Abstract

Glycosyltransferases and glycosidases work together to constructthe oligosaccharide moieties of biologically active glycoconjugates.Although many excellent glycosidase inhibitors have been developed,some of which are in clinical use, there are relatively few promisingcandidates of glycosyltransferase inhibitors. In this review, wesummarize the current state of the development of glycosyltransferaseinhibitors. 1 Introduction 2 Basic Strategy for Designing Glycosyltransferase Inhibitors 3 Sugar Nucleotide Analogues 4 Analogues of Acceptor Oligosaccharides (Acceptor [nl]Analogues) 5 Bisubstrate Inhibitors 6 High-Throughput Screening: Discovering Structurally [nl]SimpleInhibitors 7 Antisense Inhibitors 8 Questions and Future Directions

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