title: hERG drug response measured in droplet bilayers.
abstract: We show measurements of the human cardiac potassium ion channel Kv11.1 (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.
authors.affiliation: Department of Bioengineering, University of California, Los Angeles, 5121 Engineering V, 420 Westwood Plaza, Los Angeles, CA 90095, USA.
authors.forename: Shiva A
authors.initials: SA
authors.lastname: Portonovo
authors.forename: Carl S
authors.initials: CS
authors.lastname: Salazar
authors.forename: Jacob J
authors.initials: JJ
authors.lastname: Schmidt
mesh_terms: D004353:Drug Evaluation, Preclinical / Q000295:instrumentation*; D000072237:ERG1 Potassium Channel; D004867:Equipment Design; D019544:Equipment Failure Analysis; D051638:Ether-A-Go-Go Potassium Channels / Q000737:chemistry* / Q000187:drug effects; D015640:Ion Channel Gating / Q000187:drug effects; D008051:Lipid Bilayers / Q000737:chemistry*; D008564:Membrane Potentials / Q000187:drug effects*; D046210:Microfluidic Analytical Techniques / Q000295:instrumentation*; D026902:Potassium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; C000606913:KCNH2 protein, human; D008051:Lipid Bilayers; D026902:Potassium Channel Blockers