title: Single channel and ensemble hERG conductance measured in droplet bilayers.
abstract: The human ether-a-go-go related gene (hERG) encodes the potassium channel Kv11.1, which plays a key role in the cardiac action potential and has been implicated in cardiac disorders as well as a number of off-target pharmaceutical interactions. The electrophysiology of this channel has been predominantly studied using patch clamp, but lipid bilayers have the potential to offer some advantages, including apparatus simplicity, ease of use, and the ability to control the membrane and solution compositions. We made membrane preparations from hERG-expressing cells and measured them using droplet bilayers, allowing measurement of channel ensemble currents and 13.5 pS single channel currents. These currents were ion selective and were blockable by E-4031 and dofetilide in a dose-dependent manner, allowing determination of IC50 values of 17 nM and 9.65 μM for E-4031 and dofetilide, respectively. We also observed time- and voltage- dependent currents following step changes in applied potential that were similar to previously reported patch clamp measurements.
authors: Department of Bioengineering, University of California Los Angeles, Los Angeles, CA, 90095, USA.
authors: Viksita
authors: V
authors: Vijayvergiya
authors: Shiv
authors: S
authors: Acharya
authors: Jason
authors: J
authors: Poulos
authors: Jacob
authors: J
authors: Schmidt
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000737:chemistry; D000072237:ERG1 Potassium Channel; D004553:Electric Conductivity; D051638:Ether-A-Go-Go Potassium Channels / Q000737:chemistry*; D057809:HEK293 Cells; D006801:Humans; D008051:Lipid Bilayers; D051379:Mice; D010880:Piperidines / Q000737:chemistry; D011725:Pyridines / Q000737:chemistry
chemical_list: D000889:Anti-Arrhythmia Agents; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; C000606913:KCNH2 protein, human; D008051:Lipid Bilayers; D010880:Piperidines; D011725:Pyridines; C063968:E 4031