Recent Insights into Inhibition,Structure, and Mechanism of Configuration-Retaining Glycosidases

Not “from above”, but “from the side” : Configuration-retaining β-glycosidases protonate their substrate either anti or syn to the endocyclic C1−O bond as the first step in the enzymic cleavage of the glycosidic bond (see schematic drawing). Insights into the mechanism of action of glycosidases have been gained by a combination of the synthesis of inhibitors, the study of the kinetics of their inhibition, and the analysis of the crystal structures of glycosidases and glycosidase–ligand complexes.