title: Bisubstrate analogues as glycosyltransferase inhibitors.
abstract: Oligosaccharides in glycoconjugates such as glycoproteins and glycolipids play important roles in a variety of biological functions. Since glycosyltransferases are responsible for the biosynthesis of these oligosaccharides, inhibitors of glycosyltransferases are targets for drug discovery. Bisubstrate analogues, in which donor and acceptor analogue are covalently attached to each other, offer donor's high affinity and acceptor's high selectivity. In this review, we describe the design and synthesis of bisubstrate analogues of glycosyltransferases as well as their inhibitory potency hoping to inform the development of potent and selective inhibitors.
authors.affiliation: Department of Life Science, Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, Yokohama, Japan. masayuki.izumi@aist.go.jp
authors.forename: Masayuki
authors.initials: M
authors.lastname: Izumi
authors.forename: Hideya
authors.initials: H
authors.lastname: Yuasa
authors.forename: Hironobu
authors.initials: H
authors.lastname: Hashimoto
mesh_terms: D002240:Carbohydrate Sequence; D004791:Enzyme Inhibitors / Q000737:chemistry*; D005647:Fucosyltransferases / Q000037:antagonists & inhibitors / Q000737:chemistry; D005700:Galactosyltransferases / Q000037:antagonists & inhibitors; D016695:Glycosyltransferases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D008969:Molecular Sequence Data; D013329:Structure-Activity Relationship; D014415:Tunicamycin / Q000031:analogs & derivatives / Q000737:chemistry
chemical_list: D004791:Enzyme Inhibitors; D014415:Tunicamycin; D016695:Glycosyltransferases; D005647:Fucosyltransferases; D005700:Galactosyltransferases