دورية أكاديمية
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Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics.

التفاصيل البيبلوغرافية
العنوان: Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics.
المؤلفون: Voget R; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Breidenbach J; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Claff T; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Hingst A; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Sylvester K; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Steinebach C; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Vu LP; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Weiße RH; Institute of Bioanalytical Chemistry, Center for Biotechnology and Biomedicine, Leipzig University, Leipzig 04103, Germany., Bartz U; Department of Natural Sciences, University of Applied Sciences Bonn-Rhein-Sieg, Rheinbach 53359, Germany., Sträter N; Institute of Bioanalytical Chemistry, Center for Biotechnology and Biomedicine, Leipzig University, Leipzig 04103, Germany., Müller CE; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany., Gütschow M; Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, Bonn 53121, Germany.
المصدر: Acta pharmaceutica Sinica. B [Acta Pharm Sin B] 2024 May; Vol. 14 (5), pp. 2349-2357. Date of Electronic Publication: 2024 Mar 06.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Elsevier Country of Publication: Netherlands NLM ID: 101600560 Publication Model: Print-Electronic Cited Medium: Print ISSN: 2211-3835 (Print) Linking ISSN: 22113835 NLM ISO Abbreviation: Acta Pharm Sin B Subsets: PubMed not MEDLINE
أسماء مطبوعة: Original Publication: [Amsterdam] : Elsevier, 2011-
مستخلص: A titrant for the SARS-CoV-2 main protease (M pro ) was developed that enables, for the first time, the exact determination of the concentration of the enzymatically active M pro 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 M pro , including a prototypical, internally quenched Dabcyl-EDANS peptide, were compared in terms of solubility under typical assay conditions. By exploiting the new titrant, key kinetic parameters for the M pro -catalyzed cleavage of these substrates were determined.
Competing Interests: The authors declare no conflicts of interest.
(© 2024 The Authors.)
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فهرسة مساهمة: Keywords: Active-site titration; COVID-19; Fluorogenic substrates; Inner filter effect; Main protease; Peptide nitriles; SARS-CoV-2; X-ray crystallography
تواريخ الأحداث: Date Created: 20240527 Latest Revision: 20240528
رمز التحديث: 20240528
مُعرف محوري في PubMed: PMC11121168
DOI: 10.1016/j.apsb.2024.03.001
PMID: 38799620
قاعدة البيانات: MEDLINE
الوصف
تدمد:2211-3835
DOI:10.1016/j.apsb.2024.03.001