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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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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 ...
Shah, V. +1 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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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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Targeted degradation of CD147 proteins in melanoma
Bioorganic Chemistry, 2020CD147 is a transmembrane glycoprotein and a member of immunoglobulin superfamily, is strongly expressed in melanoma cells. CD147 has a pivotal role in tumor development. Therefore, it is a potential drug target for melanoma. In this article, we report the discovery of the first CD147 protein proteolysis targeting chimeras (PROTACs) derived from the ...
Zhe, Zhou +12 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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Covalent chemistry in targeted protein degradation
Advanced Drug Delivery ReviewsTargeted protein degradation (TPD) has revolutionized drug discovery by enabling the selective removal of specific proteins within and outside cells through the cell's natural degradation pathways. While various TPD modalities have demonstrated immense promise, the integration of covalent chemistry is rapidly emerging as a crucial approach to enhance ...
Jing, Tan +3 more
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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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Development of targeted protein degradation therapeutics
Nature Chemical Biology, 2019Targeted protein degradation as a therapeutic modality has seen dramatic progress and massive investment in recent years because of the convergence of two key scientific breakthroughs: optimization of first-generation peptidic proteolysis-targeted chimeras (PROTACs) into more drug-like molecules able to support in vivo proof of concept and the ...
Philip P, Chamberlain +1 more
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