Ghosh Mahua, Meiss Gregor, Pingoud Alfred M, London Robert E, Pedersen Lars C
Laboratory of Structural Biology, NIEHS, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA.
J Biol Chem. 2007 Feb 23;282(8):5682-90. doi: 10.1074/jbc.M605986200. Epub 2006 Nov 30.
Nonspecific, extracellular nucleases have received enhanced attention recently as a consequence of the critical role that these enzymes can play in infectivity by overcoming the host neutrophil defense system. The activity of the cyanobacterial nuclease NucA, a member of the betabetaalpha Me superfamily, is controlled by the specific nuclease inhibitor, NuiA. Here we report the 2.3-A resolution crystal structure of the NucA-NuiA complex, showing that NucA inhibition by NuiA involves an unusual divalent metal ion bridge that connects the nuclease with its inhibitor. The C-terminal Thr-135(NuiA) hydroxyl oxygen is directly coordinated with the catalytic Mg(2+) of the nuclease active site, and Glu-24(NuiA) also extends into the active site, mimicking the charge of a scissile phosphate. NuiA residues Asp-75 and Trp-76 form a second interaction site, contributing to the strength and specificity of the interaction. The crystallographically defined interface is shown to be consistent with results of studies using site-directed NuiA mutants. This mode of inhibition differs dramatically from the exosite mechanism of inhibition seen with the DNase colicins E7/E9 and from other nuclease-inhibitor complexes that have been studied. The structure of this complex provides valuable insights for the development of inhibitors for related nonspecific nucleases that share the DRGH active site motif such as the Streptococcus pneumoniae nuclease EndA, which mediates infectivity of this pathogen, and mitochondrial EndoG, which is involved in recombination and apoptosis.
非特异性细胞外核酸酶近来受到了更多关注,因为这些酶在克服宿主中性粒细胞防御系统从而发挥感染性方面可起到关键作用。蓝藻核酸酶NucA是ββα Me超家族的成员,其活性由特异性核酸酶抑制剂NuiA控制。在此我们报道了NucA-NuiA复合物的2.3埃分辨率晶体结构,结果表明NuiA对NucA的抑制涉及一个不同寻常的二价金属离子桥,该桥将核酸酶与其抑制剂连接起来。NuiA的C末端苏氨酸-135的羟基氧直接与核酸酶活性位点的催化性镁离子(Mg2+)配位,并且谷氨酸-24(NuiA)也延伸到活性位点,模拟了可切割磷酸基团的电荷。NuiA的天冬氨酸-75和色氨酸-76残基形成了第二个相互作用位点,有助于增强相互作用的强度和特异性。晶体学定义的界面与使用定点NuiA突变体的研究结果一致。这种抑制模式与大肠杆菌核酸酶E7/E9所呈现的别构抑制机制以及其他已研究的核酸酶-抑制剂复合物显著不同。该复合物的结构为开发针对具有DRGH活性位点基序的相关非特异性核酸酶的抑制剂提供了有价值的见解,这些核酸酶包括介导肺炎链球菌感染性的肺炎链球菌核酸酶EndA以及参与重组和凋亡的线粒体核酸酶EndoG。