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

Jun Wang; Chunlong Ma; Yibing Wu; Robert A. Lamb; Lawrence H. Pinto; William F. Degrado

doi:10.1021/ja2050666

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

Jun Wang
, Chunlong Ma
, Yibing Wu
, Robert A. Lamb
, Lawrence H. Pinto
, William F. Degrado

Research output: Contribution to journal › Article › peer-review

72 Scopus citations

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.

Original language	English (US)
Pages (from-to)	13844-13847
Number of pages	4
Journal	Journal of the American Chemical Society
Volume	133
Issue number	35
DOIs	https://doi.org/10.1021/ja2050666
State	Published - Sep 7 2011
Externally published	Yes

ASJC Scopus subject areas

Catalysis
General Chemistry
Biochemistry
Colloid and Surface Chemistry

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10.1021/ja2050666

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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.",

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AU - Wang, Jun

AU - Ma, Chunlong

AU - Wu, Yibing

AU - Lamb, Robert A.

AU - Pinto, Lawrence H.

AU - Degrado, William F.

PY - 2011/9/7

Y1 - 2011/9/7

N2 - 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.

AB - 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.

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

Abstract

ASJC Scopus subject areas

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