ArticleJournal of chemical information and modeling2010
Modeling anesthetic binding sites within the glycine alpha one receptor based on prokaryotic ion channel templates: the problem with TM4.
Article in Journal of chemical information and modeling, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- The neural γJournal of molecular modeling · 2018Article
- Inter- and Intra-Subunit Butanol/Isoflurane Sites of Action in the Human Glycine Receptor.Frontiers in molecular neuroscience · 2016Article
- Ethanol effects on glycinergic transmission: From molecular pharmacology to behavior responses.Pharmacological research · 2015Review
- Alcohol dependence: molecular and behavioral evidence.Trends in pharmacological sciences · 2014Review
- Structural models of ligand-gated ion channels: sites of action for anesthetics and ethanol.Alcoholism, clinical and experimental research · 2014Review
- GABA(A) receptor transmembrane amino acids are critical for alcohol action: disulfide cross-linking and alkyl methanethiosulfonate labeling reveal relative location of binding sites.Journal of neurochemistry · 2014Article
- How drugs get into cells: tested and testable predictions to help discriminate between transporter-mediated uptake and lipoidal bilayer diffusion.Frontiers in pharmacology · 2014Review
- Propofol modulation of α1 glycine receptors does not require a structural transition at adjacent subunits that is crucial to agonist-induced activation.ACS chemical neuroscience · 2013Article
- Assessment of homology templates and an anesthetic binding site within the γ-aminobutyric acid receptor.Anesthesiology · 2013Article
- Identification of propofol binding sites in a nicotinic acetylcholine receptor with a photoreactive propofol analog.The Journal of biological chemistry · 2013Article
- Reversal of ion-charge selectivity renders the pentameric ligand-gated ion channel GLIC insensitive to anaesthetics.The Biochemical journal · 2013Article
- Induced changes in protein receptors conferring resistance to anesthetics.Current opinion in anaesthesiology · 2012Review
- Teaching an old GABA receptor new tricks.Anesthesia and analgesia · 2012Review
- Charge and geometry of residues in the loop 2 β hairpin differentially affect agonist and ethanol sensitivity in glycine receptors.The Journal of pharmacology and experimental therapeutics · 2012Article
- Mapping general anesthetic binding site(s) in human α1β3 γ-aminobutyric acid type A receptors with [³H]TDBzl-etomidate, a photoreactive etomidate analogue.Biochemistry · 2012Article
- Molecular determinants of ivermectin sensitivity at the glycine receptor chloride channel.The Journal of biological chemistry · 2011Article
- Alcohol-binding sites in distinct brain proteins: the quest for atomic level resolution.Alcoholism, clinical and experimental research · 2011Review
- A Single phenylalanine residue in the main intracellular loop of α1 γ-aminobutyric acid type A and glycine receptors influences their sensitivity to propofol.Anesthesiology · 2011Article
- Functional prokaryotic-eukaryotic chimera from the pentameric ligand-gated ion channel family.Proceedings of the National Academy of Sciences of the United States of America · 2011Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
Ligand-gated ion channels (LGICs) significantly modulate anesthetic effects. Their exact molecular structure remains unknown. This has led to ambiguity regarding the proper amino acid alignment within their 3D structure and, in turn, the location of any anesthetic binding sites. Current controversies suggest that such a site could be located in either an intra- or intersubunit locale within the transmembrane domain of the protein. Here, we built a model of the glycine alpha one receptor (GlyRa1) based on the open-state structures of two new high-resolution ion channel templates from the prokaryote, Gloebacter violaceus (GLIC). Sequence scoring suggests reasonable homology between GlyRa1 and GLIC. Three of the residues notable for modulating anesthetic action are on transmembrane segments 1-3 (TM1-3): (ILE229, SER 267, and ALA 288). They line an intersubunit interface, in contrast to previous models. However, residues from the fourth transmembrane domain (TM4) that are known to modulate a variety of anesthetic effects are quite distant from this putative anesthetic binding site. While this model can account for a large proportion of the physicochemical data regarding such proteins, it cannot readily account for the alterations on anesthetic effects that are due to mutations within TM4.
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Registered trials
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