4.3 Article

hERG drug response measured in droplet bilayers

Journal

BIOMEDICAL MICRODEVICES
Volume 15, Issue 2, Pages 255-259

Publisher

SPRINGER
DOI: 10.1007/s10544-012-9725-9

Keywords

Ion channel; Inhibition; hERG; Lipid bilayer; Screening

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We show measurements of the human cardiac potassium ion channel K(v)11.1 (hERG) in droplet bilayers incorporated directly from commercial membrane preparations of HEK293 cells. Although we do not obtain ensemble conductance kinetics and rectification observed in patch clamp measurements of hERG, ensemble currents measured in our system showed inhibition dependent on astemizole and E-4031 concentration, with IC50 values similar to those found with patch clamp. The availability of engineered HEK cells expressing a variety of ion channels, combined with the simplicity of the inhibition measurement, suggest that droplet bilayers may have considerable technological potential for determination of ion channel drug potency.

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