Stapled Peptides Small Molecules and Peptides

Peptides are an alternative class of drug molecule, which are being used to therapeutically target previously undruggable protein-protein interactions (PPIs). The interacting surfaces of PPIs are shallow/flat, large and non-hydrophobic making them ideal targets for peptides, which are able to mimic a native protein. Peptides are highly selective, but often suffer from poor cell permeability, plasma stability and bioavailability.

Stapling a peptide overcomes these limitations by the formation ...