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J Am Chem Soc. 2011 Sep 7;133(35):13844-7. doi: 10.1021/ja2050666. Epub 2011 Aug 12.

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

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1
Department of Chemistry, School of Medicine, University of Pennsylvania, Philadelphia, 19104-6059, United States.

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.

PMID:
21819109
PMCID:
PMC3166227
DOI:
10.1021/ja2050666
[Indexed for MEDLINE]
Free PMC Article
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