The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
11 Mar 2021
11 Mar 2021
Historique:
received:
15
12
2020
accepted:
05
02
2021
entrez:
18
3
2021
pubmed:
19
3
2021
medline:
19
3
2021
Statut:
epublish
Résumé
Furin activates numerous viral glycoproteins, and its inhibition prevents virus replication and spread. Through the replacement of arginine by the less basic canavanine, new inhibitors targeting furin in the trans-Golgi network were developed. These inhibitors exert potent antiviral activity in cell culture with much lower toxicity than arginine-derived analogues, most likely due to their reduced protonation in the blood circulation. Thus, despite its important physiological functions, furin might be a suitable antiviral drug target.
Identifiants
pubmed: 33732412
doi: 10.1021/acsmedchemlett.0c00651
pmc: PMC7957917
doi:
Types de publication
Journal Article
Langues
eng
Pagination
426-432Informations de copyright
© 2021 The Authors. Published by American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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