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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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Degrading the signal amplifier: ITK as a target for targeted protein degradation
Cell Chemical Biology, 2023In this issue of Cell Chemical Biology, Jiang and colleagues show for the first time that the Tec kinase ITK can be targeted using PROTAC approaches. This new modality has implications for the treatment of T cell lymphomas, but also potentially for the treatment of T cell-mediated inflammatory diseases, that depend on ITK signaling.
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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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Clinical Translation of Targeted Protein Degraders
Clinical Pharmacology & Therapeutics, 2023Targeted protein degradation (TPD) has emerged as a potentially transformational therapeutic modality with considerable promise. Molecular glue degraders remodel the surface of E3 ligases inducing interactions with neosubstrates resulting in their polyubiquitination and proteasomal degradation.
Nikki R. Kong, Lyn H. Jones
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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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Targeted Degradation of Proteins by PROTACs
Current Protocols in Chemical Biology, 2010AbstractIn recent years, small interference RNAs (siRNAs) have greatly enhanced our understanding of protein functions by allowing knockdown of targeted proteins at the mRNA level. Similarly, in an effort to achieve degradation of targeted proteins at the post‐translational level, chimeric small molecules called “PROTACs” (PROteolysis TArgeting ...
Eun Ryoung, Jang +2 more
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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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Targeted protein degradation mechanisms
Drug Discovery Today: Technologies, 2019Targeted protein degradation mediated by small molecule degraders represents an exciting new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit E3 ubiquitin ligases to the protein of interest and mediate its ubiquitination and subsequent proteolysis by the proteasome.
Yi, Zhang +3 more
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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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Aptamer-Based Targeted Protein Degradation
ACS Nano, 2023The selective removal of misfolded, aggregated, or aberrantly overexpressed protein plays an essential role in maintaining protein-dominated biological processes. In parallel, the precise knockout of abnormal proteins is inseparable from the accurate identification of proteins within complex environments.
Yuan Liu +7 more
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