Journal article
Thiophene-fused γ-lactams inhibit the SARS-CoV-2 main protease via reversible covalent acylation
- Abstract:
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Enzyme inhibitors working by O-acylation of nucleophilic serine residues are of immense medicinal importance, as exemplified by the β-lactam antibiotics. By contrast, inhibition of nucleophilic cysteine enzymes by S-acylation has not been widely exploited for medicinal applications. The SARS-CoV-2 main protease (Mpro) is a nucleophilic cysteine protease and a validated therapeutic target for COVID-19 treatment using small-molecule ...
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- Publication status:
- Published
- Peer review status:
- Peer reviewed
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- Files:
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(Preview, Version of record, pdf, 2.4MB, Terms of use)
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- Publisher copy:
- 10.1039/d4sc01027b
Authors
Funding
+ Biotechnology and Biological Sciences Research Council
More from this funder
Grant:
BB/R000344/1
BB/J003018/1
Bibliographic Details
- Publisher:
- Royal Society of Chemistry
- Journal:
- Chemical Science More from this journal
- Volume:
- 15
- Issue:
- 20
- Pages:
- 7667-7678
- Publication date:
- 2024-04-16
- Acceptance date:
- 2024-04-15
- DOI:
- EISSN:
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2041-6539
- ISSN:
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2041-6520
- Pmid:
-
38784729
Item Description
- Language:
-
English
- Keywords:
- Pubs id:
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1994279
- Local pid:
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pubs:1994279
- Deposit date:
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2024-05-28
Terms of use
- Copyright holder:
- Gayatri et al.
- Copyright date:
- 2024
- Rights statement:
- © 2024 The Author(s). Published by the Royal Society of Chemistry. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
- Notes:
- This research was funded in part by the Wellcome Trust (106244/Z/14/Z). For the purpose of open access, the author has applied a CC BY public copyright license to any Author Accepted Manuscript version arising from this submission.
- Licence:
- CC Attribution (CC BY) 3.0
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