Structural and functional insight into human O-GlcNAcase

被引：82

作者：

Roth, Christian ^{[1
]}

Chan, Sherry ^{[1
]}

Offen, Wendy A. ^{[1
]}

Hemsworth, Glyn R. ^{[1
]}

Willems, Lianne I. ^{[2
]}

King, Dustin T. ^{[2
]}

Varghese, Vimal ^{[2
]}

Britton, Robert ^{[2
]}

Vocadlo, David J. ^{[2
]}

Davies, Gideon J. ^{[1
]}

机构：

[1] Univ York, York Struct Biol Lab, Dept Chem, York, N Yorkshire, England

[2] Simon Fraser Univ, Dept Chem, Burnaby, BC, Canada

来源：

NATURE CHEMICAL BIOLOGY | 2017年 / 13卷 / 06期

基金：

英国生物技术与生命科学研究理事会; 加拿大健康研究院;

关键词：

BETA-N-ACETYLGLUCOSAMINIDASE; MACROMOLECULAR CRYSTALLOGRAPHY; CYTOSOLIC PROTEINS; GLCNACYLATION; SOFTWARE; BRAIN; INHIBITORS; MECHANISM; SUBSTRATE; GLYCOSYLATION;

D O I：

10.1038/nchembio.2358

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

O-GlcNAc hydrolase (OGA) removes O-linked N-acetylglucosamine (O-GlcNAc) from a myriad of nucleocytoplasmic proteins. Through co-expression and assembly of OGA fragments, we determined the three-dimensional structure of human OGA, revealing an unusual helix-exchanged dimer that lays a structural foundation for an improved understanding of substrate recognition and regulation of OGA. Structures of OGA in complex with a series of inhibitors define a precise blueprint for the design of inhibitors that have clinical value.

引用

页码：610 / +

页数：5

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