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

  
@article{APS10376,
	author = {Li Yang and Rong-juan Pei and Heng Li and Xin-na Ma and Yu Zhou and Feng-hua Zhu and Pei-lan He and Wei Tang and Ye-cheng Zhang and Jin Xiong and Shu-qi Xiao and Xian-kun Tong and Bo Zhang and Jian-ping Zuo},
	title = {Identification of SARS-CoV-2 entry inhibitors among already approved drugs},
	journal = {Acta Pharmacologica Sinica},
	volume = {42},
	number = {8},
	year = {2021},
	keywords = {},
	abstract = {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 μM). Our work suggests that these 7 drugs could enter into further in vivo studies and clinical investigations for COVID-19 treatment.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/10376}
}