Channelopathies and drug discovery in the postgenomic era

Duan, Dayue Darrel; Ma, Tiantian

doi:10.1038/aps.2011.73

Cited by 1 publication

(1 citation statement)

References 36 publications

(41 reference statements)

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“…[1][2][3][4][5] As important drug targets, ion channels are of considerable interest to the pharmaceutical industry. 6 Classical electrophysiology measurements can provide detailed information about the structure-function relationship of ion channels and their modulation by pharmaceutical drugs.…”

Section: Introductionmentioning

confidence: 99%

Screening ion-channel ligand interactions with passive pumping in a microfluidic bilayer lipid membrane chip

et al. 2015

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We describe a scalable artificial bilayer lipid membrane platform for rapid electrophysiological screening of ion channels and transporters. A passive pumping method is used to flow microliter volumes of ligand solution across a suspended bilayer within a microfluidic chip. Bilayers are stable at flow rates up to $0.5 ll/ min. Phospholipid bilayers are formed across a photolithographically defined aperture made in a dry film resist within the microfluidic chip. Bilayers are stable for many days and the low shunt capacitance of the thin film support gives lownoise high-quality single ion channel recording. Dose-dependent transient blocking of a-hemolysin with b-cyclodextrin (b-CD) and polyethylene glycol is demonstrated and dose-dependent blocking studies of the KcsA potassium channel with tetraethylammonium show the potential for determining IC 50 values. The assays are fast (30 min for a complete IC 50 curve) and simple and require very small amounts of compounds (100 lg in 15 ll). The technology can be scaled so that multiple bilayers can be addressed, providing a screening platform for ion channels, transporters, and nanopores. V C 2015 AIP Publishing LLC.

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