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通过基于对接的虚拟筛选和药代动力学方法,针对负责包膜形成和病毒体组装的蛋白质,鉴定针对 SARS-CoV-2 的潜在抑制剂。

Identification of potential inhibitors against SARS-CoV-2 by targeting proteins responsible for envelope formation and virion assembly using docking based virtual screening, and pharmacokinetics approaches.

机构信息

Department of Microbiology, Assam University, Silchar 788011, Assam, India.

CAS in Crystallography and Biophysics, Guindy Campus, University of Madras, Chennai 600025, India.

出版信息

Infect Genet Evol. 2020 Oct;84:104451. doi: 10.1016/j.meegid.2020.104451. Epub 2020 Jul 5.

DOI:10.1016/j.meegid.2020.104451
PMID:32640381
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7335633/
Abstract

WHO has declared the outbreak of COVID-19 as a public health emergency of international concern. The ever-growing new cases have called for an urgent emergency for specific anti-COVID-19 drugs. Three structural proteins (Membrane, Envelope and Nucleocapsid protein) play an essential role in the assembly and formation of the infectious virion particles. Thus, the present study was designed to identify potential drug candidates from the unique collection of 548 anti-viral compounds (natural and synthetic anti-viral), which target SARS-CoV-2 structural proteins. High-end molecular docking analysis was performed to characterize the binding affinity of the selected drugs-the ligand, with the SARS-CoV-2 structural proteins, while high-level Simulation studies analyzed the stability of drug-protein interactions. The present study identified rutin, a bioflavonoid and the antibiotic, doxycycline, as the most potent inhibitor of SARS-CoV-2 envelope protein. Caffeic acid and ferulic acid were found to inhibit SARS-CoV-2 membrane protein while the anti-viral agent's simeprevir and grazoprevir showed a high binding affinity for nucleocapsid protein. All these compounds not only showed excellent pharmacokinetic properties, absorption, metabolism, minimal toxicity and bioavailability but were also remain stabilized at the active site of proteins during the MD simulation. Thus, the identified lead compounds may act as potential molecules for the development of effective drugs against SARS-CoV-2 by inhibiting the envelope formation, virion assembly and viral pathogenesis.

摘要

世界卫生组织已宣布 COVID-19 疫情为国际关注的突发公共卫生事件。不断增加的新病例呼吁紧急研发特定的抗 COVID-19 药物。三种结构蛋白(膜、包膜和核衣壳蛋白)在感染性病毒粒子的组装和形成中起着至关重要的作用。因此,本研究旨在从针对 SARS-CoV-2 结构蛋白的独特的 548 种抗病毒化合物(天然和合成抗病毒化合物)中鉴定出潜在的药物候选物。进行了高端分子对接分析,以描述所选药物-配体与 SARS-CoV-2 结构蛋白的结合亲和力,而高水平的模拟研究分析了药物-蛋白相互作用的稳定性。本研究鉴定出芦丁,一种生物类黄酮和抗生素多西环素,是 SARS-CoV-2 包膜蛋白的最有效抑制剂。发现咖啡酸和阿魏酸可抑制 SARS-CoV-2 膜蛋白,而抗病毒药物西米普雷韦和格拉瓦瑞韦对核衣壳蛋白具有高结合亲和力。所有这些化合物不仅表现出优异的药代动力学特性、吸收、代谢、最小毒性和生物利用度,而且在 MD 模拟过程中也保持在蛋白质的活性部位稳定。因此,所鉴定的先导化合物可能通过抑制包膜形成、病毒粒子组装和病毒发病机制,成为针对 SARS-CoV-2 开发有效药物的潜在分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/27ea6406dd2e/gr6_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/3b73582d174d/gr1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/0cb013752888/gr2_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/048d4d775b81/gr3_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/57f78ac18f45/gr4_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/55ac0b07cd4e/gr5_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/27ea6406dd2e/gr6_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/3b73582d174d/gr1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/0cb013752888/gr2_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/048d4d775b81/gr3_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/57f78ac18f45/gr4_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/55ac0b07cd4e/gr5_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/670e/7335633/27ea6406dd2e/gr6_lrg.jpg

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