tetano
Editor, Senior Moderator
J Med Chem. 2012 May 21. [Epub ahead of print]
Antivirals targeting influenza A virus.
Das K.
Abstract
Seasonal influenza A infections are effectively prevented by vaccines, which are reformulated each year. Antivirals are used for both prophylactic and therapeutic treatments of seasonal flu and to control pandemic flu outbreaks. Current antivirals (i) adamantanes (amantadine and rimantadine) are directed against the viral M2 ion-channel protein and (ii) zanamivir and oseltamivir are the inhibitors of a viral surface protein, neuraminidase. Emergence of drug resistance mutations limits the use of adamantanes and increasingly threatens the long-term efficacy of the commonly used oral drug oseltamivir. Understanding molecular mechanisms of drug resistance and the role of compensatory mutations that enhance the fitness of resistant viruses, as well as devising novel design strategies, may facilitate the discovery of new antivirals against existing influenza A targets, M2 and neuraminidase. Among other molecular entities of influenza A virus, the multifunctional and multisubunit viral polymerase is an attractive target for developing new flu drugs.
PMID:
22612288
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22612288
Antivirals targeting influenza A virus.
Das K.
Abstract
Seasonal influenza A infections are effectively prevented by vaccines, which are reformulated each year. Antivirals are used for both prophylactic and therapeutic treatments of seasonal flu and to control pandemic flu outbreaks. Current antivirals (i) adamantanes (amantadine and rimantadine) are directed against the viral M2 ion-channel protein and (ii) zanamivir and oseltamivir are the inhibitors of a viral surface protein, neuraminidase. Emergence of drug resistance mutations limits the use of adamantanes and increasingly threatens the long-term efficacy of the commonly used oral drug oseltamivir. Understanding molecular mechanisms of drug resistance and the role of compensatory mutations that enhance the fitness of resistant viruses, as well as devising novel design strategies, may facilitate the discovery of new antivirals against existing influenza A targets, M2 and neuraminidase. Among other molecular entities of influenza A virus, the multifunctional and multisubunit viral polymerase is an attractive target for developing new flu drugs.
PMID:
22612288
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22612288