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4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA−PB1 Protein−Protein Interaction: Structure− Activity Relationships Exploration with the Aid of Molecular Modeling

J Med Chem.. 2016-03; 
Trist IM, Nannetti G, Tintori C, Fallacara AL, Deodato D1, Mercorelli B2, Palù G2, Wijtmans M3, Gospodova T4, Edink E3, Verheij M3, de Esch I3, Viteva L4, Loregian A2, Botta M1,5.
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Monoclonal Antibody Services GST−PB1(1−25) was detected with an anti-GST monoclonal antibody conjugated to horseradish peroxidase (HRP) (GenScript). Get A Quote

摘要

Influenza is an infectious disease that represents an important public health burden, with high impact on the global morbidity, mortality, and economy. The poor protection and the need of annual updating of the anti-influenza vaccine, added to the rapid emergence of viral strains resistant to current therapy make the need for antiviral drugs with novel mechanisms of action compelling. In this regard, the viral RNA polymerase is an attractive target that allows the design of selective compounds with reduced risk of resistance. In previous studies we showed that the inhibition of the polymerase acidic protein-basic protein 1 (PA-PB1) interaction is a promising strategy for the development of anti-influenza agents... More

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