Peterson de Andrade

TL;DR: This tutorial review categorise and analyse key examples of peptide stapling in terms of their synthesis and applicability to biological systems.

TL;DR: This work reports the divergent synthesis of “functionalised” stapled peptides via an efficient two-component strategy, and improves the cell permeability and p53 activating capability of an otherwise impermeable p53 stapling peptide by introducing cationic groups on the staple linkage, rather than modifying the peptide sequence.

TL;DR: A novel stapling technique based on a double strain-promoted azide-alkyne reaction is reported, and its biocompatibility is exploited to accelerate the discovery of cell-active stapled peptides.

TL;DR: An optimized procedure for the stabilization of linear diazido peptides in an α-helical conformation upon reaction with dialkynyl linkers under Cu(I) catalysis is presented, referred to as 'double-click' stapling.

TL;DR: It is demonstrated a K24R mutation, necessary for cellular activity in hydrocarbon-stapled p53 peptides, is not required for analogous 'double-click' peptides.