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Alteen, Matthew G; Tan, Hong Yee; Vocadlo, David J
Current opinion in structural biology, 06/2021, Letnik: 68Journal Article
Display omitted •Good cell active competitive inhibitors of O-GlcNAc processing enzymes are available.•In vitro assays for O-GlcNAc processing enzymes are established.•OGA inhibitors are advancing into the clinic.•Improved inhibitors and cell-based assays are needed to advance the field. 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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Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Vir: Osebne bibliografije
in: SICRIS
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