Functional properties of a truncated recombinant GIRK5 potassium channel

Biochim Biophys Acta. 2001 May 2;1512(1):135-47. doi: 10.1016/s0005-2736(01)00314-5.

Abstract

Xenopus laevis oocytes codify a G-protein-activated inward rectifier potassium channel (GIRK5 or Kir3.5). Coinjection of other GIRKs, the muscarinic m2 receptor, or Gbetagamma protein cRNAs is required to observe functional GIRKx-GIRK5 heteromultimers in oocytes. Studies with GIRK2 isoforms have shown that the size of the amino or carboxyl terminus plays a crucial role on giving functional K(+) channels. In this work we studied the properties of a GIRK5 with 25 amino acids deleted toward its amino-terminal domain. Injection of GIRK5-Delta25 cRNA alone displayed large basal and transient inward rectifying currents in oocytes. The instantaneous currents reached a stationary level after a long duration voltage pulse (10 s). For this relaxation, fast (tau(1)) and slow (tau(2)) time constants were estimated at different voltages. Recovery from inactivation followed a monoexponential function (tau=0.95+/-0.07 s). By contrast with other inward rectifier channels, blockade of GIRK5-Delta25 by extracellular Ba(2+) was voltage-independent (K(d)=102+/-2 microM), suggesting the presence of a Ba(2+) site at the external channel vestibule. To confirm this hypothesis, the Ba(2+) sensitivity of two charged mutants GIRK5-Delta25(N129E) and GIRK5-Delta25(K157E) at each of the external loops was determined. GIRK5-Delta25(N129E) and GIRK5-Delta25(K157E) showed a 100-fold and 2-fold higher affinity to Ba(2+), respectively, supporting the existence of this Ba(2+) binding site.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Barium / chemistry
  • Barium / metabolism
  • Barium Compounds / pharmacology
  • Binding Sites
  • Cations, Divalent
  • Chlorides / pharmacology
  • Electrophysiology
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • Mutation
  • Oocytes / metabolism*
  • Potassium Channel Blockers
  • Potassium Channels / genetics
  • Potassium Channels / metabolism*
  • Potassium Channels, Inwardly Rectifying*
  • Protein Isoforms / metabolism
  • Recombinant Proteins / metabolism
  • Static Electricity
  • Transfection
  • Xenopus laevis

Substances

  • Barium Compounds
  • Cations, Divalent
  • Chlorides
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Inwardly Rectifying
  • Protein Isoforms
  • Recombinant Proteins
  • barium chloride
  • Barium