tetano
Editor, Senior Moderator
Acta Pharm Sin B. 2015 Sep;5(5):419-430. Epub 2015 Sep 6.
[h=1]New small-molecule drug design strategies for fighting resistant influenza A.[/h] Shen Z[SUP]1[/SUP], Lou K[SUP]1[/SUP], Wang W[SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Influenza A virus is the major cause of seasonal or pandemic flu worldwide. Two main treatment strategies-vaccination and small molecule anti-influenza drugs are currently available. As an effective vaccine usually takes at least 6 months to develop, anti-influenza small molecule drugs are more effective for the first line of protection against the virus during an epidemic outbreak, especially in the early stage. Two major classes of anti-influenza drugs currently available are admantane-based M2 protein blockers (amantadine and rimantadine) and neuraminidase (NA) inhibitors (oseltamivir, zanamivir, and peramivir). However, the continuous evolvement of influenza A virus and the rapid emergence of resistance to current drugs, particularly to amantadine, rimantadine, and oseltamivir, have raised an urgent need for developing new anti-influenza drugs against resistant forms of influenza A virus. In this review, we first give a brief introduction of the molecular mechanisms behind resistance, and then discuss new strategies in small-molecule drug development to overcome influenza A virus resistance targeting mutant M2 proteins and neuraminidases, and other viral proteins not associated with current drugs.
[h=4]KEYWORDS:[/h] Drug discovery; Influenza A virus; M2 ion channel; Neuraminidase; Resistance
PMID: 26579472 [PubMed - as supplied by publisher] PMCID: PMC4629447 Free full text
[h=1]New small-molecule drug design strategies for fighting resistant influenza A.[/h] Shen Z[SUP]1[/SUP], Lou K[SUP]1[/SUP], Wang W[SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Influenza A virus is the major cause of seasonal or pandemic flu worldwide. Two main treatment strategies-vaccination and small molecule anti-influenza drugs are currently available. As an effective vaccine usually takes at least 6 months to develop, anti-influenza small molecule drugs are more effective for the first line of protection against the virus during an epidemic outbreak, especially in the early stage. Two major classes of anti-influenza drugs currently available are admantane-based M2 protein blockers (amantadine and rimantadine) and neuraminidase (NA) inhibitors (oseltamivir, zanamivir, and peramivir). However, the continuous evolvement of influenza A virus and the rapid emergence of resistance to current drugs, particularly to amantadine, rimantadine, and oseltamivir, have raised an urgent need for developing new anti-influenza drugs against resistant forms of influenza A virus. In this review, we first give a brief introduction of the molecular mechanisms behind resistance, and then discuss new strategies in small-molecule drug development to overcome influenza A virus resistance targeting mutant M2 proteins and neuraminidases, and other viral proteins not associated with current drugs.
[h=4]KEYWORDS:[/h] Drug discovery; Influenza A virus; M2 ion channel; Neuraminidase; Resistance
PMID: 26579472 [PubMed - as supplied by publisher] PMCID: PMC4629447 Free full text