Targeted covalent inhibition of: O -GlcNAc transferase in cells

Matthew Worth; Chia Wei Hu; Hao Li; Dacheng Fan; Arielis Estevez; Dongsheng Zhu; Ao Wang; Jiaoyang Jiang

doi:10.1039/c9cc04560k

Targeted covalent inhibition of: O -GlcNAc transferase in cells

Matthew Worth
, Chia Wei Hu
, Hao Li
, Dacheng Fan
, Arielis Estevez
, Dongsheng Zhu
, Ao Wang
, Jiaoyang Jiang

Research output: Contribution to journal › Article › peer-review

25 Scopus citations

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.

Original language	English (US)
Pages (from-to)	13291-13294
Number of pages	4
Journal	Chemical Communications
Volume	55
Issue number	88
DOIs	https://doi.org/10.1039/c9cc04560k
State	Published - 2019
Externally published	Yes

ASJC Scopus subject areas

Electronic, Optical and Magnetic Materials
Catalysis
Ceramics and Composites
General Chemistry
Surfaces, Coatings and Films
Metals and Alloys
Materials Chemistry

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10.1039/c9cc04560k

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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.",

author = "Matthew Worth and Hu, \{Chia Wei\} and Hao Li and Dacheng Fan and Arielis Estevez and Dongsheng Zhu and Ao Wang and Jiaoyang Jiang",

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T2 - O -GlcNAc transferase in cells

AU - Worth, Matthew

AU - Hu, Chia Wei

AU - Li, Hao

AU - Fan, Dacheng

AU - Estevez, Arielis

AU - Zhu, Dongsheng

AU - Wang, Ao

AU - Jiang, Jiaoyang

PY - 2019

Y1 - 2019

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AB - 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.

UR - https://www.scopus.com/pages/publications/85074309905

UR - https://www.scopus.com/pages/publications/85074309905#tab=citedBy

U2 - 10.1039/c9cc04560k

DO - 10.1039/c9cc04560k

M3 - Article

C2 - 31626249

AN - SCOPUS:85074309905

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VL - 55

SP - 13291

EP - 13294

JO - Chemical Communications

JF - Chemical Communications

IS - 88

ER -

Targeted covalent inhibition of: O -GlcNAc transferase in cells

Abstract

ASJC Scopus subject areas

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