Screening blockers against a potassium channel with a droplet interface bilayer array

J Am Chem Soc. 2008 Nov 19;130(46):15543-8. doi: 10.1021/ja804968g. Epub 2008 Oct 25.

Abstract

Droplet interface bilayers (DIBs) form between two lipid monolayer-encased aqueous droplets submerged in oil. Both major structural classes of membrane proteins, alpha-helix bundles and beta barrels, represented by channels and pores, respectively, spontaneously insert into DIBs when freshly expressed by cell-free transcription and translation. Electrodes embedded within the droplets allow the measurement of transmembrane ionic currents carried by individual channels and pores. On the basis of these findings, we have devised a chip-based approach for the rapid screening of blockers against ion channels. The technique is demonstrated here with the viral potassium channel, Kcv.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacterial Toxins / chemistry
  • Bacterial Toxins / genetics
  • Bacterial Toxins / metabolism
  • Cell-Free System
  • Drug Evaluation, Preclinical
  • Hemolysin Proteins / chemistry
  • Hemolysin Proteins / genetics
  • Hemolysin Proteins / metabolism
  • Lipid Bilayers / chemistry*
  • Microchip Analytical Procedures
  • Potassium Channel Blockers / chemistry*
  • Potassium Channels / chemistry*
  • Potassium Channels / metabolism
  • Time Factors

Substances

  • Bacterial Toxins
  • Hemolysin Proteins
  • Lipid Bilayers
  • Potassium Channel Blockers
  • Potassium Channels
  • staphylococcal alpha-toxin