Peptidomics methods for the identification of peptidase–substrate interactions

Peptidases have important roles in controlling physiological signaling through their regulation of bioactive peptides. Understanding and controlling bioactive peptide regulation is of great biomedical interest and approaches that elucidate the interplay between peptidases and their substrates are vital for achieving this goal. Here, we highlight the utility of recent peptidomics approaches in identifying endogenous substrates of peptidases. These approaches reveal bioactive substrates and help characterize the biochemical functions of the enzyme. Most recently, peptidomics approaches have been applied to address the challenging question of identifying the peptidases responsible for regulating specific bioactive peptides. Since peptidases are of great biomedical interest, these approaches will begin to impact our ability to identify new drug targets that regulate important bioactive peptides. ⺠Peptidases control physiological signaling by regulating bioactive peptides. ⺠Understanding and controlling bioactive peptide regulation is of biomedical interest. ⺠Here, we describe peptidomics approaches to identify substrates of peptidases. ⺠Conversely, peptidomics can also identify peptidases that regulate specific peptides. ⺠Thus, peptidomics is an important new approach for identifying novel drug targets.