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Targeted protein degradation via intramolecular bivalent glues
bioRxiv, 2023Targeted protein degradation is a pharmacological modality based on the induced proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and proteasomal degradation.
Oliver Hsia +20 more
semanticscholar +1 more source
Science, 2023
Targeted protein degradation can provide advantages over inhibition approaches in the development of therapeutic strategies. Lysosome-targeting chimeras (LYTACs) harness receptors, such as the cation-independent mannose 6–phosphate receptor (CI-M6PR), to
G. Ahn +7 more
semanticscholar +1 more source
Targeted protein degradation can provide advantages over inhibition approaches in the development of therapeutic strategies. Lysosome-targeting chimeras (LYTACs) harness receptors, such as the cation-independent mannose 6–phosphate receptor (CI-M6PR), to
G. Ahn +7 more
semanticscholar +1 more source
Bifunctional Compounds as Molecular Degraders for Integrin-Facilitated Targeted Protein Degradation.
Journal of the American Chemical Society, 2022As effective ways to regulate protein levels, targeted protein degradation technologies have attracted great attention in recent years. Here, we established a novel integrin-facilitated lysosomal degradation (IFLD) strategy to degrade extracellular and ...
Jiwei Zheng +13 more
semanticscholar +1 more source
Catching proteins for degradation
Science, 2023A ubiquitin-independent pathway targets nuclear proteins to the ...
Charlotte M, Schilling +1 more
openaire +2 more sources
Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery.
Journal of Medicinal Chemistry, 2021Targeted protein degradation is a promising area in the discovery and development of innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and have intrinsic advantages over heterobifunctional proteolysis-targeting ...
Guoqiang Dong +3 more
semanticscholar +1 more source
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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Protein folding and degradation in bacteria:¶To degrade or not to degrade? That is the question
Cellular and Molecular Life Sciences, 2002In Escherichia coli protein quality control is carried out by a protein network, comprising chaperones and proteases. Central to this network are two protein families, the AAA+ and the Hsp70 family. The major Hsp70 chaperone. DnaK, efficiently prevents protein aggregation and supports the refolding of damaged proteins. In a special case, DnaK, together
Dougan, David A. +2 more
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Bispecific Aptamer Chimeras Enable Targeted Protein Degradation on Cell Membranes.
Angewandte Chemie, 2021The ability to regulate membrane protein abundance offers great opportunities for developing therapeutic sites for various diseases. Herein, we develop a platform for targeted degradation of membrane-associated proteins using bispecific aptamer chimeras ...
Yanyan Miao +6 more
semanticscholar +1 more source
Protein degradation in signaling
Current Opinion in Plant Biology, 2000Recent studies have linked proteolysis by the ubiquitin/proteasome pathway to a variety of signaling pathways in higher plants. These links were uncovered by characterization of mutants altered in signaling or by targeted disruption of components of the proteolytic pathway. Significant advances have recently revealed connections between proteolysis and
J, Callis, R D, Vierstra
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