Background: Peptide-based pharmaceuticals have recently experienced a renaissance
due to their ability to fill the gap between the two main classes of available drugs, small
molecules and biologics. Peptides combine the high potency and selectivity typical of large
proteins with some of the characteristic advantages of small molecules such as synthetic accessibility,
stability and the potential of oral bioavailability.
Methods: In the present manuscript we review the recent literature on selected peptide-based
approaches for cancer treatment, emphasizing recent advances, advantages and challenges of
Results: One of the applications in which peptide-based approaches have grown rapidly is
cancer therapy, with a focus on new and established targets. We describe, with selected examples,
some of the novel peptide-based methods for cancer treatment that have been developed
in the last few years, ranging from naturally-occurring and modified peptides to peptidedrug
conjugates, peptide nanomaterials and peptide-based vaccines.
Conclusion: This review brings out the emerging role of peptide-based strategies in oncology
research, critically analyzing the advantages and limitations of these approaches and the potential
for their development as effective anti-cancer therapies.