Inhibitors of the influenza A virus M2 proton channel discovered using a high-throughput yeast growth restoration assay.

ABSTRACT: The M2 proton channel of the influenza A virus is the target of the anti-influenza drugs amantadine and rimantadine. The effectiveness of these drugs has been dramatically limited by the rapid spread of drug resistant mutations, mainly at sites S31N, V27A and L26F in the pore of the channel. Despite progress in designing inhibitors of V27A and L26F M2, there are currently no drugs targeting these mutated channels in clinical trials. Progress in developing new drugs has been hampered by the lack of a robust assay with sufficient throughput for discovery of new active chemotypes among chemical libraries and sufficient sensitivity to provide the SAR data essential for their improvement and development as drugs. In this study we adapted a yeast growth restoration assay, in which expression of

SUBMITTER: Balgi AD 

PROVIDER: S-EPMC3562233 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature