Reuschl Ann-Kathrin, Thorne Lucy G, Zuliani-Alvarez Lorena, Bouhaddou Mehdi, Obernier Kirsten, Hiatt Joseph, Soucheray Margaret, Turner Jane, Fabius Jacqueline M, Nguyen Gina T, Swaney Danielle L, Rosales Romel, White Kris M, Avilés Pablo, Kirby Ilsa T, Melnyk James E, Shi Ying, Zhang Ziyang, Shokat Kevan M, García-Sastre Adolfo, Jolly Clare, Towers Gregory J, Krogan Nevan J
Division of Infection and Immunity, University College London, London, WC1E 6BT, United Kingdom.
Quantitative Biosciences Institute (QBI) Coronavirus Research Group (QCRG), San Francisco, CA 94158, USA.
bioRxiv. 2021 Feb 4:2021.01.24.427991. doi: 10.1101/2021.01.24.427991.
Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has resulted in millions of deaths worldwide and massive societal and economic burden. Recently, a new variant of SARS-CoV-2, known as B.1.1.7, was first detected in the United Kingdom and is spreading in several other countries, heightening public health concern and raising questions as to the resulting effectiveness of vaccines and therapeutic interventions. We and others previously identified host-directed therapies with antiviral efficacy against SARS-CoV-2 infection. Less prone to the development of therapy resistance, host-directed drugs represent promising therapeutic options to combat emerging viral variants as host genes possess a lower propensity to mutate compared to viral genes. Here, in the first study of the full-length B.1.1.7 variant virus , we find two host-directed drugs, plitidepsin (aplidin; inhibits translation elongation factor eEF1A) and ralimetinib (inhibits p38 MAP kinase cascade), as well as remdesivir, to possess similar antiviral activity against both the early-lineage SARS-CoV-2 and the B.1.1.7 variant, evaluated in both human gastrointestinal and lung epithelial cell lines. We find that plitidepsin is over an order of magnitude more potent than remdesivir against both viruses. These results highlight the importance of continued development of host-directed therapeutics to combat current and future coronavirus variant outbreaks.
2019年冠状病毒病(COVID-19)由严重急性呼吸综合征冠状病毒2(SARS-CoV-2)引起,已在全球导致数百万人死亡,并造成了巨大的社会和经济负担。最近,一种名为B.1.1.7的新型SARS-CoV-2变种首先在英国被检测到,并在其他几个国家传播,这加剧了公众对健康的担忧,并引发了关于疫苗和治疗干预措施有效性的问题。我们和其他人之前已经确定了对SARS-CoV-2感染具有抗病毒功效的宿主导向疗法。宿主导向药物不太容易产生治疗抗性,由于宿主基因与病毒基因相比具有较低的突变倾向,因此是对抗新出现的病毒变种的有前景的治疗选择。在此,在对全长B.1.1.7变种病毒的首次研究中,我们发现两种宿主导向药物,plitidepsin(阿普立定;抑制翻译延伸因子eEF1A)和ralimetinib(抑制p38丝裂原活化蛋白激酶级联反应),以及瑞德西韦,在人胃肠道和肺上皮细胞系中对早期谱系SARS-CoV-2和B.1.1.7变种均具有相似的抗病毒活性。我们发现plitidepsin对这两种病毒的效力比瑞德西韦高出一个数量级以上。这些结果凸显了持续开发宿主导向疗法以对抗当前和未来冠状病毒变种爆发的重要性。