Development of fluorescent substrate for glycan processing glycosidase, and screening of the novel glycosidase inhibitor

Glycosylation is performed by various glycosidases and glycosyltransferases. Glycan formation and degradation by these enzymes is crucial for various physiological events in cells. Recently, functional analysis of glycan-processing enzymes has actively been performed, and the enzymes are focused on novel drug targets. However, previously reported inhibitors for the glycan-process-ing enzymes have encountered major problems. Additionally, screening systems for the inhibitors of glycan-processing enzymes are lacking. Accordingly, we are developing cell-based fluorescence imaging systems for glycan-processing glycosidases and screening of their novel inhibitors. In this paper, we introduce the development of a quinone methide cleavage (QMC) fluorescent substrate platform for the glycan-processing glycosidase and the discovery of novel glycosidase inhibitors using these platform-based fluorescent substrates.