A large proportion of protein–protein interactions (PPIs) occur between a short peptide and a
globular protein domain; the peptides involved in surface interactions play important roles …

Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical
conformation. Stapling is carried out by covalently linking the side-chains of two amino …

Opioid receptors have been targeted for the treatment of pain and related disorders for
thousands of years and remain the most widely used analgesics in the clinic. Mu (μ), kappa …

Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …

Helix‐constrained polypeptides have attracted great interest for modulating protein–protein
interactions (PPI). It is not known which are the most effective helix‐inducing strategies for …

While the global market for peptide/protein-based therapeutics is witnessing significant
growth, the development of peptide drugs remains challenging due to their low oral …

Highlights•One of the most widely adopted strategies for α-helix stabilisation is peptide
stapling.•Stapled peptides are highly promising therapeutic agents.•General design …

Protein–protein interactions (PPIs) are tremendously important for the function of many
biological processes. However, because of the structure of many protein–protein interfaces …

The development of constrained peptides for inhibition of protein–protein interactions is an
emerging strategy in chemical biology and drug discovery. This manuscript introduces a …

Peptide macrocycles represent a chemical space where the best of biological tools can
synergize with the best of chemical approaches in the quest for leads against undruggable …