Medizinische Universität Graz - Research portal
Selected Publication:
Schreibmayer, W; Dessauer, CW; Vorobiov, D; Gilman, AG; Lester, HA; Davidson, N; Dascal, N.
Inhibition of an inwardly rectifying K+ channel by G-protein alpha-subunits.
NATURE. 1996; 380(6575): 624-627.
Doi: 10.1038/380624a0
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- Leading authors Med Uni Graz
- Schreibmayer Wolfgang
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- Abstract:
- Cholinergic muscarinic, serotonergic, opioid and several other G-protein-coupled neurotransmitter receptors activate inwardly rectifying K+ channels of the GIRK family, slowing the heartbeat and decreasing the excitability of neuronal cells. Inhibitory modulation of GIRKs by G-protein-coupled receptors may have important implications in cardiac and brain physiology. Previously G alpha and G beta gamma subunits of heterotrimeric G proteins have both been implicated in channel opening, but recent studies attribute this role primarily to the G beta gamma dimer that activates GIRKs in a membrane-delimited fashion, probably by direct binding to the channel protein. We report here that free GTP gamma S-activated G alpha i 1, but not G alpha i 2 or G alpha i 3, potently inhibits G beta 1 gamma 2-induced GIRK activity in excised membrane patches of Xenopus oocytes expressing GIRK1. High-affinity but partial inhibition is produced by G alpha s-GTP gamma S. G alpha i 1-GTP gamma S also inhibits G beta 1 gamma 2-activated GIRK in atrial myocytes. Antagonistic interactions between G alpha and G beta gamma may be among the mechanisms determining specificity of G protein coupling to GIRKs.
- Find related publications in this database (using NLM MeSH Indexing)
- Animals -
- Base Sequence -
- Cattle -
- Cells, Cultured -
- G Protein-Coupled Inwardly-Rectifying Potassium Channels -
- GTP-Binding Proteins - metabolism
- Guanosine 5'-O-(3-Thiotriphosphate) - metabolism
- Humans - metabolism
- Ion Channel Gating - metabolism
- Molecular Sequence Data - metabolism
- Myocardium - cytology
- Oligonucleotides, Antisense - pharmacology
- Oocytes - pharmacology
- Potassium Channel Blockers - pharmacology
- Potassium Channels - genetics
- Potassium Channels, Inwardly Rectifying - genetics
- Rats - genetics
- Recombinant Proteins - metabolism
- Xenopus - metabolism