dc.contributor.authorLau, Yu Heng
dc.contributor.authorde Andrade, Peterson
dc.contributor.authorQuah, Soo-Tng
dc.contributor.authorRossmann, Maxim
dc.contributor.authorLaraia, Luca
dc.contributor.authorSköld, Niklas
dc.contributor.authorSum, Tze Jing
dc.contributor.authorRowling, Pamela J. E.
dc.contributor.authorJoseph, Thomas L.
dc.contributor.authorVerma, Chandra
dc.contributor.authorHyvönen, Marko
dc.contributor.authorItzhaki, Laura S.
dc.contributor.authorVenkitaraman, Ashok R.
dc.contributor.authorBrown, Christopher J.
dc.contributor.authorLane, David P.
dc.contributor.authorSpring, David R.
dc.identifier.citationLau, Y. H., de Andrade, P., Quah, S.-T., Rossmann, M., Laraia, L., Sköld, N., et al. (2014). Functionalised staple linkages for modulating the cellular activity of stapled peptides. Chemical Science, 5(5), 1804-1809.en_US
dc.description.abstractStapled peptides are a promising class of alpha-helix mimetic inhibitors for protein–protein interactions. We report the divergent synthesis of “functionalised” stapled peptides via an efficient two-component strategy. Starting from a single unprotected diazido peptide, dialkynyl staple linkers bearing different unprotected functional motifs are introduced to create different alpha-helical peptides in one step, functionalised on the staple linkage itself. Applying this concept to the p53/MDM2 interaction, we improve the cell permeability and p53 activating capability of an otherwise impermeable p53 stapled peptide by introducing cationic groups on the staple linkage, rather than modifying the peptide sequence.en_US
dc.description.sponsorshipASTAR (Agency for Sci., Tech. and Research, S’pore)en_US
dc.relation.ispartofseriesChemical Scienceen_US
dc.subjectCell permeability
dc.subjectDRNTU::Science::Biological sciences
dc.titleFunctionalised staple linkages for modulating the cellular activity of stapled peptidesen_US
dc.typeJournal Article
dc.contributor.schoolSchool of Biological Sciencesen_US
dc.description.versionAccepted version

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