Bisubstrate Analogues as Glycosyltransferase Inhibitors

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 9 , Issue 1 , 2009

Become EABM
Become Reviewer

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.

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

Rights & PermissionsPrintExport Cite as


Article Details

VOLUME: 9
ISSUE: 1
Year: 2009
Page: [87 - 105]
Pages: 19
DOI: 10.2174/156802609787354351

Article Metrics

PDF: 32