💎 PREMIUM: Gallery - Complete Album!
An official website of the United States government
The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before
sharing sensitive information, make sure you’re on a federal
government site.
The site is secure.
The https:// ensures that you are connecting to the
official website and that any information you provide is encrypted
and transmitted securely.
Mechanism-based covalent neuraminidase inhibitors with broad-spectrum influenza antiviral activity
- PMID: 23429702
- DOI: 10.1126/science.1232552
Mechanism-based covalent neuraminidase inhibitors with broad-spectrum influenza antiviral activity
Abstract
Influenza antiviral agents play important roles in modulating disease severity and in controlling pandemics while vaccines are prepared, but the development of resistance to agents like the commonly used neuraminidase inhibitor oseltamivir may limit their future utility. We report here on a new class of specific, mechanism-based anti-influenza drugs that function through the formation of a stabilized covalent intermediate in the influenza neuraminidase enzyme, and we confirm this mode of action with structural and mechanistic studies. These compounds function in cell-based assays and in animal models, with efficacies comparable to that of the neuraminidase inhibitor zanamivir and with broad-spectrum activity against drug-resistant strains in vitro. The similarity of their structure to that of the natural substrate and their mechanism-based design make these attractive antiviral candidates.
Comment in
-
Infectious diseases: Novel agents fight flu infection.Nat Rev Drug Discov. 2013 May;12(5):345. doi: 10.1038/nrd4013. Epub 2013 Apr 19. Nat Rev Drug Discov. 2013. PMID: 23598508 No abstract available.
Publication types
MeSH terms
Substances
Associated data
- Actions
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources
