Identification of SARS-CoV-2 entry inhibitors among already approved drugs
文献类型：期刊论文
| 作者 | Yang, Li1; Pei, Rong-juan3; Li, Heng1,2; Ma, Xin-na4; Zhou, Yu1 ; Zhu, Feng-hua1; He, Pei-lan1; Tang, Wei1; Zhang, Ye-cheng3; Xiong, Jin3
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2020-10-28 |
| 页码 | 7 |
| 关键词 | COVID-19 SARS-CoV-2 virus entry inhibitors high throughput screening assay approved drug library histamine receptor antagonists clemastine |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/s41401-020-00556-6 |
| 通讯作者 | Tong, Xian-kun(xktong@simm.ac.cn) ; Zhang, Bo(zhangbo@wh.iov.cn) ; Zuo, Jian-ping(jpzuo@simm.ac.cn) |
| 英文摘要 | To discover effective drugs for COVID-19 treatment amongst already clinically approved drugs, we developed a high throughput screening assay for SARS-CoV-2 virus entry inhibitors using SARS2-S pseudotyped virus. An approved drug library of 1800 small molecular drugs was screened for SARS2 entry inhibitors and 15 active drugs were identified as specific SARS2-S pseudovirus entry inhibitors. Antiviral tests using native SARS-CoV-2 virus in Vero E6 cells confirmed that 7 of these drugs (clemastine, amiodarone, trimeprazine, bosutinib, toremifene, flupenthixol, and azelastine) significantly inhibited SARS2 replication, reducing supernatant viral RNA load with a promising level of activity. Three of the drugs were classified as histamine receptor antagonists with clemastine showing the strongest anti-SARS2 activity (EC50 = 0.95 +/- 0.83 mu M). Our work suggests that these 7 drugs could enter into further in vivo studies and clinical investigations for COVID-19 treatment. |
| WOS关键词 | RESPIRATORY SYNDROME CORONAVIRUS ; TRIMEPRAZINE TARTRATE ; VIRUS ; REPLICATION ; PNEUMONIA ; INFECTION ; COMPOUND ; ABL |
| 资助项目 | National Key Research and Development Program of China[2018YFC1200604] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000584865400002 |
| 出版者 | NATURE PUBLISHING GROUP |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/292527]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Tong, Xian-kun; Zhang, Bo; Zuo, Jian-ping |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Lab Immunopharmacol, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Ctr Biosafety Megasci, Wuhan Inst Virol, Key Lab Special Pathogens & Biosafety, Wuhan 430071, Peoples R China 4.Shanghai Univ Tradit Chinese Med, Lab Immunol & Virol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Li,Pei, Rong-juan,Li, Heng,et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs[J]. ACTA PHARMACOLOGICA SINICA,2020:7. |
| APA | Yang, Li.,Pei, Rong-juan.,Li, Heng.,Ma, Xin-na.,Zhou, Yu.,...&Zuo, Jian-ping.(2020).Identification of SARS-CoV-2 entry inhibitors among already approved drugs.ACTA PHARMACOLOGICA SINICA,7. |
| MLA | Yang, Li,et al."Identification of SARS-CoV-2 entry inhibitors among already approved drugs".ACTA PHARMACOLOGICA SINICA (2020):7. |
入库方式： OAI收割
来源：上海药物研究所
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