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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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Detalles Bibliográficos
Autores principales: Knape, Kirsten, Linder, Tobias, Wolschann, Peter, Beyer, Anton, Stary-Weinzinger, Anna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2011
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