Novel approaches for the design and synthesis of selective mannosidase inhibitors

CARB 12

Geert-Jan Boons, gjboons@ccrc.uga.edu, Complex Carbohydrate Research Center, University of Georgia, 315 Riverbend Road, Athens, GA 30602-4712
Compounds that can interfere in the biosynthesis of oligosaccharides may offer potential as therapeutics for a wide range of diseases. We have developed a general approach for the design of selective glycosidase inhibitors based on feedback inhibition. In this approach, a pro-drug is converted into an active inhibitor by the action of a targeted glycosidase. The exquisite selectivity of glycosidases for their substrates assures that high selectivity is achieved. The approach has been applied for the development of a selective inhibitor of Golgi Mannosidase II, which is a target for cancer therapy development.