Simon Fraser University virologist Masahiro Niikura and his doctoral 
student Nicole Bance are among an international group of scientists that
 has discovered a new class of molecular compounds capable of killing 
the influenza virus.
Working on the premise that too much of a good thing can be a killer,
 the scientists have advanced previous researchers' methods of 
manipulating an enzyme that is key to how influenza replicates and 
spreads.
Their new compounds will lead to a new generation of anti-influenza 
drugs that the virus' strains can't adapt to, and resist, as easily as 
they do Tamiflu. It's an anti-influenza drug that is becoming less 
effective against the constantly mutating flu virus.
These increasingly less adequate anti-influenza drugs are currently 
doctors' best weapons against influenza. They helped the world beat 
H1N1, swine flu, into submission four years ago.
The journal Science Express has just published online the 
scientists' study, revealing how to use their newly discovered compounds
 to interrupt the enzyme neuraminidase's facilitation of influenza's 
spread.
Tamiflu and another anti-influenza drug, Relenza, focus on 
interrupting neuraminidase's ability to help influenza detach from an 
infected cell's surface by digesting sialic acid, a sugar on the surface
 of the cell. The flu virus uses the same sugar to stick to the cell 
while invading it. Once attached, influenza can invade the cell and 
replicate.
This is where the newly discovered compounds come to the 
still-healthy cells' rescue. They clog up neuraminidase, stopping the 
enzyme from dissolving the sialic acid, which prevents the virus from 
escaping the infected cell and spreading.
The new compounds are also more effective because they're 
water-soluble. "They reach the patient's throat where the flu virus is 
replicating after being taken orally," says Niikura, a Faculty of Health
 Sciences associate professor.
"Influenza develops resistance to Relenza less frequently, but it's 
not the drug of choice like Tamiflu because it's 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."
Ultimately, the new compounds will buy scientists more time to 
develop new vaccines for emerging strains of influenza that are 
resistant to existing vaccines.
Journal Reference:
- Jin-Hyo Kim, Ricardo Resende, Tom Wennekes, Hong-Ming Chen, Nicole Bance, Sabrina Buchini, Andrew G. Watts, Pat Pilling, Victor A. Streltsov, Martin Petric, Richard Liggins, Susan Barrett, Jennifer L. McKimm-Breschkin, Masahiro Niikura, and Stephen G. Withers. Mechanism-Based Covalent Neuraminidase Inhibitors with Broad Spectrum Influenza Antiviral Activity. Science, 21 February 2013 DOI: 10.1126/science.1232552
 
Courtesy: ScienceDaily 


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