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.
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