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Amine-bearing hydrocarbon cross-links: Tailoring helix stability, hydrophilicity, and synthetic adaptability in peptides

Authors
Tran, Duc V.H.Pham, Thanh K.Kim, Young-Woo
Issue Date
Oct-2024
Publisher
Elsevier Ltd.
Keywords
Amine cross-link; Peptide drugs; Peptide stapling; Ring-closing metathesis; α-Helix
Citation
Bioorganic & Medicinal Chemistry, v.112, pp 1 - 8
Pages
8
Indexed
SCIE
SCOPUS
Journal Title
Bioorganic & Medicinal Chemistry
Volume
112
Start Page
1
End Page
8
URI
https://scholarworks.dongguk.edu/handle/sw.dongguk/23006
DOI
10.1016/j.bmc.2024.117893
ISSN
0968-0896
1464-3391
Abstract
This study comprehensively explored the helix-stabilizing effects of amine-bearing hydrocarbon cross-links (ABXs), revealing their context-dependent nature influenced by various structural parameters. Notably, we identified a 9-atom ABX as a robust helix stabilizer, showcasing versatile synthetic adaptability while preserving peptide water solubility. Future investigations are imperative to fully exploit this system's potential and enrich our chemical toolkit for designing innovative peptide-based biomolecules. © 2024 Elsevier Ltd
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