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Exploring organosilane amines as potent inhibitors and structural probes of influenza a virus M2 proton channel.

ABSTRACT: We describe the use of organosilanes as inhibitors and structural probes of a membrane protein, the M2 proton channel from influenza A virus. Organosilane amine inhibitors were found to be generally as potent as their carbon analogues in targeting WT A/M2 and more potent against the drug-resistant A/M2-V27A mutant. In addition, intermolecular NOESY spectra with dimethyl-substituted organosilane amine inhibitors clearly located the drug binding site at the N-terminal lumen of the A/M2 channel close to V27.

SUBMITTER: Wang J

PROVIDER: S-EPMC3166227 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature

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Exploring organosilane amines as potent inhibitors and structural probes of influenza a virus M2 proton channel.

Wang Jun J Ma Chunlong C Wu Yibing Y Lamb Robert A RA Pinto Lawrence H LH DeGrado William F WF

Journal of the American Chemical Society 20110812 35

We describe the use of organosilanes as inhibitors and structural probes of a membrane protein, the M2 proton channel from influenza A virus. Organosilane amine inhibitors were found to be generally as potent as their carbon analogues in targeting WT A/M2 and more potent against the drug-resistant A/M2-V27A mutant. In addition, intermolecular NOESY spectra with dimethyl-substituted organosilane amine inhibitors clearly located the drug binding site at the N-terminal lumen of the A/M2 channel clo ...[more]

PMID: 21819109

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