Description
Experimental Technique/Method:X-RAY DIFFRACTION
Resolution:3.01
Classification:IMMUNE SYSTEM/TRANSPORT PROTEIN
Release Date:2005-04-27
Deposition Date:2005-04-09
Revision Date:2011-05-08#2011-07-13#2017-07-12
Molecular Weight:61126.19
Macromolecule Type:Protein
Residue Count:555
Atom Site Count:4096
DOI:10.2210/pdb2boc/pdb
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.
Resolution:3.01
Classification:IMMUNE SYSTEM/TRANSPORT PROTEIN
Release Date:2005-04-27
Deposition Date:2005-04-09
Revision Date:2011-05-08#2011-07-13#2017-07-12
Molecular Weight:61126.19
Macromolecule Type:Protein
Residue Count:555
Atom Site Count:4096
DOI:10.2210/pdb2boc/pdb
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.
| Date made available | 2005 |
|---|---|
| Publisher | RCSB-PDB |