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Targeted covalent inhibition of O-GlcNAc transferase in cells.

ABSTRACT: O-GlcNAc transferase (OGT) glycosylates numerous proteins and is implicated in many diseases. To date, most OGT inhibitors lack either sufficient potency or characterized specificity in cells. We report the first targeted covalent inhibitor that predominantly reacts with OGT but does not affect other functionally similar enzymes. This study provides a new strategy to interrogate cellular OGT functions and to investigate other glycosyltransferases.

SUBMITTER: Worth M

PROVIDER: S-EPMC6823131 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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Targeted covalent inhibition of O-GlcNAc transferase in cells.

Worth Matthew M Hu Chia-Wei CW Li Hao H Fan Dacheng D Estevez Arielis A Zhu Dongsheng D Wang Ao A Jiang Jiaoyang J

Chemical communications (Cambridge, England) 20191001 88

O-GlcNAc transferase (OGT) glycosylates numerous proteins and is implicated in many diseases. To date, most OGT inhibitors lack either sufficient potency or characterized specificity in cells. We report the first targeted covalent inhibitor that predominantly reacts with OGT but does not affect other functionally similar enzymes. This study provides a new strategy to interrogate cellular OGT functions and to investigate other glycosyltransferases. ...[more]

PMID: 31626249

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