Document Detail


Exploring organosilane amines as potent inhibitors and structural probes of influenza a virus M2 proton channel.
MedLine Citation:
PMID:  21819109     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Jun Wang; Chunlong Ma; Yibing Wu; Robert A Lamb; Lawrence H Pinto; William F DeGrado
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2011-08-12
Journal Detail:
Title:  Journal of the American Chemical Society     Volume:  133     ISSN:  1520-5126     ISO Abbreviation:  J. Am. Chem. Soc.     Publication Date:  2011 Sep 
Date Detail:
Created Date:  2011-08-31     Completed Date:  2011-12-21     Revised Date:  2014-09-24    
Medline Journal Info:
Nlm Unique ID:  7503056     Medline TA:  J Am Chem Soc     Country:  United States    
Other Details:
Languages:  eng     Pagination:  13844-7     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Amines / chemistry,  pharmacology
Antiviral Agents / chemistry,  pharmacology*
Binding Sites
Drug Resistance, Viral
Humans
Influenza A virus / drug effects*,  genetics
Influenza, Human / drug therapy
Models, Molecular
Mutation
Proton Pump Inhibitors / chemistry,  pharmacology*
Proton Pumps / genetics,  metabolism*
Silanes / chemistry,  pharmacology*
Viral Proteins / antagonists & inhibitors,  genetics,  metabolism*
Grant Support
ID/Acronym/Agency:
AI74571/AI/NIAID NIH HHS; GM56423/GM/NIGMS NIH HHS; R01 AI020201/AI/NIAID NIH HHS; R01 GM056423/GM/NIGMS NIH HHS; R01 GM056423-12/GM/NIGMS NIH HHS; U01 AI074571/AI/NIAID NIH HHS; U01 AI074571-05/AI/NIAID NIH HHS
Chemical
Reg. No./Substance:
0/Amines; 0/Antiviral Agents; 0/Proton Pump Inhibitors; 0/Proton Pumps; 0/Silanes; 0/Viral Proteins
Comments/Corrections

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