ArticleProceedings of the National Academy of Sciences of the United States of America2002
Graded contribution of the Gbeta gamma binding domains to GIRK channel activation.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Live-cell quantitative monitoring reveals distinct, high-affinity Gβγ regulations of GIRK2 and GIRK1/2 channels.Nature communications · 2025Article
- Live-cell quantitative monitoring reveals distinct, high-affinity Gβγ regulations of GIRK2 and GIRK1/2 channels.bioRxiv : the preprint server for biology · 2025Article
- Direct modulation of G protein-gated inwardly rectifying potassium (GIRK) channels.Frontiers in physiology · 2024Review
- Neuronal G protein-gated KAmerican journal of physiology. Cell physiology · 2022Review
- Encephalopathy-causing mutations in GβiScience · 2021Article
- A biochemical mechanism for time-encoding memory formation within individual synapses of Purkinje cells.PloS one · 2021Article
- A Collision Coupling Model Governs the Activation of Neuronal GIRK1/2 Channels by Muscarinic-2 Receptors.Frontiers in pharmacology · 2020Article
- Highlights for the 6th International Ion Channel Conference: ion channel structure, function, disease and therapeutics.Acta pharmaceutica Sinica. B · 2017Article
- KCTD Hetero-oligomers Confer Unique Kinetic Properties on Hippocampal GABAB Receptor-Induced K+ Currents.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2017Article
- Emergence of ion channel modal gating from independent subunit kinetics.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- A Quantitative Model of the GIRK1/2 Channel Reveals That Its Basal and Evoked Activities Are Controlled by Unequal Stoichiometry of Gα and Gβγ.PLoS computational biology · 2015Article
- Two distinct aspects of coupling between Gα(i) protein and G protein-activated K+ channel (GIRK) revealed by fluorescently labeled Gα(i3) protein subunits.The Journal of biological chemistry · 2011Article
- G protein {beta}{gamma} gating confers volatile anesthetic inhibition to Kir3 channels.The Journal of biological chemistry · 2010Article
- Astrocytes as gatekeepers of GABAB receptor function.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2010Article
- G alpha(i) and G betagamma jointly regulate the conformations of a G betagamma effector, the neuronal G protein-activated K+ channel (GIRK).The Journal of biological chemistry · 2010Article
- Generation of a constitutive Na+-dependent inward-rectifier current in rat adult atrial myocytes by overexpression of Kir3.4.The Journal of physiology · 2007Article
- Modulation of midbrain dopamine neurotransmission by serotonin, a versatile interaction between neurotransmitters and significance for antipsychotic drug action.Current neuropharmacology · 2006Article
- Spinal G-protein-gated potassium channels contribute in a dose-dependent manner to the analgesic effect of mu- and delta- but not kappa-opioids.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2005Article
- Kinetic modeling of Na(+)-induced, Gbetagamma-dependent activation of G protein-gated K(+) channels.Journal of molecular neuroscience : MN · 2005Article
- The calcium-sensing receptor and its interacting proteins.Journal of cellular and molecular medicineReview
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Authors and funding
3 authors.
Funding
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Abstract
G protein coupled inwardly rectifying K(+) channels (GIRK/Kir3.x) are mainly activated by a direct interaction with Gbetagamma subunits, released upon the activation of inhibitory neurotransmitter receptors. Although Gbetagamma binding domains on all four subunits have been found, the relative contribution of each of these binding sites to channel gating has not yet been defined. It is also not known whether GIRK channels open once all Gbetagamma sites are occupied, or whether gating is a graded process. We used a tandem tetrameric approach to enable the selective elimination of specific Gbetagamma binding domains in the tetrameric context. Here, we show that tandem tetramers are fully operational. Tetramers with only one wild-type channel subunit showed receptor-independent high constitutive activity. The presence of two or three wild-type subunits reconstituted receptor activation gradually. Furthermore, a tetramer with no GIRK1 Gbetagamma binding domain displayed slower kinetics of activation. The slowdown in activation was found to be independent of regulator of G protein signaling or receptor coupling, but this slowdown could be reversed once only one Gbetagamma binding domain of GIRK1 was added. These results suggest that partial activation can occur under low Gbetagamma occupancy and that full activation can be accomplished by the interaction with three Gbetagamma binding subunits.
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