Identifying SARS-CoV-2 Entry Inhibitors through Drug Repurposing Screens of SARS-S and MERS-S Pseudotyped Particles,ACS Pharmacology & Translational Science

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Identifying SARS-CoV-2 Entry Inhibitors through Drug Repurposing Screens of SARS-S and MERS-S Pseudotyped Particles
ACS Pharmacology & Translational Science ( IF 4.9 ) Pub Date : 2020-10-19 , DOI: 10.1021/acsptsci.0c00112
Catherine Z Chen ₁ , Miao Xu ₁ , Manisha Pradhan ₁ , Kirill Gorshkov ₁ , Jennifer D Petersen ₂ , Marco R Straus ₃ , Wei Zhu ₁ , Paul Shinn ₁ , Hui Guo ₁ , Min Shen ₁ , Carleen Klumpp-Thomas ₁ , Samuel G Michael ₁ , Joshua Zimmerberg ₂ , Wei Zheng ₁ , Gary R Whittaker ₃

Affiliation

While vaccine development will hopefully quell the global pandemic of COVID-19 caused by SARS-CoV-2, small molecule drugs that can effectively control SARS-CoV-2 infection are urgently needed. Here, inhibitors of spike (S) mediated cell entry were identified in a high throughput screen of an approved drugs library with SARS-S and MERS-S pseudotyped particle entry assays. We discovered six compounds (cepharanthine, abemaciclib, osimertinib, trimipramine, colforsin, and ingenol) to be broad spectrum inhibitors for spike-mediated entry. This work could contribute to the development of effective treatments against the initial stage of viral infection and provide mechanistic information that might aid the design of new drug combinations for clinical trials for COVID-19 patients.

中文翻译：

通过 SARS-S 和 MERS-S 假型颗粒的药物再利用筛选鉴定 SARS-CoV-2 进入抑制剂

虽然疫苗的开发有望平息由 SARS-CoV-2 引起的 COVID-19 全球大流行，但迫切需要能够有效控制 SARS-CoV-2 感染的小分子药物。在这里，通过 SARS-S 和 MERS-S 假型颗粒进入测定，在已批准药物库的高通量筛选中鉴定出尖峰 (S) 介导的细胞进入抑制剂。我们发现六种化合物（千金藤素、abemaciclib、奥西替尼、曲米帕明、colforsin 和巨大戟二萜醇）是尖峰介导进入的广谱抑制剂。这项工作可能有助于开发针对病毒感染初始阶段的有效治疗方法，并提供可能有助于设计用于 COVID-19 患者临床试验的新药物组合的机制信息。

更新日期：2020-12-12

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