Features | Partner Sites | Information | LinkXpress
Sign In
GLOBETECH PUBLISHING
JIB
GLOBETECH PUBLISHING

New Class of Anti-Influenza Drugs Less Likely to Trigger Resistance

By BiotechDaily International staff writers
Posted on 06 Mar 2013
A team of molecular virologists has designed a small molecule drug that blocks the spread of the influenza virus more effectively and with less likelihood of triggering development of resistance than the currently available antiviral agents.

Drugs for treatment of influenza are neuraminidase inhibitors that target the virus' surface neuraminidase enzyme. They work by blocking the function of the viral neuraminidase protein, thus preventing the virus from reproducing by budding from the host cell. Oseltamivir (Tamiflu) a prodrug, Zanamivir (Relenza), Laninamivir (Inavir), and Peramivir belong to this class. Unlike the M2 inhibitors, which work only against influenza A, neuraminidase inhibitors act against both influenza A and influenza B.

The main failing of the currently used neuraminidase inhibitors is the rapid development of strains of the virus that are resistant to the drugs. To counter this problem investigators at Simon Fraser University (Burnaby, BC, Canada) searched for potential drugs that would be as efficient as the currently used drugs but less likely to trigger development of resistant strains of the virus.

They reported in the February 21, 2013, online edition of the journal Science Express that they had discovered—and confirmed the mode of action via structural and mechanistic studies—a new class of specific, mechanism-based anti-influenza drugs that functioned via the formation of a stabilized covalent intermediate in the influenza neuraminidase enzyme.

These compounds functioned 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 investigators maintain that the similarity of the drugs' structure to that of sialic acid, the natural substrate of neuraminidase, and their mechanism-based design make them attractive antiviral candidates.

The new class of drugs is particularly effective due to its water solubility. “They reach the patient’s throat where the flu virus is replicating after being taken orally,” said contributing author Dr. Masahiro Niikura, associate professor of virology at Simon Fraser University. “Influenza develops resistance to Repenza less frequently, but it is not the drug of choice like Tamiflu because it is not water-soluble and has to be taken as a nasal spray. Our new compounds are structurally more similar to sialic acid than Tamiflu. We expect this closer match will make it much more difficult for influenza to adapt to new drugs.”

Related Links:

Simon Fraser University



comments powered by Disqus

Channels

Genomics/Proteomics

view channel
Image: This micrograph depicts the presence of aerobic Gram-negative Neisseria meningitidis diplococcal bacteria; magnification 1150x (Photo courtesy of the CDC - US Centers for Disease Control and Prevention).

Infection by Meningitis Bacteria Depends on Dimerization State of Certain Host Cell Proteins

A team of molecular microbiologists has untangled the complex three-way interaction between the non-integrin laminin receptor (LAMR1), galectin-3 (Gal-2), and the pathogenic bacterium Neisseria meningitidis.... Read more

Lab Technologies

view channel
Image: Yale West Campus is organized into research institutes and core facilities — all designed to promote collaboration and interdisciplinary dialogue (Photo courtesy of Yale University).

American and European Partners Establish a Microscopy Center of Excellence

A prominent American university has announced a partnership agreement with a major European producer of microscopes and imaging tools that will establish a center for the use of cutting-edge imaging technologies... Read more

Business

view channel

Interest in Commercial Applications for Proteomics Continues to Grow

Increasing interest in the field of proteomics has led to a series of agreements between private proteomic companies and academic institutions as well as deals between pharmaceutical companies and novel proteomics innovator biotech companies. Proteomics is the study of the structure and function of proteins.... Read more
 
Copyright © 2000-2014 Globetech Media. All rights reserved.