Signalling via the G protein-activated K+ channels

Cell Signal. 1997 Dec;9(8):551-73. doi: 10.1016/s0898-6568(97)00095-8.


The inwardly rectifying K+ channels of the GIRK (Kir3) family, members of the superfamily of inwardly rectifying K+ channels (Kir), are important physiological tools to regulate excitability in heart and brain by neurotransmitters, and the only ion channels conclusively shown to be activated by a direct interaction with heterotrimeric G protein subunits. During the last decade, especially since their cloning in 1993, remarkable progress has been made in understanding the structure, mechanisms of gating, activation by G proteins, and modulation of these channels. However, much of the molecular details of structure and of gating by G protein subunits and other factors, mechanisms of modulation and desensitization, and determinants of specificity of coupling to G proteins, remain unknown. This review summarizes both the recent advances and the unresolved questions now on the agenda in GIRK studies.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • GTP-Binding Proteins / metabolism*
  • Humans
  • Ion Channel Gating
  • Models, Molecular
  • Molecular Sequence Data
  • Potassium Channels / chemistry
  • Potassium Channels / metabolism*
  • Potassium Channels, Inwardly Rectifying*
  • Protein Conformation
  • Signal Transduction*
  • Structure-Activity Relationship


  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • Potassium Channels
  • Potassium Channels, Inwardly Rectifying
  • GTP-Binding Proteins