Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected cells
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- dc.contributor.author Vanhoutte, Roeland
- dc.contributor.author Barniol Xicota, Marta
- dc.contributor.author Chiu, Winston
- dc.contributor.author Vangeel, Laura
- dc.contributor.author Jochmans, Dirk
- dc.contributor.author De Jonghe, Steven
- dc.contributor.author Zidane, Hadeer
- dc.contributor.author Barr, Haim M.
- dc.contributor.author London, Nir
- dc.contributor.author Neyts, Johan
- dc.contributor.author Verhelst, Steven
- dc.date.accessioned 2025-05-05T06:13:24Z
- dc.date.available 2025-05-05T06:13:24Z
- dc.date.issued 2023
- dc.description Includes supplementary materials for the online appendix.
- dc.description.abstract The COVID-19 pandemic has revealed the vulnerability of the modern, global society. With expected waves of future infections by SARS-CoV-2, treatment options for infected individuals will be crucial in order to decrease mortality and hospitalizations. The SARS-CoV-2 main protease is a validated drug target, for which the first inhibitor has been approved for use in patients. To facilitate future work on this drug target, we designed a solid-phase synthesis route towards azapeptide activity-based probes that are capped with a cysteine-reactive electrophile for covalent modification of the active site of Mpro. This design led to the most potent ABP for Mpro and one of the most potent inhibitors reported thus far. We demonstrate that this ABP can be used to visualize Mpro activity and target engagement by drugs in infected cells.en
- dc.format.mimetype application/pdf
- dc.identifier.citation Vanhoutte R, Barniol-Xicota M, Chiu W, Vangeel L, Jochmans D, De Jonghe S, et al. Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected cells. Chem Sci. 2023 Feb 21;14(7):1666-72. DOI: 10.1039/d2sc04147b
- dc.identifier.doi http://dx.doi.org/10.1039/D2SC04147B
- dc.identifier.issn 2041-6520
- dc.identifier.uri http://hdl.handle.net/10230/70265
- dc.language.iso eng
- dc.publisher Royal Society of Chemistry
- dc.relation.ispartof Chemical Science. 2023 Feb 21;14(7):1666-72
- dc.rights This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.
- dc.rights.accessRights info:eu-repo/semantics/openAccess
- dc.rights.uri http://creativecommons.org/licenses/by-nc/3.0/
- dc.subject.other COVID-19 (Malaltia)ca
- dc.subject.other Pandèmia de COVID-19, 2020-ca
- dc.subject.other Pandèmiesca
- dc.title Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected cellsen
- dc.type info:eu-repo/semantics/article
- dc.type.version info:eu-repo/semantics/publishedVersion