Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/81934
Title: Functionalised staple linkages for modulating the cellular activity of stapled peptides
Authors: Lau, Yu Heng
de Andrade, Peterson
Quah, Soo-Tng
Rossmann, Maxim
Laraia, Luca
Sköld, Niklas
Sum, Tze Jing
Rowling, Pamela J. E.
Joseph, Thomas L.
Verma, Chandra
Hyvönen, Marko
Itzhaki, Laura S.
Venkitaraman, Ashok R.
Brown, Christopher J.
Lane, David P.
Spring, David R.
Keywords: Cell permeability
Biomimetics
DRNTU::Science::Biological sciences
Issue Date: 2014
Source: Lau, 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.
Series/Report no.: Chemical Science
Abstract: Stapled 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.
URI: https://hdl.handle.net/10356/81934
http://hdl.handle.net/10220/41069
DOI: 10.1039/c4sc00045e
Schools: School of Biological Sciences 
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SBS Journal Articles

Files in This Item:
File Description SizeFormat 
Functionalised staple linkages for modulating the cellular activity of stapled peptides.pdf4.09 MBAdobe PDFThumbnail
View/Open

SCOPUSTM   
Citations 5

145
Updated on Mar 28, 2024

Web of ScienceTM
Citations 5

147
Updated on Oct 26, 2023

Page view(s) 50

614
Updated on Apr 16, 2024

Download(s) 20

204
Updated on Apr 16, 2024

Google ScholarTM

Check

Altmetric


Plumx

Items in DR-NTU are protected by copyright, with all rights reserved, unless otherwise indicated.