Increasing O-GlcNAc levels: An overview of small-molecule inhibitors of O-GlcNAcase - PubMed (original) (raw)

Review

. 2010 Feb;1800(2):107-21.

doi: 10.1016/j.bbagen.2009.07.028. Epub 2009 Aug 4.

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Review

Increasing O-GlcNAc levels: An overview of small-molecule inhibitors of O-GlcNAcase

Matthew S Macauley et al. Biochim Biophys Acta. 2010 Feb.

Abstract

The O-GlcNAc modification is found on many nucleocytoplasmic proteins. The dynamic nature of O-GlcNAc, which in some ways is reminiscent of phosphorylation, has enabled investigators to modulate the stoichiometry of O-GlcNAc on proteins in order to study its function. Although several genetic and pharmacological methods for manipulating O-GlcNAc levels have been described, one of the most direct approaches of increasing global O-GlcNAc levels is by using small-molecule inhibitors of O-GlcNAcase (OGA). As the interest in increasing O-GlcNAc levels has grown, so too has the number of OGA inhibitors. This review provides an overview of the available methods of increasing O-GlcNAc levels, with a special emphasis on inhibition of OGA by small molecules. Known inhibitors of OGA are discussed with particular attention on those most suitable for cell-based biological studies. Several examples in which OGA inhibitors have been used to study the functional role of the O-GlcNAc modification in biological systems are discussed, highlighting the pros and cons of different inhibitors.

Copyright 2009 Elsevier B.V. All rights reserved.

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