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Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors

Since the outbreak of SARS‐CoV‐2 in December 2019 millions of infections have been reported globally. The viral chymotrypsin‐like main protease (M(Pro)) exhibits a crucial role in viral replication and represents a relevant target for antiviral drug development. In order to screen potential M(Pro) i...

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Autores principales: Sondag, Daan, Merx, Jona, Rossing, Emiel, Boltje, Thomas J., Löwik, Dennis W. P. M., Nelissen, Frank H. T., van Geffen, Mark, van 't Veer, Cornelis, van Heerde, Waander L., Rutjes, Floris P. J. T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9401586/
https://www.ncbi.nlm.nih.gov/pubmed/35649961
http://dx.doi.org/10.1002/cbic.202200190
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author Sondag, Daan
Merx, Jona
Rossing, Emiel
Boltje, Thomas J.
Löwik, Dennis W. P. M.
Nelissen, Frank H. T.
van Geffen, Mark
van 't Veer, Cornelis
van Heerde, Waander L.
Rutjes, Floris P. J. T.
author_facet Sondag, Daan
Merx, Jona
Rossing, Emiel
Boltje, Thomas J.
Löwik, Dennis W. P. M.
Nelissen, Frank H. T.
van Geffen, Mark
van 't Veer, Cornelis
van Heerde, Waander L.
Rutjes, Floris P. J. T.
author_sort Sondag, Daan
collection PubMed
description Since the outbreak of SARS‐CoV‐2 in December 2019 millions of infections have been reported globally. The viral chymotrypsin‐like main protease (M(Pro)) exhibits a crucial role in viral replication and represents a relevant target for antiviral drug development. In order to screen potential M(Pro) inhibitors we developed a luminescent assay using a peptide based probe containing a cleavage site specific for M(Pro). This assay was validated showing IC(50) values similar to those reported in the literature for known M(Pro) inhibitors and can be used to screen new inhibitors.
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spelling pubmed-94015862022-08-26 Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors Sondag, Daan Merx, Jona Rossing, Emiel Boltje, Thomas J. Löwik, Dennis W. P. M. Nelissen, Frank H. T. van Geffen, Mark van 't Veer, Cornelis van Heerde, Waander L. Rutjes, Floris P. J. T. Chembiochem Research Articles Since the outbreak of SARS‐CoV‐2 in December 2019 millions of infections have been reported globally. The viral chymotrypsin‐like main protease (M(Pro)) exhibits a crucial role in viral replication and represents a relevant target for antiviral drug development. In order to screen potential M(Pro) inhibitors we developed a luminescent assay using a peptide based probe containing a cleavage site specific for M(Pro). This assay was validated showing IC(50) values similar to those reported in the literature for known M(Pro) inhibitors and can be used to screen new inhibitors. John Wiley and Sons Inc. 2022-06-14 2022-08-03 /pmc/articles/PMC9401586/ /pubmed/35649961 http://dx.doi.org/10.1002/cbic.202200190 Text en © 2022 The Authors. ChemBioChem published by Wiley-VCH GmbH https://creativecommons.org/licenses/by/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Articles
Sondag, Daan
Merx, Jona
Rossing, Emiel
Boltje, Thomas J.
Löwik, Dennis W. P. M.
Nelissen, Frank H. T.
van Geffen, Mark
van 't Veer, Cornelis
van Heerde, Waander L.
Rutjes, Floris P. J. T.
Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors
title Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors
title_full Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors
title_fullStr Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors
title_full_unstemmed Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors
title_short Luminescent Assay for the Screening of SARS‐CoV‐2 M(Pro) Inhibitors
title_sort luminescent assay for the screening of sars‐cov‐2 m(pro) inhibitors
topic Research Articles
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9401586/
https://www.ncbi.nlm.nih.gov/pubmed/35649961
http://dx.doi.org/10.1002/cbic.202200190
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