Functionalised staple linkages for modulating the cellular activity of stapled peptides

• Main 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.
• Other Authors: School of Biological Sciences
• Format: Article
• Language: English
• Published: 2016
• Subjects: Cell permeability; Biomimetics; DRNTU::Science::Biological sciences
• Online Access: https://hdl.handle.net/10356/81934; http://hdl.handle.net/10220/41069
• Institution: Nanyang Technological University

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 bear...