ArticleProceedings of the National Academy of Sciences of the United States of America2000
Activation and inhibition of G protein-coupled inwardly rectifying potassium (Kir3) channels by G protein beta gamma subunits.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 86 citations in OpenAlex.
- Article
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- Pacemaker Channels and the Chronotropic Response in Health and Disease.Circulation research · 2024Review
- Bioengineered peptibodies as blockers of ion channels.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Discovery, synthesis and biological characterization of a series ofRSC medicinal chemistry · 2021Article
- Adaptive thermogenesis in brown adipose tissue involves activation of pannexin-1 channels.Molecular metabolism · 2021Article
- Structural mechanism underlying G protein family-specific regulation of G protein-gated inwardly rectifying potassium channel.Nature communications · 2019Article
- Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.ACS chemical neuroscience · 2019Article
- GPCR regulation of secretion.Pharmacology & therapeutics · 2018Review
- Knockdown of cardiac Kir3.1 gene with siRNA can improve bradycardia in an experimental sinus bradycardia rat model.Molecular and cellular biochemistry · 2017Article
- Dopamine Receptor Signaling in MIN6 β-Cells Revealed by Fluorescence Fluctuation Spectroscopy.Biophysical journal · 2016Article
- 60 YEARS OF POMC: Regulation of feeding and energy homeostasis by α-MSH.Journal of molecular endocrinology · 2016Review
- Kir3 channel ontogeny - the role of Gβγ subunits in channel assembly and trafficking.Frontiers in cellular neuroscience · 2014Article
- GPCR mediated regulation of synaptic transmission.Progress in neurobiology · 2012Review
- Estrogen regulation of the dopamine-activated GIRK channel in pituitary lactotrophs: implications for regulation of prolactin release during the estrous cycle.American journal of physiology. Regulatory, integrative and comparative physiology · 2011Article
- A Simple, Highly Efficient Method for Heterologous Expression in Mammalian Primary Neurons Using Cationic Lipid-mediated mRNA Transfection.Frontiers in neuroscience · 2010Article
- Shuttling and translocation of heterotrimeric G proteins and Ras.Trends in pharmacological sciences · 2009Review
- Molecular mechanisms of go signaling.Neuro-Signals · 2009Review
- Differential dissociation of G protein heterotrimers.The Journal of physiology · 2008Article
- Abscisic acid regulation of guard-cell K+ and anion channels in Gbeta- and RGS-deficient Arabidopsis lines.Proceedings of the National Academy of Sciences of the United States of America · 2008Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
G protein-coupled inwardly rectifying potassium (GIRK) channels can be activated or inhibited by different classes of receptors, suggesting a role for G proteins in determining signaling specificity. Because G protein betagamma subunits containing either beta1 or beta2 with multiple Ggamma subunits activate GIRK channels, we hypothesized that specificity might be imparted by beta3, beta4, or beta5 subunits. We used a transfection assay in cell lines expressing GIRK channels to examine effects of dimers containing these Gbeta subunits. Inwardly rectifying K(+) currents were increased in cells expressing beta3 or beta4, with either gamma2 or gamma11. Purified, recombinant beta3gamma2 and beta4gamma2 bound directly to glutathione-S-transferase fusion proteins containing N- or C-terminal cytoplasmic domains of GIRK1 and GIRK4, indicating that beta3 and beta4, like beta1, form dimers that bind to and activate GIRK channels. By contrast, beta5-containing dimers inhibited GIRK channel currents. This inhibitory effect was obtained with either beta5gamma2 or beta5gamma11, was observed with either GIRK1,4 or GIRK1,2 channels, and was evident in the context of either basal or agonist-induced currents, both of which were mediated by endogenous Gbetagamma subunits. In cotransfection assays, beta5gamma2 suppressed beta1gamma2-activated GIRK currents in a dose-dependent manner consistent with competitive inhibition. Moreover, we found that beta5gamma2 could bind to the same GIRK channel cytoplasmic domains as other, activating Gbetagamma subunits. Thus, beta5-containing dimers inhibit Gbetagamma-stimulated GIRK channels, perhaps by directly binding to the channels. This suggests that beta5-containing dimers could act as competitive antagonists of other Gbetagamma dimers on GIRK channels.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.