Roth Christian, Chan Sherry, Offen Wendy A, Hemsworth Glyn R, Willems Lianne I, King Dustin T, Varghese Vimal, Britton Robert, Vocadlo David J, Davies Gideon J
York Structural Biology Laboratory, Department of Chemistry University of York, York, UK.
Department of Chemistry, Simon Fraser University, Burnaby, British Columbia, Canada.
Nat Chem Biol. 2017 Jun;13(6):610-612. doi: 10.1038/nchembio.2358. Epub 2017 Mar 27.
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.
O-连接的N-乙酰葡糖胺水解酶（OGA）从众多核质蛋白上去除O-连接的N-乙酰葡糖胺（O-GlcNAc）。通过OGA片段的共表达和组装，我们确定了人OGA的三维结构，揭示了一种不寻常的螺旋交换二聚体，为更好地理解OGA的底物识别和调控奠定了结构基础。OGA与一系列抑制剂复合物的结构为具有临床价值的抑制剂设计提供了精确蓝图。
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