Monitoring and modulating O-GlcNAcylation: assays and inhibitors of O-GlcNAc processing enzymes
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| Authors: | Alteen, MG; Tan, HY; Vocadlo, DJ |
| Year: | 2021 |
| Journal: | Curr. Opin. Struct. Biol. 68: 157-165 Article Link (DOI) PubMed |
| Title: | Monitoring and modulating O-GlcNAcylation: assays and inhibitors of O-GlcNAc processing enzymes |
| Abstract: | O-linked N-acetylglucosamine (O-GlcNAc) is protein modification that is emerging as a regulator of diverse aspects of cellular physiology. Aberrant O-GlcNAcylation has been linked to several diseases, spurring the creation of methods to detect and perturb the activity of the two enzymes that govern this modification - O-GlcNAc transferase (OGT) and O-GlcNAcase (OGA). Here we summarize assays used for these two enzymes. We also detail the latest structure-guided development of inhibitors of these two enzymes and touch on selected reports that underscore the utility of inhibitors as tools for uncovering the diverse roles of O-GlcNAc in cell function. Finally, we summarize recent reports on the potential therapeutic benefits of antagonizing these enzymes and comment on outstanding challenges within the field. |
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