Chemo-Enzymatic Synthesis of Novel Oligosaccharide Hydrolase Inhibitors Using Glycosynthases

The chemical and structural diversity of naturally occurring glycosides affords an impressive array of enzymes hydrolyzing this molecules, which consequently play an important role in cell biology. Glycosidase- and glycoprotein processing inhibitors as therapeutics offer potential for the treatment of viral infections such as those caused by HIV and influenza. Such compounds also show anticancer properties by inhibition of glycosylation or oligosaccharide processing enzymes on the surface of tumour cells. The chemo-enzymatic synthesis of such inhibitors has become a major challenge, many approaches are in the literature. Lately glycosynthases, mutant glycosidases, where the unwanted hydrolyzing activity is inactivated, were successfully employed, allowing to increase the yields of the desired products dramatically. Novel oligosaccharide hydrolase inhibitors will be synthesised using such glycosynthases and their biological activities will be studied.