The Pore-Lipid Interface: Role of Amino-Acid Determinants of Lipophilic Access by Ivabradine to the hERG1 Pore Domain

Abnormal cardiac electrical activity is a common side effect caused by unintended block of the promiscuous drug target human ether-à-go-go-related gene (hERG1), the pore-forming domain of the delayed rectifier K+ channel in the heart. hERG1 block leads to a prolongation of the QT interval, a phase o...

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Veröffentlicht in:	Molecular pharmacology 2019-08, Vol.96 (2), p.259-271
Hauptverfasser:	Perissinotti, Laura, Guo, Jiqing, Kudaibergenova, Meruyert, Lees-Miller, James, Ol’khovich, Marina, Sharapova, Angelica, Perlovich, German L., Muruve, Daniel A., Gerull, Brenda, Noskov, Sergei Yu, Duff, Henry J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Ether-A-Go-Go Potassium Channels - chemistry Ether-A-Go-Go Potassium Channels - genetics Ether-A-Go-Go Potassium Channels - metabolism Humans Ivabradine - chemistry Ivabradine - pharmacology Membrane Lipids - metabolism Models, Molecular Molecular Docking Simulation Molecular Dynamics Simulation Mutagenesis, Site-Directed Phenethylamines - pharmacology Protein Binding Protein Structure, Tertiary Sulfonamides - pharmacology
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