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

被引：7
|
作者：
Sondag, Daan [1 ]
Merx, Jona [1 ]
Rossing, Emiel [1 ]
Boltje, Thomas J. [1 ]
Lowik, Dennis W. P. M. [1 ]
Nelissen, Frank H. T. [1 ]
van Geffen, Mark [2 ]
Veer, Cornelis van 't [2 ]
van Heerde, Waander L. [2 ,3 ,4 ]
Rutjes, Floris P. J. T. [1 ]
机构：
[1] Radboud Univ Nijmegen, Inst Mol & Mat, NL-6525 AL Nijmegen, Netherlands
[2] Enzyre BV, Novio Tech Campus,Transistorweg 5-I, NL-6534 AT Nijmegen, Netherlands
[3] Radboud Univ Nijmegen Med Ctr, Dept Haematol, Nijmegen, Netherlands
[4] Nijmegen Eindhoven Maastricht HTC NEM, Nijmegen, Netherlands
来源：
CHEMBIOCHEM | 2022年 / 23卷 / 15期
基金：
荷兰研究理事会;
关键词：
enzymes; inhibitors; imaging agents; luminescence; PROTEASE;
D O I：
10.1002/cbic.202200190
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 IC50 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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页数：5
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