bifunctional robots inducing targeted protein degradation
European Journal of Medicinal Chemistry, 2023The gaining importance of Targeted Protein Degradation (TPD) and PROTACs (PROteolysis-TArgeting Chimeras) have drawn the scientific community's attention. PROTACs are considered bifunctional robots owing to their avidity for the protein of interest (POI) and E3-ligase, which induce the ubiquitination of POI.
M Elizabeth, Sobhia +2 more
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SnapShot: Targeted protein degradation
CellTargeted protein degradation strategies leverage endogenous cellular degradation machinery to selectively eliminate a protein of interest. Emerging technologies are opening avenues in drug discovery and functional characterization of intracellular, membrane, and extracellular proteins. To view this SnapShot, open or download the PDF.
Yu, Ding, Boxun, Lu
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Optical control of targeted protein degradation
Cell Chemical Biology, 2021Molecular glues and proteolysis targeting chimeras (PROTACs) have emerged as small-molecule tools that selectively induce the degradation of a chosen protein and have shown therapeutic promise. Recently, several approaches employing light as an additional stimulus to control induced protein degradation have been reported.
Martin Reynders, Dirk Trauner
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Proteolysis-targeting Chimeras for Targeting Protein for Degradation
Future Medicinal Chemistry, 2019Proteolysis-targeting chimeras (PROTACs) are an emerging tool for therapeutic intervention by reducing or eliminating disease-causing proteins. PROTACs are bifunctional molecules that consist of a target protein ligand, a linker and an E3 ligase ligand, which mediate the polyubiquitination of the target protein, ultimately leading to the target protein
Jianguo, Qi, Gang, Zhang
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Autophagy‐Mediated Targeted Protein Degradation
ChemMedChemAbstractAutophagy is an evolutionarily conserved turnover process in eukaryotes, mediating the delivery of various cellular components to lysosomes for degradation and facilitating the recycling of the breakdown products to maintain homeostasis.
Jinning Shao +3 more
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Leveraging aptamers for targeted protein degradation
Trends in Pharmacological Sciences, 2023Targeted protein degradation (TPD) technologies, particularly proteolysis-targeting chimeras (PROTACs), have emerged as a significant advancement in drug discovery. However, several hurdles - such as the difficulty of identifying suitable ligands for traditionally undruggable proteins, poor solubility and impermeability, nonspecific biodistribution ...
Zhihao, Yang +4 more
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