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The basicity makes the difference: improved canavanine-derived inhibitors of the proprotein convertase furin

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...

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Main Authors: Van Lam van, Thuy (Author) , Heindl, Miriam Ruth (Author) , Schlutt, Christine (Author) , Böttcher-Friebertshäuser, Eva (Author) , Bartenschlager, Ralf (Author) , Klebe, Gerhard (Author) , Brandstetter, Hans (Author) , Dahms, Sven O. (Author) , Steinmetzer, Torsten (Author)
Format: Article (Journal)
Language:English
Published: February 9, 2021
In: ACS medicinal chemistry letters
Year: 2021, Volume: 12, Issue: 3, Pages: 426-432
ISSN:1948-5875
DOI:10.1021/acsmedchemlett.0c00651
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/acsmedchemlett.0c00651
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Author Notes:Thuy Van Lam van, Miriam Ruth Heindl, Christine Schlutt, Eva Böttcher-Friebertshäuser, Ralf Bartenschlager, Gerhard Klebe, Hans Brandstetter, Sven O. Dahms, and Torsten Steinmetzer
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Summary: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.
Item Description:Gesehen am 29.06.2021
Physical Description:Online Resource
ISSN:1948-5875
DOI:10.1021/acsmedchemlett.0c00651

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