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Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors |
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| Authors: | Daan Sondag Jona Merx Emiel Rossing Thomas J Boltje Dennis W P M Löwik Frank H T Nelissen Mark van Geffen Cornelis van 't Veer Waander L van Heerde Floris P J T Rutjes |
| Affiliation: | 1. Institute for Molecules and Materials, Radboud University, 6525 AJ Nijmegen, The Netherlands
These authors contributed equally to this work.;2. Institute for Molecules and Materials, Radboud University, 6525 AJ Nijmegen, The Netherlands;3. Enzyre BV, Novio Tech Campus Transistorweg 5-i, 6534 AT Nijmegen, The Netherlands;4. Enzyre BV, Novio Tech Campus Transistorweg 5-i, 6534 AT Nijmegen, The Netherlands Department of Haematology, Radboud University Medical Centre, Nijmegen, The Netherlands) and Haemophilia Treatment Centre Nijmegen Eindhoven Maastricht (HTC-NEM) (The Netherlands |
| Abstract: | Since the outbreak of SARS-CoV-2 in December 2019 millions of infections have been reported globally. The viral chymotrypsin-like main protease (MPro) exhibits a crucial role in viral replication and represents a relevant target for antiviral drug development. In order to screen potential MPro inhibitors we developed a luminescent assay using a peptide based probe containing a cleavage site specific for MPro. This assay was validated showing IC50 values similar to those reported in the literature for known MPro inhibitors and can be used to screen new inhibitors. |
| Keywords: | enzymes inhibitors imaging agents luminescence |