Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors

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

doi:https://doi.org/10.1002/cbic.202200190

Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors

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

Research output: Contribution to journal › Article › Academic › peer-review

4 Citations (Scopus)

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.

Original language	English
Article number	e202200190
Journal	Chembiochem
Volume	23
Issue number	15
Early online date	2022
DOIs	https://doi.org/10.1002/cbic.202200190
Publication status	Published - 3 Aug 2022

Keywords

enzymes
imaging agents
inhibitors
luminescence

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https://doi.org/10.1002/cbic.202200190

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title = "Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors",

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, imaging agents, inhibitors, luminescence",

author = "Daan Sondag and Jona Merx and Emiel Rossing and Boltje, {Thomas J.} and L{\"o}wik, {Dennis W. P. M.} and Nelissen, {Frank H. T.} and {van Geffen}, Mark and {van 't Veer}, Cornelis and {van Heerde}, {Waander L.} and Rutjes, {Floris P. J. T.}",

note = "Funding Information: This work was supported by LIFT grant 741.018.406 from the Dutch Research Council (NWO) awarded to F.P.J.T.R., T.J.B. and W.L.v.H. Publisher Copyright: {\textcopyright} 2022 The Authors. ChemBioChem published by Wiley-VCH GmbH.",

year = "2022",

month = aug,

day = "3",

doi = "https://doi.org/10.1002/cbic.202200190",

language = "English",

volume = "23",

journal = "Chembiochem",

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TY - JOUR

T1 - Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors

AU - Sondag, Daan

AU - Merx, Jona

AU - Rossing, Emiel

AU - Boltje, Thomas J.

AU - Löwik, Dennis W. P. M.

AU - Nelissen, Frank H. T.

AU - van Geffen, Mark

AU - van 't Veer, Cornelis

AU - van Heerde, Waander L.

AU - Rutjes, Floris P. J. T.

N1 - Funding Information: This work was supported by LIFT grant 741.018.406 from the Dutch Research Council (NWO) awarded to F.P.J.T.R., T.J.B. and W.L.v.H. Publisher Copyright: © 2022 The Authors. ChemBioChem published by Wiley-VCH GmbH.

PY - 2022/8/3

Y1 - 2022/8/3

N2 - 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.

AB - 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.

KW - enzymes

KW - imaging agents

KW - inhibitors

KW - luminescence

UR - http://www.scopus.com/inward/record.url?scp=85131792510&partnerID=8YFLogxK

U2 - https://doi.org/10.1002/cbic.202200190

DO - https://doi.org/10.1002/cbic.202200190

M3 - Article

C2 - 35649961

SN - 1439-4227

VL - 23

JO - Chembiochem

JF - Chembiochem

IS - 15

M1 - e202200190

ER -

Luminescent Assay for the Screening of SARS-CoV-2 MPro Inhibitors

Abstract

Keywords

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