Bevilacqua P C, Cech T R
Department of Chemistry and Biochemistry, Howard Hughes Medical Institute, University of Colorado, Boulder 80309-0215, USA.
Biochemistry. 1996 Aug 6;35(31):9983-94. doi: 10.1021/bi9607259.
The human double-stranded RNA- (dsRNA) activated protein kinase (PKR) has a dsRNA-binding domain (dsRBD) that contains two tandem copies of the dsRNA-binding motif (dsRBM). The minimal-length polypeptide required to bind dsRNA contains both dsRBMs, as determined by mobility-shift and filter-binding assays. Mobility-shift experiments indicate binding requires a minimum of 16 base pairs of dsRNA, while a minimal-length site for saturation of longer RNAs is 11 base pairs. Bulge defects in the helix disfavor binding, and single-stranded tails do not strongly influence the dsRNA length requirement. These polypeptides do not bind an RNA-DNA hybrid duplex or dsDNA as judged by either mobility-shift or competition experiments, suggesting 2'-OH contacts on both strands of the duplex stabilize binding. Related experiments on chimeric duplexes in which specific sets of 2'-OHs are substituted with 2'-H or 2'-OCH3 reveal that the 2'-OHs required for binding are located along the entire 11 basepair site. These results are supported by Fe(II) EDTA footprinting experiments that show protein-dependent protection of the minor groove of dsRNA. The dependence of dsRNA-protein binding on salt concentration suggests that only one ionic contact is made between the protein and dsRNA phosphate backbone and that at physiological salt concentrations 90% of the free energy of binding is nonelectrostatic. Thus, the specificity of PKR for dsRNA over RNA-DNA hybrids and dsDNA is largely due to molecular recognition of a network of 2'-OHs involving both strands of dsRNA and present along the entire 11 base-pair site.
人类双链RNA(dsRNA)激活蛋白激酶(PKR)具有一个双链RNA结合结构域(dsRBD),该结构域包含双链RNA结合基序(dsRBM)的两个串联拷贝。通过迁移率变动和滤膜结合试验确定,结合dsRNA所需的最短长度多肽包含两个dsRBM。迁移率变动实验表明,结合至少需要16个碱基对的dsRNA,而使较长RNA饱和的最短位点是11个碱基对。螺旋中的凸起缺陷不利于结合,单链尾巴对dsRNA长度要求的影响不大。通过迁移率变动或竞争实验判断,这些多肽不结合RNA-DNA杂交双链体或dsDNA,这表明双链体两条链上的2'-OH接触稳定了结合。对特定2'-OH被2'-H或2'-OCH3取代的嵌合双链体进行的相关实验表明,结合所需的2'-OH沿着整个11个碱基对的位点分布。Fe(II)EDTA足迹实验支持了这些结果,该实验表明蛋白质对dsRNA小沟有依赖性保护作用。dsRNA与蛋白质结合对盐浓度的依赖性表明,蛋白质与dsRNA磷酸骨架之间仅形成一个离子接触,并且在生理盐浓度下,90%的结合自由能是非静电的。因此,PKR对dsRNA相对于RNA-DNA杂交体和dsDNA的特异性很大程度上归因于对涉及dsRNA两条链并沿整个11个碱基对位点存在的2'-OH网络的分子识别。