Peptidomics methods for the identification of peptidase-substrate interactions

► Peptidases control physiological signaling by regulating bioactive peptides. ► Understanding and controlling bioactive peptide regulation is of biomedical interest. ► Here, we describe peptidomics approaches to identify substrates of peptidases. ► Conversely, peptidomics can also identify peptidases that regulate specific peptides. ► Thus, peptidomics is an important new approach for identifying novel drug targets.