Three-Dimensional Control of Ion Channel Function through Optogenetics and Co-Culture

SLAS Discov. 2018 Jan;23(1):102-108. doi: 10.1177/2472555217722990. Epub 2017 Aug 7.


The lack of miniaturized and cost-effective methods to control cellular excitability with dosable and temporally precise electrical perturbations represents a long-lasting and unsolved bottleneck for ion channel drug discovery pipelines. Here we developed a high-throughput-compatible fluorescent-based cellular assay that combines optogenetics and co-culture approaches to obtain spatial, temporal, and quantitative control of ion channel activity. The modularity and increased flexibility of control of this light-tandem assay, combined with contained costs and compatibility with conventional drug-screening platforms, make this system suitable for temporally precise screening of ion channel function in controlled conformations and can also be used to recapitulate other complexly regulated biological processes.

Keywords: FLIPR; high-throughput screening; ion channels; optogenetics; syncytium.

MeSH terms

  • Calcium Channels, L-Type / chemistry
  • Cell Line
  • Coculture Techniques
  • Drug Discovery / methods*
  • High-Throughput Screening Assays*
  • Humans
  • Ion Channels / agonists
  • Ion Channels / antagonists & inhibitors
  • Ion Channels / chemistry*
  • Kinetics
  • Ligands
  • Optogenetics / methods*


  • Calcium Channels, L-Type
  • Ion Channels
  • Ligands