Thiophene-fused γ-lactams inhibit the SARS-CoV-2 main protease <i>via</i> reversible covalent acylation-Reference-Cited by-同舟云学术

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Thiophene-fused γ-lactams inhibit the SARS-CoV-2 main protease via reversible covalent acylation

Published:2024 Issue:20 Volume:15 Page:7667-7678
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Gayatri ¹,Brewitz Lennart¹^ORCID,Ibbotson Lewis¹,Salah Eidarus¹,Basak Shyam¹,Choudhry Hani²,Schofield Christopher J.¹^ORCID

Affiliation:

1. Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford, 12 Mansfield Road, OX1 3TA, Oxford, UK

2. Department of Biochemistry, Center for Artificial Intelligence in Precision Medicines, King Abdulaziz University, Jeddah, Saudi Arabia

Abstract

Thiophene-fused γ-lactams are reversible covalent inhibitors of the SARS-CoV-2 main protease, a nucleophilic cysteine enzyme. γ-Lactams can inhibit nucleophilic cysteine enzymes by S-acylation as well as nucleophilic serine enzymes by O-acylation.

Funder

Wellcome Trust

Biotechnology and Biological Sciences Research Council

Cancer Research UK

Publisher

Royal Society of Chemistry (RSC)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/SC/D4SC01027B

Reference101 articles.

1. Biologically active γ-lactams: synthesis and natural sources

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5. Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells.

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