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Adv Ther (Weinh). 2021 May;4(5):2000224. doi: 10.1002/adtp.202000224. Epub 2021 Feb 22.
2
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本文引用的文献

1
Nanoparticle Vaccines Based on the Receptor Binding Domain (RBD) and Heptad Repeat (HR) of SARS-CoV-2 Elicit Robust Protective Immune Responses.基于 SARS-CoV-2 受体结合域（RBD）和七肽重复（HR）的纳米颗粒疫苗可诱导出强大的保护性免疫应答。
Immunity. 2020 Dec 15;53(6):1315-1330.e9. doi: 10.1016/j.immuni.2020.11.015. Epub 2020 Nov 25.
2
SARS-CoV-2 spike-protein D614G mutation increases virion spike density and infectivity.SARS-CoV-2 刺突蛋白 D614G 突变增加了病毒粒子刺突密度和感染力。
Nat Commun. 2020 Nov 26;11(1):6013. doi: 10.1038/s41467-020-19808-4.
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Metallodrug ranitidine bismuth citrate suppresses SARS-CoV-2 replication and relieves virus-associated pneumonia in Syrian hamsters.金属药物雷尼替丁枸橼酸铋抑制 SARS-CoV-2 复制并缓解叙利亚仓鼠的病毒相关性肺炎。
Nat Microbiol. 2020 Nov;5(11):1439-1448. doi: 10.1038/s41564-020-00802-x. Epub 2020 Oct 7.
4
Salvianolic acid C potently inhibits SARS-CoV-2 infection by blocking the formation of six-helix bundle core of spike protein.丹酚酸C通过阻断刺突蛋白六螺旋束核心的形成来有效抑制新型冠状病毒2型（SARS-CoV-2）感染。
Signal Transduct Target Ther. 2020 Oct 6;5(1):220. doi: 10.1038/s41392-020-00325-1.
5
Recovered COVID-19 patients with recurrent viral RNA exhibit lower levels of anti-RBD antibodies.新冠病毒核糖核酸（RNA）复发的康复新冠患者体内抗受体结合域（RBD）抗体水平较低。
Cell Mol Immunol. 2020 Oct;17(10):1098-1100. doi: 10.1038/s41423-020-00528-0. Epub 2020 Sep 16.
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Entry Inhibitors: Efficient Means to Block Viral Infection.进入抑制剂：阻断病毒感染的有效手段。
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Structural and functional properties of SARS-CoV-2 spike protein: potential antivirus drug development for COVID-19.SARS-CoV-2 刺突蛋白的结构和功能特性：COVID-19 的潜在抗病毒药物研发。
Acta Pharmacol Sin. 2020 Sep;41(9):1141-1149. doi: 10.1038/s41401-020-0485-4. Epub 2020 Aug 3.
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Adaptation of SARS-CoV-2 in BALB/c mice for testing vaccine efficacy.用于测试疫苗效力的 SARS-CoV-2 在 BALB/c 小鼠中的适应性。
Science. 2020 Sep 25;369(6511):1603-1607. doi: 10.1126/science.abc4730. Epub 2020 Jul 30.
9
Lack of antibody-mediated cross-protection between SARS-CoV-2 and SARS-CoV infections.SARS-CoV-2 感染与 SARS-CoV 感染之间缺乏抗体介导的交叉保护作用。
EBioMedicine. 2020 Aug;58:102890. doi: 10.1016/j.ebiom.2020.102890. Epub 2020 Jul 21.
10
Structure-based design of prefusion-stabilized SARS-CoV-2 spikes.基于结构的 SARS-CoV-2 刺突蛋白预融合稳定构象设计。
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通过阻断严重急性呼吸综合征冠状病毒2（SARS-CoV-2）刺突蛋白介导的膜融合，将伊曲康唑和苯甲酸雌二醇用于新型冠状病毒肺炎的药物重新利用

Drug Repurposing of Itraconazole and Estradiol Benzoate against COVID-19 by Blocking SARS-CoV-2 Spike Protein-Mediated Membrane Fusion.

作者信息

Yang Chan, Pan Xiaoyan, Huang Yuan, Cheng Chen, Xu Xinfeng, Wu Yan, Xu Yunxia, Shang Weijuan, Niu Xiaoge, Wan Yihong, Li Zhaofeng, Zhang Rong, Liu Shuwen, Xiao Gengfu, Xu Wei

机构信息

School of Pharmaceutical Sciences Southern Medical University Guangzhou 510515 China.

Chinese Academy of Sciences Wuhan 430071 China.

出版信息

Adv Ther (Weinh). 2021 May;4(5):2000224. doi: 10.1002/adtp.202000224. Epub 2021 Feb 22.

DOI:10.1002/adtp.202000224
PMID:33786369
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7994988/
Abstract

SARS-CoV-2 caused the emerging epidemic of coronavirus disease in 2019 (COVID-19). To date, there are more than 82.9 million confirmed cases worldwide, there is no clinically effective drug against SARS-CoV-2 infection. The conserved properties of the membrane fusion domain of the spike (S) protein across SARS-CoV-2 make it a promising target to develop pan-CoV therapeutics. Herein, two clinically approved drugs, Itraconazole (ITZ) and Estradiol benzoate (EB), are found to inhibit viral entry by targeting the six-helix (6-HB) fusion core of SARS-CoV-2 S protein. Further studies shed light on the mechanism that ITZ and EB can interact with the heptad repeat 1 (HR1) region of the spike protein, to present anti-SARS-CoV-2 infections in vitro, indicating they are novel potential therapeutic remedies for COVID-19 treatment. Furthermore, ITZ shows broad-spectrum activity targeting 6-HB in the S2 subunit of SARS-CoV and MERS-CoV S protein, inspiring that ITZ have the potential for development as a pan-coronavirus fusion inhibitor.

摘要

严重急性呼吸综合征冠状病毒2（SARS-CoV-2）引发了2019年新型冠状病毒肺炎（COVID-19）疫情。截至目前，全球确诊病例超过8290万例，尚无针对SARS-CoV-2感染的临床有效药物。SARS-CoV-2刺突（S）蛋白膜融合结构域的保守特性使其成为开发泛冠状病毒疗法的一个有前景的靶点。在此，发现两种临床批准药物伊曲康唑（ITZ）和苯甲酸雌二醇（EB）通过靶向SARS-CoV-2 S蛋白的六螺旋（6-HB）融合核心来抑制病毒进入。进一步研究揭示了ITZ和EB可与刺突蛋白的七肽重复序列1（HR1）区域相互作用的机制，从而在体外呈现抗SARS-CoV-2感染作用，表明它们是用于COVID-19治疗的新型潜在治疗药物。此外，ITZ对SARS-CoV的S2亚基和中东呼吸综合征冠状病毒（MERS-CoV）S蛋白中的6-HB具有广谱靶向活性，这表明ITZ有潜力开发成为一种泛冠状病毒融合抑制剂。