Exploring Organosilane Amines as Potent Inhibitors and Structural Probes of Influenza A Virus M2 Proton Channel
摘要:
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 dose to V27.
[EN] ΡΡΑRγ MODULATORS AND METHODS OF USE<br/>[FR] MODULATEURS DE ΡΡΑRγ ET MÉTHODES D'UTILISATION
申请人:EISAI R&D MANGEMENT CO LTD
公开号:WO2022099144A1
公开(公告)日:2022-05-12
Disclosed herein are novel PPARy modulators of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the same, and methods of using the same, in particular for the treatment of cancers.
Exploring Organosilane Amines as Potent Inhibitors and Structural Probes of Influenza A Virus M2 Proton Channel
作者:Jun Wang、Chunlong Ma、Yibing Wu、Robert A. Lamb、Lawrence H. Pinto、William F. DeGrado
DOI:10.1021/ja2050666
日期:2011.9.7
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 dose to V27.