School of Science, Western Sydney University, Penrith, New South Wales, Australia.
Department of Microbiology, The Ohio State University, Columbus, Ohio, USA.
Proteins. 2024 Nov;92(11):1308-1317. doi: 10.1002/prot.26725. Epub 2024 Jul 3.
The ongoing global pandemic of the coronavirus 2019 (COVID-19) disease is caused by the virus SARS-CoV-2, with very few highly effective antiviral treatments currently available. The machinery responsible for the replication and transcription of viral RNA during infection is made up of several important proteins. Two of these are nsp12, the catalytic subunit of the viral polymerase, and nsp9, a cofactor of nsp12 involved in the capping and priming of viral RNA. While several recent studies have determined the structural details of the interaction of nsp9 with nsp12 in the context of RNA capping, very few biochemical or biophysical details are currently available. In this study, we have used a combination of surface plasmon resonance (SPR) experiments, size exclusion chromatography (SEC) experiments, and biochemical assays to identify specific nsp9 residues that are critical for nsp12 binding as well as RNAylation, both of which are essential for the RNA capping process. Our data indicate that nsp9 dimerization is unlikely to play a significant functional role in the virus. We confirm that a set of recently discovered antiviral peptides inhibit nsp9-nsp12 interaction by specifically binding to nsp9; however, we find that these peptides do not impact RNAylation. In summary, our results have important implications for future drug discovery efforts to combat SARS-CoV-2 and any newly emerging coronaviruses.
正在全球流行的 2019 年冠状病毒(COVID-19)疾病是由病毒 SARS-CoV-2 引起的,目前仅有极少数非常有效的抗病毒治疗方法。负责在感染过程中复制和转录病毒 RNA 的机制由几种重要的蛋白质组成。其中两种是 nsp12,病毒聚合酶的催化亚基,以及 nsp9,一种参与病毒 RNA 加帽和引发的 nsp12 辅助因子。尽管最近有几项研究确定了 nsp9 与 RNA 加帽背景下 nsp12 相互作用的结构细节,但目前仅获得了很少的生化或生物物理细节。在这项研究中,我们结合使用表面等离子体共振(SPR)实验、排阻层析(SEC)实验和生化测定来鉴定对 nsp12 结合以及 RNA 酰化至关重要的特定 nsp9 残基,这两者对于 RNA 加帽过程都是必不可少的。我们的数据表明,nsp9 二聚化不太可能在病毒中发挥重要功能。我们证实,一组最近发现的抗病毒肽通过特异性结合 nsp9 来抑制 nsp9-nsp12 相互作用;然而,我们发现这些肽不会影响 RNA 酰化。总之,我们的结果对未来针对 SARS-CoV-2 和任何新出现的冠状病毒的药物发现工作具有重要意义。