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

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 classe...

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Veröffentlicht in:RSC chemical biology 2023-08, Vol.4 (8), p.533-547
Hauptverfasser: Stubbing, Louise A, Hubert, Jonathan G, Bell-Tyrer, Joseph, Hermant, Yann O, Yang, Sung Hyun, McSweeney, Alice M, McKenzie-Goldsmith, Geena M, Ward, Vernon K, Furkert, Daniel P, Brimble, Margaret A
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container_end_page 547
container_issue 8
container_start_page 533
container_title RSC chemical biology
container_volume 4
creator Stubbing, Louise A
Hubert, Jonathan G
Bell-Tyrer, Joseph
Hermant, Yann O
Yang, Sung Hyun
McSweeney, Alice M
McKenzie-Goldsmith, Geena M
Ward, Vernon K
Furkert, Daniel P
Brimble, Margaret A
description 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/3CL pro , which play a key role in viral replication and present minimal homology with mammalian proteases. Particular focus is put on the reported development of P 1 glutamine isosteres to generate potent inhibitors mimicking the natural substrate sequence at the site of recognition.’ 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.
doi_str_mv 10.1039/d3cb00075c
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title P1 Glutamine isosteres in the design of inhibitors of 3C/3CL protease of human viruses of the Pisoniviricetes class
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