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In silico Analysis of Conformational Changes Induced by Mutation of Aromatic Binding Residues: Consequences for Drug Binding in the hERG K+ Channel
Pharmacological inhibition of cardiac hERG K(+) channels is associated with increased risk of lethal arrhythmias. Many drugs reduce hERG current by directly binding to the channel, thereby blocking ion conduction. Mutation of two aromatic residues (F656 and Y652) substantially decreases the potency...
Autores principales: | Knape, Kirsten, Linder, Tobias, Wolschann, Peter, Beyer, Anton, Stary-Weinzinger, Anna |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3240635/ https://www.ncbi.nlm.nih.gov/pubmed/22194911 http://dx.doi.org/10.1371/journal.pone.0028778 |
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