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Issue 7, 2013
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Biomimetic membrane platform containing hERG potassium channel and its application to drug screening

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Abstract

The hERG (human ether-à-go-go-related gene) potassium channel has been extensively studied by both academia and industry because of its relation to inherited or drug-induced long QT syndrome (LQTS). Unpredicted hERG and drug interaction affecting channel activity is of main concern for drug discovery. Although there are several methods to test hERG and drug interaction, it is still necessary to develop some efficient and economic ways to probe hERG and drug interactions. To contribute this aim, we have developed a biomimetic lipid membrane platform into which the hERG channel can be folded. Expression and integration of the hERG channel was achieved using a cell-free (CF) expression system. The folding of hERG in the biomimetic membrane system was investigated using Surface Plasmon Enhanced Fluorescence Spectroscopy (SPFS) and Imaging Surface Plasmon Resonance (iSPR). In addition, the hERG channel folded into our biomimetic membrane platform was used for probing the channel and drug interactions through fluorescence polarization (FP) assay. Our results suggest that the biomimetic system employed is capable of detecting the interaction between hERG and different channel blockers at varied concentrations. We believe that our current approach could be applied to other membrane proteins for drug screening or other protein-related interactions.

Graphical abstract: Biomimetic membrane platform containing hERG potassium channel and its application to drug screening

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Publication details

The article was received on 20 Aug 2012, accepted on 19 Jan 2013 and first published on 21 Jan 2013


Article type: Paper
DOI: 10.1039/C3AN36159D
Citation: Analyst, 2013,138, 2007-2012
  • Open access: Creative Commons BY-NC license
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    Biomimetic membrane platform containing hERG potassium channel and its application to drug screening

    A. Arslan Yildiz, C. Kang and E. Sinner, Analyst, 2013, 138, 2007
    DOI: 10.1039/C3AN36159D

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