Leeper Thomas, Zhang Suxin, Van Voorhis Wesley C, Myler Peter J, Varani Gabriele
School of Medicine, University of Washington, Seattle, WA 98195, USA.
Acta Crystallogr Sect F Struct Biol Cryst Commun. 2011 Sep 1;67(Pt 9):1141-7. doi: 10.1107/S1744309111012346. Epub 2011 Aug 16.
Glutaredoxin proteins (GLXRs) are essential components of the glutathione system that reductively detoxify substances such as arsenic and peroxides and are important in the synthesis of DNA via ribonucleotide reductases. NMR solution structures of glutaredoxin domains from two Gram-negative opportunistic pathogens, Brucella melitensis and Bartonella henselae, are presented. These domains lack the N-terminal helix that is frequently present in eukaryotic GLXRs. The conserved active-site cysteines adopt canonical proline/tyrosine-stabilized geometries. A difference in the angle of α-helix 2 relative to the β-sheet surface and the presence of an extended loop in the human sequence suggests potential regulatory regions and/or protein-protein interaction motifs. This observation is consistent with mutations in this region that suppress defects in GLXR-ribonucleotide reductase interactions. These differences between the human and bacterial forms are adjacent to the dithiol active site and may permit species-selective drug design.
谷氧还蛋白(GLXRs)是谷胱甘肽系统的重要组成部分,该系统可对砷和过氧化物等物质进行还原性解毒,并且在通过核糖核苷酸还原酶合成DNA的过程中发挥重要作用。本文展示了两种革兰氏阴性机会致病菌——羊布鲁氏菌和汉氏巴尔通体的谷氧还蛋白结构域的核磁共振溶液结构。这些结构域缺乏真核生物GLXRs中常见的N端螺旋。保守的活性位点半胱氨酸采用典型的脯氨酸/酪氨酸稳定几何结构。α螺旋2相对于β折叠表面的角度差异以及人类序列中存在的延伸环表明存在潜在的调控区域和/或蛋白质-蛋白质相互作用基序。这一观察结果与该区域中抑制GLXR-核糖核苷酸还原酶相互作用缺陷的突变一致。人类和细菌形式之间的这些差异与二硫醇活性位点相邻,可能有助于进行物种选择性药物设计。