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Glycobiology Advance Access published online on July 8, 2003
Glycobiology, doi:10.1093/glycob/cwg090
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Submitted on April 3, 2003
Revised on May 23, 2003
Accepted on May 24, 2003

© 2003 Oxford University Press

REVIEW

Glycosidase inhibitors: update and perspectives on practical use

Naoki Asano 1*

1 Faculty of Pharmaceutical Sciences, Hokuriku University, Ho-3 Kanagawa-machi, Kanazawa 920-1181, Japan

* To whom correspondence should be addressed. E-mail: naoki22{at}po.incl.ne.jp.

Abstract

About 40 years have passed since the classical glycosidase inhibitor, nojirimycin was discovered from the cultured broth of the Streptomyces species. Since then, over one hundred glycosidase inhibitors have been isolated from plants and micro-organisms. Modifying or blocking biological processes by specific glycosidase inhibitors has revealed the vital functions of glycosidases in living systems. Since enzyme-catalyzed carbohydrate hydrolysis is a biologically widespread process, glycosidase inhibitors have many potential applications as agrochemicals and therapeutic agents. Glycosidases are involved in the biosynthesis of the oligosaccharide chains and quality control mechanisms in the endoplasmic reticulum (ER) of the N-linked glycoproteins. Inhibition of these glycosidases can have profound effects on quality control, maturation, transport, and secretion of glycoproteins and can alter cell-cell or cell-virus recognition processes. This principle is the basis for the potential use of glycosidase inhibitors for viral infection, cancer, and genetic disorders. In this review, the past and current applications of glycosidase inhibitors to agricultural and medical fields and the prospect for new therapeutic applications will be reviewed.


agrochemicals, antidiabetic agents, antiviral agents, genetic disorders, glycosidase inhibitors
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