Mechanisms of the inhibition of Shaker potassium channels by protons

Pflugers Arch. 2003 Oct;447(1):44-54. doi: 10.1007/s00424-003-1121-0. Epub 2003 Aug 12.

Abstract

Potassium channels are regulated by protons in various ways and, in most cases, acidification results in potassium current reduction. To elucidate the mechanisms of proton-channel interactions we investigated N-terminally truncated Shaker potassium channels (Kv1 channels) expressed in Xenopus oocytes, varying pH at the intracellular and the extracellular face of the membrane. Intracellular acidification resulted in rapid and reversible channel block. The block was half-maximal at pH 6.48, thus even physiological excursions of intracellular pH will have an impact on K+ current. The block displayed only very weak voltage dependence and C-type inactivation and activation were not affected. Extracellular acidification (up to pH 4) did not block the channel, indicating that protons are effectively excluded from the selectivity filter. Channel current, however, was reduced greatly due to marked acceleration of C-type inactivation at low pH. In contrast, inactivation was not affected in the T449V mutant channel, in which C-type inactivation is impaired. The pH effect on inactivation of the wild-type channel had an apparent pK of 4.7, suggesting that protonation of extracellular acidic residues in Kv channels makes them subject to pH regulation.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Female
  • Ion Channel Gating / drug effects
  • Ion Channel Gating / physiology
  • Potassium Channel Blockers* / pharmacology
  • Potassium Channels / physiology*
  • Protons*
  • Shaker Superfamily of Potassium Channels
  • Xenopus

Substances

  • Potassium Channel Blockers
  • Potassium Channels
  • Protons
  • Shaker Superfamily of Potassium Channels