Allosteric Coupling Between Drug Binding and the Aromatic Cassette in the Pore Domain of the hERG1 Channel: Implications for a State-Dependent Blockade

• Main Authors: Meruyert Kudaibergenova (Author), Jiqing Guo (Author), Hanif M. Khan (Author), Farhan Zahid (Author), James Lees-Miller (Author), Sergei Yu. Noskov (Author), Henry J. Duff (Author)
• Format: Book
• Published: Frontiers Media S.A., 2020-06-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Human-ether-a-go-go-related channel (hERG1) is the pore-forming domain of the delayed rectifier K+ channel in the heart which underlies the IKr current. The channel has been extensively studied due to its propensity to bind chemically diverse group of drugs. The subsequent hERG1 block can lead to a...