Exploring Organosilane Amines as Potent Inhibitors and Structural Probes of Influenza A Virus M2 Proton Channel

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• 作者：Jun Wang ; Chunlong Ma ; Yibing Wu ; Robert A. Lamb ; Lawrence H. Pinto ; William F. DeGrado
• 刊名：Journal of the American Chemical Society
• 出版年：2011
• 出版时间：September 7, 2011
• 年：2011
• 卷：133
• 期：35
• 页码：13844-13847
• 全文大小：789K
• 年卷期：v.133,no.35(September 7, 2011)
• ISSN：1520-5126

文摘

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.