Background: Because of their wide range of functions, endogenous peptides have great potential either as drugs themselves or as drug targets.
Objective: To provide an overview of the current use of peptides as drugs (targets) and describe how improvements in peptide biochemistry and the application of peptidomics studies can lead to the discovery of new diagnostic and therapeutic targets.
Methods: We discuss the different peptidomics technologies and their application in the study of human and animal disease models, animal venoms, antimicrobial peptides, G-protein-coupled receptor ligands and biomarkers.
Results/conclusions: At present, peptide drugs represent a small but growing number of pharmaceutical molecules. The peptidomics methodology, which was introduced 7 years ago to study naturally occurring peptides, will lead to a plethora of new peptide drug leads.