Structural basis of TEA blockade in a model potassium channel

Michael J. Lenaeus, Magdalini Vamvouka, Pamela J. Focia, Adrian Gross*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

110 Scopus citations

Abstract

Potassium channels catalyze the selective transfer of potassium across the cell membrane and are essential for setting the resting potential in cells, controlling heart rate and modulating the firing pattern in neurons. Tetraethylammonium (TEA) blocks ion conduction through potassium channels in a voltage-dependent manner from both sides of the membrane. Here we show the structural basis of TEA blockade by cocrystallizing the prokaryotic potassium channel KcsA with two selective TEA analogs. TEA binding at both sites alters ion occupancy in the selectivity filter; these findings underlie the mutual destabilization and voltage-dependence of TEA blockade. We propose that TEA blocks potassium channels by acting as a potassium analog at the dehydration transition step during permeation.

Original languageEnglish (US)
Pages (from-to)454-459
Number of pages6
JournalNature Structural and Molecular Biology
Volume12
Issue number5
DOIs
StatePublished - May 2005

ASJC Scopus subject areas

  • Structural Biology
  • Molecular Biology

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