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Cellular and Molecular Life Sciences: CMLS logoLink to Cellular and Molecular Life Sciences: CMLS
. 2009 Jan 12;66(9):1479–1492. doi: 10.1007/s00018-008-8522-3

Sugar-mimicking glycosidase inhibitors: bioactivity and application

N Asano 1,
PMCID: PMC11131492  PMID: 19132292

Abstract.

A large number of compounds mimicking the structures of monosaccharides or oligosaccharides have been discovered from natural sources. Such sugar mimics inhibit carbohydrate-degrading enzymes because of a structural resemblance to the sugar moiety of the natural substrate. Carbohydrate-degrading enzymes are involved in a wide range of important biological processes, such as intestinal digestion, posttranslational processing of the sugar chain of glycoproteins, their quality control mechanisms, lysosomal catabolism of glycoconjugates, and some viral infections. It has now been realized that inhibitors of the enzymes have enormous therapeutic potential in diabetes and lysosomal storage disorders. In this review, the general bioactivity, current applications, and the prospects for new therapeutic applications are described.

Keywords. Six-membered sugar mimics, five-membered sugar mimics, α-glucosidase inhibitor, glycogen-degrading enzyme inhibitor, diabetes, glucosylceramide synthase inhibitor, pharmacological chaperone, lysosomal storage disorder

Footnotes

Received 27 August 2008; received after revision 08 November 2008; accepted 03 December 2008


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