Abstract
AbstractThe discovery of new anti-influenza drugs is urgent, particularly considering the recent threat of swine flu. In this study, the influenza virus M2 protein was expressed in HEK293 cells and shown to have selective ion channel activity for monovalent ions. The anti-influenza virus drug amantadine hydrochloride significantly attenuated the inward current induced by hyperpolarization of HEK293 cell membranes. Although adamantine derivatives are the only M2 drugs for influenza virus A, their use is limited in the US due to drug resistance. Here we report the discovery of multiple M2 inhibitor lead compounds that were rapidly generated through focused screening of a small primary amine library. The screen was designed using a scaffold-hopping strategy based on amantadine. This study suggests that an antiviral compound directed against a conserved motif may be more useful than amantadine in inhibiting viral replication.
Highlights
There is currently an outbreak of H1N1 influenza around the world[1,2]
Dr Gillet mentioned in his paper that[10] focused screening involves the selection of a subset of compounds according to existing structure-activity relationships
Many publications[12,13,14,15] have discussed the trends and high-throughput screening (HTS) application in drug discovery, there is a shortage of successful case studies that validate this approach
Summary
There is currently an outbreak of H1N1 influenza (swine flu) around the world[1,2]. vaccination is the ideal way to prevent influenza virus infection, the preparation of a new vaccine requires more than 6 months[3]. Very few effective drugs are available to combat the influenza virus. The only known anti-influenza A drugs[3,4,5,6] are M2 inhibitors (amantadine and its derivative rimantadine) and NA inhibitors (zanamivir and oseltamivir). There is growing concern that anti-neuraminidase-resistant viruses may emerge if these drugs are widely used[7].
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