Jørgensen René, Merrill A Rod, Yates Susan P, Marquez Victor E, Schwan Adrian L, Boesen Thomas, Andersen Gregers R
Centre for Structural Biology, Department of Molecular Biology, University of Aarhus, Gustav Wieds Vej 10C, DK-8000, Denmark.
Nature. 2005 Aug 18;436(7053):979-84. doi: 10.1038/nature03871.
The bacteria causing diphtheria, whooping cough, cholera and other diseases secrete mono-ADP-ribosylating toxins that modify intracellular proteins. Here, we describe four structures of a catalytically active complex between a fragment of Pseudomonas aeruginosa exotoxin A (ETA) and its protein substrate, translation elongation factor 2 (eEF2). The target residue in eEF2, diphthamide (a modified histidine), spans across a cleft and faces the two phosphates and a ribose of the non-hydrolysable NAD+ analogue, betaTAD. This suggests that the diphthamide is involved in triggering NAD+ cleavage and interacting with the proposed oxacarbenium intermediate during the nucleophilic substitution reaction, explaining the requirement of diphthamide for ADP ribosylation. Diphtheria toxin may recognize eEF2 in a manner similar to ETA. Notably, the toxin-bound betaTAD phosphates mimic the phosphate backbone of two nucleotides in a conformational switch of 18S rRNA, thereby achieving universal recognition of eEF2 by ETA.
引起白喉、百日咳、霍乱及其他疾病的细菌会分泌单ADP核糖基化毒素,这些毒素可修饰细胞内蛋白质。在此,我们描述了铜绿假单胞菌外毒素A(ETA)片段与其蛋白质底物翻译延伸因子2(eEF2)之间具有催化活性的复合物的四种结构。eEF2中的靶标残基二羟基赖氨酸(一种修饰的组氨酸)跨越一个裂缝,面向不可水解的NAD+类似物βTAD的两个磷酸基团和一个核糖。这表明二羟基赖氨酸在亲核取代反应中参与触发NAD+裂解并与拟议的氧碳鎓中间体相互作用,解释了二羟基赖氨酸对ADP核糖基化的必要性。白喉毒素可能以与ETA类似的方式识别eEF2。值得注意的是,毒素结合的βTAD磷酸基团在18S rRNA的构象转换中模拟了两个核苷酸的磷酸主链,从而实现了ETA对eEF2的普遍识别。