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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...

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Detalhes bibliográficos
Main Authors: Knape, Kirsten, Linder, Tobias, Wolschann, Peter, Beyer, Anton, Stary-Weinzinger, Anna
Formato: Artigo
Idioma:Inglês
Publicado em: Public Library of Science 2011
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3240635/
https://ncbi.nlm.nih.gov/pubmed/22194911
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1371/journal.pone.0028778
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