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- W4296093485 abstract "Targeted protein degradation (TPD) by PROteolysis TArgeting Chimeras (PROTACs) is of great interest for probe molecule and drug development. However, current bivalent PROTACs are rule-breaking molecules with sub-optimal cellular permeability, solubility, and other drug-like properties. In this study, we report a novel approach for TPD by Self-Assembled Proteolysis TArgeting Chimeras (SAPTACs) in which the target protein and E3 Ubiquitin ligase ligands assemble in cellulo via reversible, bioorthogonal reactions. SAPTACs that me-diate the degradation of the Von Hippel Landau (VHL) E3 Ubiquitin ligase are described. We show that pseu-do-homodimeric degraders for VHL can be assembled in situ through the interaction of VHL ligands linked to phenylboronic acid and catechol as well as to o-acetlyphenylboronic acid and an alkoxyamine. The efficiency of VHL degradation by these SAPTACs is linked to the strength of the reversible covalent interaction." @default.
- W4296093485 created "2022-09-17" @default.
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- W4296093485 date "2022-09-15" @default.
- W4296093485 modified "2023-09-26" @default.
- W4296093485 title "Self-Assembly of Proteolysis Targeting Chimeras Via Reversible Bioorthogonal Reactions" @default.
- W4296093485 doi "https://doi.org/10.26434/chemrxiv-2022-1g1p4" @default.
- W4296093485 hasPublicationYear "2022" @default.
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