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- W4249555005 abstract "Proteolysis-targeting chimeras (PROTAC) are mainly focused on small molecules, whereas peptide-based PROTACs are less researched, and it might due to poor physiochemical properties of the unmodified peptides, such as poor cell permeability and low intracellular stability. Compared with small-molecule inhibitors, PROTAC methods generally have better therapeutic effects because they can enhance the regulation of related basic signaling pathways and reduce drug resistance. The design of a peptide PROTAC includes the design of peptide-targeting fragments, linker, E3 ubiquitin ligase-recruiting ligand and cell-penetrating peptide fragments, and the most important of which are peptide-targeting fragments and the ligand of E3 ligase. The linker length and composition play a central role in determining the degradation efficacy of the PROTAC targeting bromodomain-containing protein 4. The chapter summarizes the successful therapeutic applications of stabilized peptide PROTAC by highlighting their unique stapling strategies and advantages. Wnt/ β-catenin is an important signal pathway for cell proliferation, differentiation and survival, and other physiological processes." @default.
- W4249555005 created "2022-05-12" @default.
- W4249555005 date "2021-06-25" @default.
- W4249555005 modified "2023-10-17" @default.
- W4249555005 title "Stabilized Peptide <scp>PROTAC</scp>" @default.
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- W4249555005 doi "https://doi.org/10.1002/9783527343430.ch6" @default.
- W4249555005 hasPublicationYear "2021" @default.
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