Article
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting.
Nature communications - 12 Oct 2016
Wrobel Eva, Rothenberg Ina, Krisp Christoph, Hundt Franziska, Fraenzel Benjamin, Eckey Karina, Linders Joannes T M, Gallacher David J, Towart Rob, Pott Lutz, Pusch Michael, Yang Tao, Roden Dan M, Kurata Harley T, Schulze-Bahr Eric, Strutz-Seebohm Nathalie, Wolters Dirk, Seebohm Guiscard
Abstract excerpt
Most small-molecule inhibitors of voltage-gated ion channels display poor subtype specificity because they bind to highly conserved residues located in the channel's central cavity. Using a combined approach of scanning mutagenesis, electrophysiology, chemical ligand modification, chemical cross-linking, MS/MS-analyses and molecular modelling, we provide evidence for the binding site for adamantane derivatives...
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