Structure, mechanism and inhibition of Golgi α-mannosidase II

► Golgi mannosidase II (GMII) is a core component of the N-glycosylation pathway. ► GMII inhibitors are of interest as potential anti-cancer or anti-infection compounds. ► Structural analysis of the Drosophila GMII (dGMII) has shed light on the catalytic process and mode of inhibition. ► The mechanism by which GMII binds the substrate and then rearranges to cleave two different glycosidic linkages is described. ► Novel GMII inhibitors show effectiveness in inhibiting the growth of tumor cells.