Furin: A Potential Therapeutic Target for COVID-19

iScience

卷:23

Yali Wang¹  Xiaoxia Gu¹  Yirong Zhou¹  Lixia Chen¹  Qingzhe Zhang¹  Canrong Wu²  Mengzhu Zheng²  Qiqi Wang²  Kaiyin Yang²  Mingxue Li²  Yang Liu³  Peng Zhang³  Yonghui Zhang³  Hua Li³  Yang Xu³  Yueying Yang³ 

[1] Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China;

[2] Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji-Rongcheng Center for Biomedicine, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China;

[3] Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design &

关键词: Computational Molecular Modelling;    Disease;    Drugs;    Virology;   

DOI  :  

来源: DOAJ

【 摘 要 】

Summary: COVID-19 broke out in the end of December 2019 and is still spreading rapidly, which has been listed as an international concerning public health emergency. We found that the Spike protein of SARS-CoV-2 contains a furin cleavage site, which did not exist in any other betacoronavirus subtype B. Based on a series of analysis, we speculate that the presence of a redundant furin cut site in its Spike protein is responsible for SARS-CoV-2's stronger infectious nature than other coronaviruses, which leads to higher membrane fusion efficiency. Subsequently, a library of 4,000 compounds including approved drugs and natural products was screened against furin through structure-based virtual screening and then assayed for their inhibitory effects on furin activity. Among them, an anti-parasitic drug, diminazene, showed the highest inhibition effects on furin with an IC50 of 5.42 ± 0.11 μM, which might be used for the treatment of COVID-19.

【 授权许可】

Unknown