Bisubstrate Analogues as Glycosyltransferase Inhibitors

Title: Bisubstrate Analogues as Glycosyltransferase Inhibitors

Volume: 9 Issue: 1

Author(s): Masayuki Izumi, Hideya Yuasa and Hironobu Hashimoto

Affiliation:

Keywords: Bisubstrate analogue, glycosyltransferase, inhibitor, design, synthesis

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 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.

Cite this article as:

Izumi Masayuki, Yuasa Hideya and Hashimoto Hironobu, Bisubstrate Analogues as Glycosyltransferase Inhibitors, Current Topics in Medicinal Chemistry 2009; 9 (1) . https://dx.doi.org/10.2174/156802609787354351