From the Institute for Integrative Biology of the Cell (I2BC), CEA, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 91198 Gif sur Yvette cedex, France.
From the Institute for Integrative Biology of the Cell (I2BC), CEA, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 91198 Gif sur Yvette cedex, France
J Biol Chem. 2019 May 10;294(19):7573-7587. doi: 10.1074/jbc.RA118.005209. Epub 2019 Mar 13.
RNA viruses synthesize new genomes in the infected host thanks to dedicated, virally-encoded RNA-dependent RNA polymerases (RdRps). As such, these enzymes are prime targets for antiviral therapy, as has recently been demonstrated for hepatitis C virus (HCV). However, peculiarities in the architecture and dynamics of RdRps raise fundamental questions about access to their active site during RNA polymerization. Here, we used molecular modeling and molecular dynamics simulations, starting from the available crystal structures of HCV NS5B in ternary complex with template-primer duplexes and nucleotides, to address the question of ribonucleotide entry into the active site of viral RdRp. Tracing the possible passage of incoming UTP or GTP through the RdRp-specific entry tunnel, we found two successive checkpoints that regulate nucleotide traffic to the active site. We observed that a magnesium-bound nucleotide first binds next to the tunnel entry, and interactions with the triphosphate moiety orient it such that its base moiety enters first. Dynamics of RdRp motifs F1 + F3 then allow the nucleotide to interrogate the RNA template base prior to nucleotide insertion into the active site. These dynamics are finely regulated by a second magnesium dication, thus coordinating the entry of a magnesium-bound nucleotide with shuttling of the second magnesium necessary for the two-metal ion catalysis. The findings of our work suggest that at least some of these features are general to viral RdRps and provide further details on the original nucleotide selection mechanism operating in RdRps of RNA viruses.
RNA 病毒利用专门的病毒编码 RNA 依赖性 RNA 聚合酶(RdRps)在受感染的宿主中合成新的基因组。因此,这些酶是抗病毒治疗的主要靶点,最近丙型肝炎病毒(HCV)的研究已经证明了这一点。然而,RdRps 的结构和动力学的特殊性提出了关于在 RNA 聚合过程中进入其活性部位的基本问题。在这里,我们使用分子建模和分子动力学模拟,从 HCV NS5B 与模板-引物双链体和核苷酸的三元复合物的现有晶体结构开始,解决了核糖核苷酸进入病毒 RdRp 活性部位的问题。跟踪进入的 UTP 或 GTP 可能通过 RdRp 特异性进入隧道的情况,我们发现了两个连续的检查点,它们调节核苷酸向活性部位的流动。我们观察到,一个结合镁的核苷酸首先结合在隧道入口附近,并且与三磷酸部分的相互作用使其定向,使其碱基部分首先进入。RdRp 模体 F1 + F3 的动力学允许核苷酸在插入活性部位之前先与 RNA 模板碱基进行询问。这些动力学由第二个镁二价阳离子精细调节,从而协调与二价离子催化所需的第二个镁一起进入结合镁的核苷酸。我们工作的发现表明,至少其中一些特征是病毒 RdRps 的普遍特征,并进一步详细说明了在 RNA 病毒的 RdRps 中起作用的原始核苷酸选择机制。