Regulation of protein–protein interactions using stapled peptides

The targeting of protein–protein interactions (PPIs) that include secondary structure motifs such as the α -helix and ß -sheet is a challenge in chemical biology. A new class of compounds called stapled peptides have been developed that mimic α -helix secondary structures involved in PPIs. These conformationally constrained peptides also show favorable physicochemical properties and so are promising lead compounds for drug discovery. This review focuses on the design aspects of hydrocarbon constrained α -helical proteomimetics and provides examples in which they target biologically relevant PPIs.