期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 12, 期 3, 页码 426-432出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00651
关键词
furin inhibitors; proprotein convertases; canavanine; crystal structure analysis; proteolytic activation of viruses
资金
- LOEWE Center DRUID (Novel Drug Targets against Poverty-Related and Neglected Tropical Infectious Diseases)
- Austrian Science Fund (FWF) [M 2730]
Furin activates viral glycoproteins, and inhibiting it can prevent virus replication. New inhibitors targeting furin have been developed, showing potent antiviral activity in cell culture.
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.
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