A drug repurposing screen identifies hepatitis C antivirals as inhibitors of the SARS-CoV2 main protease

Effective SARS-CoV-2 antiviral drugs are desperately needed. The SARS-CoV-2 main protease (Mpro) appears as an attractive target for drug development. We show that the existing pharmacopeia contains many drugs with potential for therapeutic repurposing as selective and potent inhibitors of SARS-CoV-...

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Veröffentlicht in:	PloS one 2021-02, Vol.16 (2), p.e0245962-e0245962, Article 0245962
Hauptverfasser:	Baker, Jeremy D., Uhrich, Rikki L., Kraemer, Gerald C., Love, Jason E., Kraemer, Brian C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiviral agents Antiviral Agents - pharmacology Antiviral Agents - therapeutic use Antiviral drugs Biological Assay Biology and Life Sciences Clinical trials Computer programs Coronaviridae Coronaviruses COVID-19 Drafting software Drug development Drug dosages Drug Evaluation, Preclinical Drug Repositioning Drug screening Drug therapy Editing Education Fluorescence Genomes Geriatrics Gerontology Global health Health care Hepacivirus - drug effects Hepatitis Hepatitis C Hepatitis C - drug therapy Hepatitis C virus High-Throughput Screening Assays Humans Infections Medicine Medicine and health sciences Methodology Multidisciplinary Sciences Pandemics Pathology Pharmacodynamics Pharmacokinetics Pharmacology Pharmacology, Experimental Protease inhibitors Protease Inhibitors - pharmacology Proteins Psychiatry Public health Reproducibility of Results Research and Analysis Methods Respiratory diseases Reviews RNA viruses SARS-CoV-2 - drug effects Science & Technology Science & Technology - Other Topics Severe acute respiratory syndrome Severe acute respiratory syndrome coronavirus 2 Software Toxicity Veterans Viral diseases Viruses
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Beschreibung
Zusammenfassung:	Effective SARS-CoV-2 antiviral drugs are desperately needed. The SARS-CoV-2 main protease (Mpro) appears as an attractive target for drug development. We show that the existing pharmacopeia contains many drugs with potential for therapeutic repurposing as selective and potent inhibitors of SARS-CoV-2 Mpro. We screened a collection of similar to 6,070 drugs with a previous history of use in humans for compounds that inhibit the activity of Mpro in vitro and found similar to 50 compounds with activity against Mpro. Subsequent dose validation studies demonstrated 8 dose responsive hits with an IC50
ISSN:	1932-6203 1932-6203
DOI:	10.1371/journal.pone.0245962