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Bisubstrate Analogues as Glycosyltransferase Inhibitors

[ Vol. 9 , Issue. 1 ]


Masayuki Izumi, Hideya Yuasa and Hironobu Hashimoto   Pages 87 - 105 ( 19 )


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 donors high affinity and acceptors 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.


Bisubstrate analogue, glycosyltransferase, inhibitor, design, synthesis


Research Center of Advanced Bionics, National Institute of Industrial Science and Technology (AIST), 1-1-1 Higashi, Tsukuba, Ibaraki 305-8565 Japan.

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