Potassium-selective block of barium permeation through single KcsA channels

J Gen Physiol. 2011 Oct;138(4):421-36. doi: 10.1085/jgp.201110684. Epub 2011 Sep 12.

Abstract

Ba(2+), a doubly charged analogue of K(+), specifically blocks K(+) channels by virtue of electrostatic stabilization in the permeation pathway. Ba(2+) block is used here as a tool to determine the equilibrium binding affinity for various monovalent cations at specific sites in the selectivity filter of a noninactivating mutant of KcsA. At high concentrations of external K(+), the block-time distribution is double exponential, marking at least two Ba(2+) sites in the selectivity filter, in accord with a Ba(2+)-containing crystal structure of KcsA. By analyzing block as a function of extracellular K(+), we determined the equilibrium dissociation constant of K(+) and of other monovalent cations at an extracellular site, presumably S1, to arrive at a selectivity sequence for binding at this site: Rb(+) (3 µM) > Cs(+) (23 µM) > K(+) (29 µM) > NH(4)(+) (440 µM) >> Na(+) and Li(+) (>1 M). This represents an unusually high selectivity for K(+) over Na(+), with |ΔΔG(0)| of at least 7 kcal mol(-1). These results fit well with other kinetic measurements of selectivity as well as with the many crystal structures of KcsA in various ionic conditions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacterial Proteins / genetics
  • Bacterial Proteins / metabolism*
  • Barium / metabolism*
  • Binding Sites
  • Cell Membrane / physiology*
  • Cesium
  • Dose-Response Relationship, Drug
  • Escherichia coli / genetics
  • Escherichia coli / metabolism*
  • Gene Expression Regulation, Bacterial
  • Mutagenesis, Site-Directed
  • Mutation
  • Permeability
  • Potassium / metabolism*
  • Potassium Channels, Voltage-Gated / genetics
  • Potassium Channels, Voltage-Gated / metabolism*
  • Quaternary Ammonium Compounds
  • Rubidium

Substances

  • Bacterial Proteins
  • KcsA protein, Streptomyces coelicolor
  • Potassium Channels, Voltage-Gated
  • Quaternary Ammonium Compounds
  • Cesium
  • Barium
  • Rubidium
  • Potassium