期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 2, 期 4, 页码 307-312出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100297w
关键词
Influenza A/M2; A/M2 channel inhibitor; two-electrode voltage clamp assay (TEVC)
资金
- NIH [GM56423, AI74571]
Inhibitors targeting the influenza A virus M2 (A/M2) proton channel have lost their effectiveness due to widespread resistance. As a first step in the development of new inhibitors that address this problem, we have screened several focused collections of small molecules using two-electrode voltage patch clamp assays (TEVC) on Xenopus laevis oocytes. Diverse head groups and scaffolds of A/M2 inhibitors have been explored. It has been found that not only amine but also hydroxyl, aminooxyl, guanidine, and amidine compounds are active against the A/M2 proton channel. Moreover, the channel is able to accommodate a wide range of structural variation in the apolar scaffold. This study offers information to guide the next generation of A/M2 proton channel inhibitor design.
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