Identification of SARS-CoV-2 entry inhibitors among already approved drugs

doi:10.1038/s41401-020-00556-6

	Identification of SARS-CoV-2 entry inhibitors among already approved drugs
	Yang, Li 1; Pei, Rong-juan 2; Li, Heng 1,3; Ma, Xin-na 4; Zhou, Yu 1; Zhu, Feng-hua 1; He, Pei-lan 1; Tang, Wei 1; Zhang, Ye-cheng 2; Xiong, Jin 2
刊名	ACTA PHARMACOLOGICA SINICA
	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.
资助项目	National Key Research and Development Program of China[2018YFC1200604]
WOS关键词	RESPIRATORY SYNDROME CORONAVIRUS ; TRIMEPRAZINE TARTRATE ; VIRUS ; REPLICATION ; PNEUMONIA ; INFECTION ; COMPOUND ; ABL
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	NATURE PUBLISHING GROUP
WOS记录号	WOS:000584865400002
内容类型	期刊论文
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.Chinese Acad Sci, Ctr Biosafety Megasci, Wuhan Inst Virol, Key Lab Special Pathogens & Biosafety, Wuhan 430071, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, 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.