Department of Microbiology and Immunology, Department of Paediatrics, IWK Health Center, Canadian Centre for Vaccinology (CCfV), Faculty of Medicine, Dalhousie University, Halifax, Canada.
European Virus Bioinformatics Center, Jena, Germany.
J Cell Biochem. 2023 May;124(5):701-715. doi: 10.1002/jcb.30397. Epub 2023 Mar 22.
Mpox (formerly Monkeypox), a zoonotic illness caused by the Mpox virus, belongs to the Orthopoxvirus genus in the family Poxviridae. To design and develop effective antiviral therapeutics against DNA viruses, the DNA-dependent RNA polymerase (DdRp) of poxviruses has emerged as a promising drug target. In the present study, we modeled the three-dimensional (3D) structure of DdRp using a template-based homology approach. After modeling, virtual screening was performed to probe the molecular interactions between 1755 Food and Drug Administration-approved small molecule drugs (≤500 molecular weight) and the DdRp of Mpox. Based on the binding affinity and molecular interaction patterns, five drugs, lumacaftor (-11.7 kcal/mol), conivaptan (-11.7 kcal/mol), betulinic acid (-11.6 kcal/mol), fluspirilene (-11.3 kcal/mol), and imatinib (-11.2 kcal/mol), have been ranked as the top drug compounds interacting with Mpox DdRp. Complexes of these shortlisted drugs with DdRp were further evaluated using state-of-the-art all-atoms molecular dynamics (MD) simulations on 200 nanoseconds followed by principal component analysis (PCA). MD simulations and PCA results revealed highly stable interactions of these small drugs with DdRp. After due validation in wet-lab using available in vitro and in vivo experiments, these repurposed drugs can be further utilized for the treatment of contagious Mpox virus. The outcome of this study may establish a solid foundation to screen repurposed and natural compounds as potential antiviral therapeutics against different highly pathogenic viruses.
猴痘(以前称为猴痘)是一种由猴痘病毒引起的人畜共患病,属于正痘病毒科痘病毒科的正痘病毒属。为了设计和开发针对 DNA 病毒的有效抗病毒治疗方法,痘病毒的 DNA 依赖性 RNA 聚合酶(DdRp)已成为有前途的药物靶点。在本研究中,我们使用基于模板的同源建模方法对 DdRp 的三维(3D)结构进行建模。建模后,进行虚拟筛选以探测 1755 种美国食品和药物管理局批准的小分子药物(≤500 分子量)与猴痘 DdRp 之间的分子相互作用。根据结合亲和力和分子相互作用模式,五种药物(lumacaftor(-11.7 kcal/mol)、conivaptan(-11.7 kcal/mol)、betulinic acid(-11.6 kcal/mol)、fluspirilene(-11.3 kcal/mol)和 imatinib(-11.2 kcal/mol))被评为与猴痘 DdRp 相互作用的顶级药物化合物。使用最先进的全原子分子动力学(MD)模拟对这些入围药物与 DdRp 的复合物进行进一步评估,模拟时间为 200 纳秒,随后进行主成分分析(PCA)。MD 模拟和 PCA 结果表明,这些小分子药物与 DdRp 之间存在高度稳定的相互作用。在使用现有体外和体内实验进行适当的湿实验室验证后,这些重新利用的药物可以进一步用于治疗传染性猴痘病毒。这项研究的结果可能为筛选重新利用和天然化合物作为针对不同高致病性病毒的潜在抗病毒治疗方法奠定坚实的基础。