Issue 8, 2023

P1 Glutamine isosteres in the design of inhibitors of 3C/3CL protease of human viruses of the Pisoniviricetes class

Abstract

Viral infections are one of the leading causes of acute morbidity in humans and much endeavour has been made by the synthetic community for the development of drugs to treat associated diseases. Peptide-based enzyme inhibitors, usually short sequences of three or four residues, are one of the classes of compounds currently under development for enhancement of their activity and pharmaceutical properties. This review reports the advances made in the design of inhibitors targeting the family of highly conserved viral proteases 3C/3CLpro, which play a key role in viral replication and present minimal homology with mammalian proteases. Particular focus is put on the reported development of P1 glutamine isosteres to generate potent inhibitors mimicking the natural substrate sequence at the site of recognition.’

Graphical abstract: P1 Glutamine isosteres in the design of inhibitors of 3C/3CL protease of human viruses of the Pisoniviricetes class

Article information

Article type
Review Article
Submitted
25 5 2023
Accepted
19 6 2023
First published
21 6 2023
This article is Open Access
Creative Commons BY-NC license

RSC Chem. Biol., 2023,4, 533-547

P1 Glutamine isosteres in the design of inhibitors of 3C/3CL protease of human viruses of the Pisoniviricetes class

L. A. Stubbing, J. G. Hubert, J. Bell-Tyrer, Y. O. Hermant, S. H. Yang, A. M. McSweeney, G. M. McKenzie-Goldsmith, V. K. Ward, D. P. Furkert and M. A. Brimble, RSC Chem. Biol., 2023, 4, 533 DOI: 10.1039/D3CB00075C

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