Development of bestatin-based activity-based probes for metallo-aminopeptidases.

摘要: A novel set of activity-based probes (ABPs) for functionally profiling metallo-aminopeptidases was synthesized based on the bestatin inhibitor scaffold, first synthesis analogues using solid-phase techniques. These ABPs were shown to label metallo-aminopeptidases, both a biotin and fluorophore reporter, in an activity-dependent manner. This probe class also be amenable ‘click’ chemistry labeling possible use live cells. Finally, we demonstrate that are able aminopeptidase complex proteome. Thus, these bestatin-based should have wide utility profile aminopeptidases many biological systems.