N-Butyl-l-deoxynojirimycin (l-NBDNJ): Synthesis of an Allosteric Enhancer of α-Glucosidase Activity for the Treatment of Pompe Disease.
Daniele D'AlonzoMaria De FenzaCaterina PortoRoberta IaconoMylene HuebeckerBeatrice Cobucci-PonzanoDavid A PriestmanFrances PlattGiancarlo ParentiMarco MoracciGiovanni PalumboAnnalisa GuaragnaPublished in: Journal of medicinal chemistry (2017)
The highly stereocontrolled de novo synthesis of l-NBDNJ (the unnatural enantiomer of the iminosugar drug Miglustat) and a preliminary evaluation of its chaperoning potential are herein reported. l-NBDNJ is able to enhance lysosomal α-glucosidase levels in Pompe disease fibroblasts, either when administered singularly or when coincubated with the recombinant human α-glucosidase. In addition, differently from its d-enantiomer, l-NBDNJ does not act as a glycosidase inhibitor.