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Furin: A Potential Therapeutic Target for COVID-19
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...
Autores principales: | , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7534598/ https://www.ncbi.nlm.nih.gov/pubmed/33043282 http://dx.doi.org/10.1016/j.isci.2020.101642 |
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author | Wu, Canrong Zheng, Mengzhu Yang, Yueying Gu, Xiaoxia Yang, Kaiyin Li, Mingxue Liu, Yang Zhang, Qingzhe Zhang, Peng Wang, Yali Wang, Qiqi Xu, Yang Zhou, Yirong Zhang, Yonghui Chen, Lixia Li, Hua |
author_facet | Wu, Canrong Zheng, Mengzhu Yang, Yueying Gu, Xiaoxia Yang, Kaiyin Li, Mingxue Liu, Yang Zhang, Qingzhe Zhang, Peng Wang, Yali Wang, Qiqi Xu, Yang Zhou, Yirong Zhang, Yonghui Chen, Lixia Li, Hua |
author_sort | Wu, Canrong |
collection | PubMed |
description | 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 IC(50) of 5.42 ± 0.11 μM, which might be used for the treatment of COVID-19. |
format | Online Article Text |
id | pubmed-7534598 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-75345982020-10-06 Furin: A Potential Therapeutic Target for COVID-19 Wu, Canrong Zheng, Mengzhu Yang, Yueying Gu, Xiaoxia Yang, Kaiyin Li, Mingxue Liu, Yang Zhang, Qingzhe Zhang, Peng Wang, Yali Wang, Qiqi Xu, Yang Zhou, Yirong Zhang, Yonghui Chen, Lixia Li, Hua iScience Article 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 IC(50) of 5.42 ± 0.11 μM, which might be used for the treatment of COVID-19. Elsevier 2020-10-05 /pmc/articles/PMC7534598/ /pubmed/33043282 http://dx.doi.org/10.1016/j.isci.2020.101642 Text en © 2020 The Author(s) http://creativecommons.org/licenses/by/4.0/ This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Wu, Canrong Zheng, Mengzhu Yang, Yueying Gu, Xiaoxia Yang, Kaiyin Li, Mingxue Liu, Yang Zhang, Qingzhe Zhang, Peng Wang, Yali Wang, Qiqi Xu, Yang Zhou, Yirong Zhang, Yonghui Chen, Lixia Li, Hua Furin: A Potential Therapeutic Target for COVID-19 |
title | Furin: A Potential Therapeutic Target for COVID-19 |
title_full | Furin: A Potential Therapeutic Target for COVID-19 |
title_fullStr | Furin: A Potential Therapeutic Target for COVID-19 |
title_full_unstemmed | Furin: A Potential Therapeutic Target for COVID-19 |
title_short | Furin: A Potential Therapeutic Target for COVID-19 |
title_sort | furin: a potential therapeutic target for covid-19 |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7534598/ https://www.ncbi.nlm.nih.gov/pubmed/33043282 http://dx.doi.org/10.1016/j.isci.2020.101642 |
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