Targeting the Main Protease of SARS‐CoV‐2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors

The main protease of SARS‐CoV‐2 (Mpro), the causative agent of COVID‐19, constitutes a significant drug target. A new fluorogenic substrate was kinetically compared to an internally quenched fluorescent peptide and shown to be ideally suitable for high throughput screening with recombinantly express...

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Veröffentlicht in:	Angewandte Chemie International Edition 2021-04, Vol.60 (18), p.10423-10429
Hauptverfasser:	Breidenbach, Julian, Lemke, Carina, Pillaiyar, Thanigaimalai, Schäkel, Laura, Al Hamwi, Ghazl, Diett, Miriam, Gedschold, Robin, Geiger, Nina, Lopez, Vittoria, Mirza, Salahuddin, Namasivayam, Vigneshwaran, Schiedel, Anke C., Sylvester, Katharina, Thimm, Dominik, Vielmuth, Christin, Phuong Vu, Lan, Zyulina, Maria, Bodem, Jochen, Gütschow, Michael, Müller, Christa E.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiviral Agents - chemistry Antiviral Agents - pharmacology azapeptide nitriles Cathepsin L Coronavirus 3C Proteases - antagonists & inhibitors Coronavirus 3C Proteases - metabolism COVID-19 COVID-19 - metabolism COVID-19 - virology COVID-19 Drug Treatment Drug Design Drug development Drug Discovery Esters Fluorescence fluorogenic substrates HEK293 Cells High-throughput screening High-Throughput Screening Assays Humans Indoles Molecular Docking Simulation Nitriles - chemistry Nitriles - pharmacology Peptides Protease Protease inhibitors Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Proteinase inhibitors Pyridines - chemistry Pyridines - pharmacology pyridinyl 1H-indole-carboxylates SARS-CoV-2 - drug effects SARS-CoV-2 - enzymology SARS-CoV-2 - physiology SARS-CoV-2 main protease Screening Severe acute respiratory syndrome Severe acute respiratory syndrome coronavirus 2 Substrates Therapeutic targets Virus Internalization - drug effects
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