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Potential inhibitors for blocking the interaction of the coronavirus SARS-CoV-2 spike protein and its host cell receptor ACE2

By Changzhi Li, Hongjuan Zhou, Lingling Guo, Dehuan Xie, Huiping He, Hong Zhang, Yixiu Liu, Lixia Peng, Lisheng Zheng, Wenhua Lu, Yan Mei, Zhijie Liu, Jie Huang, Mingdian Wang, Ditian Shu, Liuyan Ding, Yanhong Lang, Feifei Luo, Jing Wang, Bijun Huang, Peng Huang, Song Gao, Jindong Chen, Chao-Nan Qian

Posted 15 Dec 2021
bioRxiv DOI: 10.1101/2021.12.14.472545

The outbreak of SARS-CoV-2 continues to pose a serious threat to human health and social and economic stability. In this study, we established an anti-coronavirus drug screening platform based on the Homogeneous Time Resolved Fluorescence (HTRF) technology and the interaction between the coronavirus S protein and its host receptor ACE2. This platform is a rapid, sensitive, specific, and high throughput system. With this platform, we screened two compound libraries of 2,864 molecules and identified three potential anti-coronavirus compounds: tannic acid (TA), TS-1276 (anthraquinone), and TS-984 (9-Methoxycanthin-6-one). Our in vitro validation experiments indicated that TS-984 strongly inhibits the interaction of the coronavirus S-protein and the human cell ACE2 receptor. This data suggests that TS-984 is a potent blocker of the interaction between the S-protein and ACE2, which might have the potential to be developed into an effective anti-coronavirus drug.

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