State Key Laboratory of Microbial Technology, Shandong University, 72 Binhai Road, Qingdao 266237, PR China.
State Key Laboratory of Microbial Technology, Shandong University, 72 Binhai Road, Qingdao 266237, PR China.
Int J Biol Macromol. 2023 Jan 31;226:946-955. doi: 10.1016/j.ijbiomac.2022.12.112. Epub 2022 Dec 14.
The coronavirus disease 2019 has been ravaging throughout the world for three years and has severely impaired both human health and the economy. The causative agent, severe acute respiratory syndrome coronavirus 2 employs the viral RNA dependent RNA polymerase (RdRp) complex for genome replication and transcription, making RdRp an appealing target for antiviral drug development. Systematic characterization of RdRp will undoubtedly aid in the development of antiviral drugs targeting RdRp. Here, our research reveals that RdRp can recognize and utilize nucleoside diphosphates as a substrate to synthesize RNA with an efficiency of about two thirds of using nucleoside triphosphates as a substrate. Nucleoside diphosphates incorporation is also template-specific and has high fidelity. Moreover, RdRp can incorporate β-d-N4-hydroxycytidine into RNA while using diphosphate form molnupiravir as a substrate. This incorporation results in genome mutation and virus death. It is also observed that diphosphate form molnupiravir is a better substrate for RdRp than the triphosphate form molnupiravir, presenting a new strategy for drug design.
新型冠状病毒病肆虐全球已达三年,严重损害了人类健康和经济。其病原体严重急性呼吸系统综合征冠状病毒 2 使用病毒 RNA 依赖性 RNA 聚合酶(RdRp)复合物进行基因组复制和转录,使 RdRp 成为抗病毒药物开发的一个有吸引力的靶点。对 RdRp 的系统表征无疑将有助于开发针对 RdRp 的抗病毒药物。在这里,我们的研究表明,RdRp 可以识别和利用核苷二磷酸作为底物,以大约三分之二的使用核苷三磷酸作为底物的效率合成 RNA。核苷二磷酸的掺入也是模板特异性的,具有高保真度。此外,RdRp 可以在使用二磷酸形式的莫努匹韦作为底物时将 β-d-N4-羟基胞苷掺入 RNA 中。这种掺入导致基因组突变和病毒死亡。还观察到二磷酸形式的莫努匹韦是 RdRp 的比三磷酸形式的莫努匹韦更好的底物,为药物设计提供了一种新策略。