Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2

There is an urgent need for antiviral agents that treat severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. We screened a library of 1900 clinically safe drugs against OC43, a human beta coronavirus that causes the common cold, and evaluated the top hits against SARS-CoV-2. Twent...

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Veröffentlicht in:	Science (American Association for the Advancement of Science) 2021-08, Vol.373 (6557), p.931-936
Hauptverfasser:	Drayman, Nir, DeMarco, Jennifer K, Jones, Krysten A, Azizi, Saara-Anne, Froggatt, Heather M, Tan, Kemin, Maltseva, Natalia Ivanovna, Chen, Siquan, Nicolaescu, Vlad, Dvorkin, Steve, Furlong, Kevin, Kathayat, Rahul S, Firpo, Mason R, Mastrodomenico, Vincent, Bruce, Emily A, Schmidt, Madaline M, Jedrzejczak, Robert, Muñoz-Alía, Miguel Á, Schuster, Brooke, Nair, Vishnu, Han, Kyu-Yeon, O'Brien, Amornrat, Tomatsidou, Anastasia, Meyer, Bjoern, Vignuzzi, Marco, Missiakas, Dominique, Botten, Jason W, Brooke, Christopher B, Lee, Hyun, Baker, Susan C, Mounce, Bryan C, Heaton, Nicholas S, Severson, William E, Palmer, Kenneth E, Dickinson, Bryan C, Joachimiak, Andrzej, Randall, Glenn, Tay, Savaş
Format:	Artikel
Sprache:	eng
Schlagworte:	A549 Cells Animals Antiviral agents Antiviral Agents - chemistry Antiviral Agents - metabolism Antiviral Agents - pharmacology Antiviral Agents - therapeutic use Benzamides Bioavailability Catalytic Domain Common cold Coronavirus 3C Proteases - antagonists & inhibitors Coronavirus 3C Proteases - chemistry Coronavirus 3C Proteases - metabolism Coronavirus OC43, Human - drug effects Coronavirus OC43, Human - physiology Coronaviruses COVID-19 COVID-19 - virology COVID-19 Drug Treatment Crystallography Cysteine Proteinase Inhibitors - chemistry Cysteine Proteinase Inhibitors - metabolism Cysteine Proteinase Inhibitors - pharmacology Drug screening Drugs Enzyme inhibitors Genomes HEK293 Cells Humans Inhibitory Concentration 50 Kinases Libraries Lungs Mice Mice, Transgenic Microbial Sensitivity Tests Narcotics Piperidines Polyproteins Protease Protein-tyrosine kinase Proteinase Pyridines Replication Respiratory diseases SARS-CoV-2 - drug effects SARS-CoV-2 - enzymology SARS-CoV-2 - physiology Severe acute respiratory syndrome Severe acute respiratory syndrome coronavirus 2 Therapeutic targets Thiazoles - chemistry Thiazoles - metabolism Thiazoles - pharmacology Thiazoles - therapeutic use Tyrosine Viral diseases Viral Load - drug effects Virus Replication - drug effects Viruses X-ray crystallography
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