ArticleThe Journal of pharmacology and experimental therapeutics2009
Blockade of ethanol-induced potentiation of glycine receptors by a peptide that interferes with Gbetagamma binding.
Article in The Journal of pharmacology and experimental therapeutics, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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Who cites it
19 citing papers in PubMed, 21 citations in OpenAlex.
- Conformational transitions and allosteric modulation in a heteromeric glycine receptor.Nature communications · 2023Article
- Structures of highly flexible intracellular domain of human α7 nicotinic acetylcholine receptor.Nature communications · 2022Article
- Presence of ethanol-sensitive and ethanol-insensitive glycine receptors in the ventral tegmental area and prefrontal cortex in mice.British journal of pharmacology · 2021Article
- Presence of ethanol-sensitive glycine receptors in medium spiny neurons in the mouse nucleus accumbens.The Journal of physiology · 2017Article
- The ClusPro web server for protein-protein docking.Nature protocols · 2017Article
- Reversal of Ethanol-induced Intoxication by a Novel Modulator of Gβγ Protein Potentiation of the Glycine Receptor.The Journal of biological chemistry · 2016Article
- Potentiation of Gamma Aminobutyric Acid Receptors (GABAAR) by Ethanol: How Are Inhibitory Receptors Affected?Frontiers in cellular neuroscience · 2016Review
- Ethanol effects on glycinergic transmission: From molecular pharmacology to behavior responses.Pharmacological research · 2015Review
- Control of ethanol sensitivity of the glycine receptor α3 subunit by transmembrane 2, the intracellular splice cassette and C-terminal domains.The Journal of pharmacology and experimental therapeutics · 2015Article
- Evidence for α-helices in the large intracellular domain mediating modulation of the α1-glycine receptor by ethanol and Gβγ.The Journal of pharmacology and experimental therapeutics · 2015Article
- Altered sedative effects of ethanol in mice with α1 glycine receptor subunits that are insensitive to Gβγ modulation.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2014Article
- Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel.Nature communications · 2013Article
- Inhibition of the ethanol-induced potentiation of α1 glycine receptor by a small peptide that interferes with Gβγ binding.The Journal of biological chemistry · 2012Article
- Introduction to the special issue "Pharmacotherapies for the treatment of alcohol abuse and dependence" and a summary of patents targeting other neurotransmitter systems.Recent patents on CNS drug discovery · 2012Article
- Ethanol alters opioid regulation of Ca(2+) influx through L-type Ca(2+) channels in PC12 cells.Alcoholism, clinical and experimental research · 2012Article
- The TM2 6' position of GABA(A) receptors mediates alcohol inhibition.The Journal of pharmacology and experimental therapeutics · 2012Article
- Activated G protein α s subunits increase the ethanol sensitivity of human glycine receptors.The Journal of pharmacology and experimental therapeutics · 2011Article
- Identification of novel specific allosteric modulators of the glycine receptor using phage display.The Journal of biological chemistry · 2010Article
- Molecular targets and mechanisms for ethanol action in glycine receptors.Pharmacology & therapeutics · 2010Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
The large intracellular loop (IL) of the glycine receptor (GlyR) interacts with various signaling proteins and plays a fundamental role in trafficking and regulation of several receptor properties, including a direct interaction with Gbetagamma. In the present study, we found that mutation of basic residues in the N-terminal region of the IL reduced the binding of Gbetagamma to 21 +/- 10% of control. Two basic residues in the C-terminal region, on the other hand, contributed to a smaller extent to Gbetagamma binding. Using docking analysis, we found that both basic regions of the IL bind in nearby regions to the Gbetagamma dimer, within an area of high density of amino acids having an electronegative character. Thereafter, we generated a 17-amino acid peptide with the N-terminal sequence of the wild-type IL (RQH) that was able to inhibit the in vitro binding of Gbetagamma to GlyRs to 57 +/- 5% of control in glutathione S-transferase pull-down assays using purified proteins. More interestingly, when the peptide was intracellularly applied to human embryonic kidney 293 cells, it inhibited the Gbetagamma-mediated modulations of G protein-coupled inwardly rectifying potassium channel by baclofen (24 +/- 14% of control) and attenuated the GlyR potentiation by ethanol (51 +/- 10% versus 10 +/- 3%).
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Registered trials
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.