首页|Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics
Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics
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A titrant for the SARS-CoV-2 main protease(Mpro)was developed that enables,for the first time,the exact determination of the concentration of the enzymatically active Mpro by active-site titration.The covalent binding mode of the tetrapeptidic titrant was elucidated by the determination of the crystal structure of the enzyme-titrant complex.Four fluorogenic substrates of Mpro,including a prototypical,intemally quenched Dabcyl-EDANS peptide,were compared in terms of solubility under typical assay conditions.By exploiting the new titrant,key kinetic parameters for the Mpro-catalyzed cleavage of these substrates were determined.
Pharmaceutical Institute,Pharmaceutical & Medicinal Chemistry,University of Bonn,Bonn 53121,Germany
Institute of Bioanalytical Chemistry,Center for Biotechnology and Biomedicine,Leipzig University,Leipzig 04103,Germany
Department of Natural Sciences,University of Applied Sciences Bonn-Rhein-Sieg,Rheinbach 53359,Germany
Volkswagen FoundationRabea Voget,Christian Steinebach,Christa E.Müller and Michael Gütschow by the German Research FoundationNorbert Str?ter by the Volkswagen Foundation
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