In a recent study, a new type of peptide drug, called a stapled peptide, was designed as a dual inhibitor of both MDM2 and MDMX, which are inhibitors of the p53 tumor suppressor. The peptide drug design, includes a hydrocarbon bond (called a staple) to impart enhanced stability and protein-protein interaction targeting, and was able to re-activate the p53 apoptosis and cell cycle arrest pathway in xenograft cancer models.


Stapled peptides represent a new type of therapeutics that may address the low stability, and target specificity that is often seen in traditional peptide and small molecule therapeutics. Stapled peptides are part of the growing therapeutic macrocyclic and constrained peptide movement aimed at tackling targets that were once considered un-druggable.