Mass spectrometry reveals potential of β-lactams as SARS-CoV-2 M(pro) inhibitors

The main viral protease (M(pro)) of SARS-CoV-2 is a nucleophilic cysteine hydrolase and a current target for anti-viral chemotherapy. We describe a high-throughput solid phase extraction coupled to mass spectrometry M(pro) assay. The results reveal some β-lactams, including penicillin esters, are ac...

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Detalles Bibliográficos
Autores principales: Malla, Tika R., Tumber, Anthony, John, Tobias, Brewitz, Lennart, Strain-Damerell, Claire, Owen, C David, Lukacik, Petra, Chan, H. T. Henry, Maheswaran, Pratheesh, Salah, Eidarus, Duarte, Fernanda, Yang, Haitao, Rao, Zihe, Walsh, Martin A., Schofield, Christopher J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8006714/
https://www.ncbi.nlm.nih.gov/pubmed/33462575
http://dx.doi.org/10.1039/d0cc06870e
Descripción
Sumario:The main viral protease (M(pro)) of SARS-CoV-2 is a nucleophilic cysteine hydrolase and a current target for anti-viral chemotherapy. We describe a high-throughput solid phase extraction coupled to mass spectrometry M(pro) assay. The results reveal some β-lactams, including penicillin esters, are active site reacting M(pro) inhibitors, thus highlighting the potential of acylating agents for M(pro) inhibition.

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