Asaccharolytic gram-negative bacteria, such as Stenotrophomonas maltophiliia (multidrug-resistant opportunistic pathogen) and Porphyromonas gingivalis (a periodontal pathogen), utilizes peptides or protein as an energy source instead of carbohydrate. Inner membrane of these bacteria preferentially transports not amino acids, but dipeptides. Thus, production of dipeptide by dipeptidyl peptidases (DPPs), which exists in periplasm region are very important for growth of these bacteria. DPPs of these bacteria are classified into Clan SC Family S9 (DPP4, POP) and Clan PA Family S46 (DPP7), peptidases belonging to Family S46 are not found in mammals. In addition, Family S46 peptides play mainly dipeptides production, so the peptides are promising as target for antibiotics.
At this time, we determined the three-dimensional structure of DAP BII (Bacterial DPP7) from Pseudoxanthomonas mexicana WO24. This is the first structure example as peptidase belonging to Family S46 peptidases. The overall structure of DAP BII reveals that it comprised of a chymotrypsin fold catalytic domain and α-helical domain. The enzymes belonging to Clan PA contain chymotrypsin fold and are endopeptidase except for S46 peptidases. Structure analysis of apo and peptide-bound forms of DAP BII reveal that the Asn330 in α-helical domain involved in recognition of the N-terminus of the substrate peptide. Furthermore, it reveals the residues comprising an S1 pocket of DAP BII and the substrate recognition mode of the peptide. Development of new inhibitors, which is target to metabolic pathway of peptides for asaccharolytic gram-negative bacteria is expected by this structural studies.