Genomes and Genes
Gene Symbol: GLRA3
Description: glycine receptor alpha 3
Alias: glycine receptor subunit alpha-3, glycine receptor, alpha-3 polypeptide, ligand gated ion channel
Publications115 found, 100 shown here
- Musgrave I, Hughes R. Investigation of I1-imidazoline receptors using microphysiometry and molecular modelling. J Auton Nerv Syst. 1998;72:137-46 pubmed..This suggests that a phencyclidine-binding site motif may represent a novel site of action for I1-site ligands, and a search for receptors based on this motif may reveal novel imidazoline 'receptors'...
- Yang J, Yang S, Na J, Hahn H, Cho S. 3-(Naphthalen-2-yl(propoxy)methyl)azetidine hydrochloride attenuates NLRP3 inflammasome-mediated signaling pathway in lipopolysaccharide-stimulated BV2 microglial cells. Biochem Biophys Res Commun. 2018;495:151-156 pubmed publisher..Our results suggest that the anti-inflammatory functions of KHG26792 may be, at least in part, due to regulation of the P2X7R/NLRP3-mediated signaling pathway during microglial activation. ..
- Danquah W, Meyer Schwesinger C, Rissiek B, Pinto C, Serracant Prat A, Amadi M, et al. Nanobodies that block gating of the P2X7 ion channel ameliorate inflammation. Sci Transl Med. 2016;8:366ra162 pubmed..Our results show that nanobody technology can generate potent, specific therapeutics against ion channels, confirm P2X7 as a therapeutic target for inflammatory disorders, and characterize a potent new drug candidate that targets P2X7. ..
- Horvath G, Otrokocsi L, Bekő K, Baranyi M, Kittel A, Fritz Ruenes P, et al. P2X7 Receptors Drive Poly(I:C) Induced Autism-like Behavior in Mice. J Neurosci. 2019;39:2542-2561 pubmed publisher..This is the first report showing the key role of a ligand gated ion channel, the purinergic P2X7 receptor in MIA-induced autism-like behavioral and biochemical features...
- Walsh R, Roh S, Gharpure A, Morales Perez C, Teng J, Hibbs R. Structural principles of distinct assemblies of the human α4β2 nicotinic receptor. Nature. 2018;557:261-265 pubmed publisher..The results reveal principles of subunit assembly and the structural basis of the distinctive biophysical and pharmacological properties of the two different stoichiometries of this receptor. ..
- Gao H, Li D, Yang P, Zhao L, Wei L, Chen Y, et al. Suppression of CD36 attenuates adipogenesis with a reduction of P2X7 expression in 3T3-L1 cells. Biochem Biophys Res Commun. 2017;491:204-208 pubmed publisher..In addition, purinergic receptor P2X, ligand-gated ion channel 7 (P2X7) was downregulated in CD36-knockdown 3T3-L1 cells, suggesting that the suppression of CD36 attenuates adipogenesis via the P2X7 pathway in 3T3-L1 cells. ..
- Rienzo M, Lummis S, Dougherty D. Structural requirements in the transmembrane domain of GLIC revealed by incorporation of noncanonical histidine analogs. Chem Biol. 2014;21:1700-6 pubmed publisher..In contrast, our data show that two other His residues are not involved in the acid-sensing mechanism. ..
- Brackley A, Gomez R, Guerrero K, Akopian A, Glucksman M, Du J, et al. A-Kinase Anchoring Protein 79/150 Scaffolds Transient Receptor Potential A 1 Phosphorylation and Sensitization by Metabotropic Glutamate Receptor Activation. Sci Rep. 2017;7:1842 pubmed publisher..Collectively, these results identify a novel AKAP-mediated biochemical mechanism that increases TRPA1 sensitivity in peripheral sensory neurons, and likely contributes to persistent mechanical hypersensitivity. ..
- Helley M, Abate W, Jackson S, Bennett J, Thompson S. The expression of Toll-like receptor 4, 7 and co-receptors in neurochemical sub-populations of rat trigeminal ganglion sensory neurons. Neuroscience. 2015;310:686-98 pubmed publisher..Together, our results show that nociceptors express the molecular machinery required to directly respond to pathogenic challenge independently from the innate immune system. ..
- Ma K, Qian Y. Alpha 7 nicotinic acetylcholine receptor and its effects on Alzheimer's disease. Neuropeptides. 2019;73:96-106 pubmed publisher..Finally, we stressed the AD therapy that targets the α7 nAChR. ..
- Jones A, Buckingham S, Brown L, Sattelle D. Alternative splicing of the Anopheles gambiae nicotinic acetylcholine receptor, Agamalphabeta9, generates both alpha and beta subunits. Invert Neurosci. 2009;9:77-84 pubmed publisher..Our findings further characterise a potential target to control the malaria mosquito as well as provide insights into the diversification of nAChRs. ..
- Newcombe J, Chatzidaki A, Sheppard T, Topf M, Millar N. Diversity of Nicotinic Acetylcholine Receptor Positive Allosteric Modulators Revealed by Mutagenesis and a Revised Structural Model. Mol Pharmacol. 2018;93:128-140 pubmed publisher..Thus, our revised structural models may provide a useful tool for interpreting functional effects of PAMs. ..
- Nys M, Wijckmans E, Farinha A, Yoluk O, Andersson M, Brams M, et al. Allosteric binding site in a Cys-loop receptor ligand-binding domain unveiled in the crystal structure of ELIC in complex with chlorpromazine. Proc Natl Acad Sci U S A. 2016;113:E6696-E6703 pubmed..Our results extend on previous observations and further substantiate our understanding of a multisite model for allosteric modulation of Cys-loop receptors. ..
- Wang W, Perens E, Oikonomou G, Wallace S, Lu Y, Shaham S. IGDB-2, an Ig/FNIII protein, binds the ion channel LGC-34 and controls sensory compartment morphogenesis in C. elegans. Dev Biol. 2017;430:105-112 pubmed publisher..Our findings reveal a novel membrane protein complex and suggest possible mechanisms for how sensory compartment size is controlled. ..
- Wang Y, Zhang Y, Li W, Han Y, Guo B. Study on neurotoxicity of dinotefuran, thiamethoxam and imidacloprid against Chinese lizards (Eremias argus). Chemosphere. 2019;217:150-157 pubmed publisher..This study provided a new perspective on the neotoxic effects of neonicotinoids. ..
- Balsera B, Mulet J, FernÃ¡ndez Carvajal A, de la Torre MartÃnez R, Ferrer Montiel A, HernÃ¡ndez JimÃ©nez J, et al. Chalcones as positive allosteric modulators of Î±7 nicotinic acetylcholine receptors: a new target for a privileged structure. Eur J Med Chem. 2014;86:724-39 pubmed publisher..The most potent compound (2,4,2',5'-tetrahydroxychalcone, 111) was further characterized showing its potential as neuroprotective, analgesic and cognitive enhancer, opening the way for future developments around the chalcone structure. ..
- Kabbani N, Nichols R. Beyond the Channel: Metabotropic Signaling by Nicotinic Receptors. Trends Pharmacol Sci. 2018;39:354-366 pubmed publisher..Delineation of the ionotropic and metabotropic properties of the α7 nAChR will provide definitive indicators of moment-to-moment receptor functional status that will, in turn, spearhead new drug development. ..
- Fletcher E. 2016 Glenn A. Fry Award Lecture: Mechanisms and Potential Treatments of Early Age-Related Macular Degeneration. Optom Vis Sci. 2017;94:939-945 pubmed publisher..By understanding the fundamental cell biological changes that occur in patients and animal models of disease, we have uncovered mechanisms that may help us manage and treat patients in the future. ..
- Gottschald Chiodi C, Baptista Hon D, Hunter W, Hales T. Amino acid substitutions in the human homomeric β3 GABAA receptor that enable activation by GABA. J Biol Chem. 2019;294:2375-2385 pubmed publisher..This work demonstrated that only two substitutions, Q89R and G152T, in β3 GABAAR are sufficient to reconstitute GABA-mediated activation and suggests that Tyr87 prevents inhibitory effects of GABA. ..
- Kim H, Kim H, Kwon J, Seo J, Shin D, Moon S. Drosophila Gr64e mediates fatty acid sensing via the phospholipase C pathway. PLoS Genet. 2018;14:e1007229 pubmed publisher..Our results identify a novel FA transduction molecule and reveal that Drosophila Grs can act via distinct molecular mechanisms depending on context. ..
- Sun Y, Cheng X, Zhang L, Hu J, Chen Y, Zhan L, et al. The Functional and Molecular Properties, Physiological Functions, and Pathophysiological Roles of GluN2A in the Central Nervous System. Mol Neurobiol. 2017;54:1008-1021 pubmed publisher..The following review investigates the functional and molecular properties, physiological functions, and pathophysiological roles of the GluN2A subunit. ..
- Jiang L, Hao Y, Mousawi F, Peng H, Yang X. Expression of P2 Purinergic Receptors in Mesenchymal Stem Cells and Their Roles in Extracellular Nucleotide Regulation of Cell Functions. J Cell Physiol. 2017;232:287-297 pubmed publisher..J. Cell. Physiol. 232: 287-297, 2017. © 2016 Wiley Periodicals, Inc. ..
- Bertaccini E. The Molecular Mechanisms of Anesthetic Action: Updates and Cutting Edge Developments from the Field of Molecular Modeling. Pharmaceuticals (Basel). 2010;3:2178-2196 pubmed
- Moeder W, Phan V, Yoshioka K. Ca2+ to the rescue - Ca2+channels and signaling in plant immunity. Plant Sci. 2019;279:19-26 pubmed publisher..Members of two ligand gated ion channel families, glutamate receptor-like channels (GLRs) and cyclic nucleotide-gated channels (CNGCs) have been ..
- Rheinberger J, Hassaine G, Chami M, Stahlberg H, Vogel H, Li X. Two-dimensional crystallization of the mouse serotonin 5-HT3A receptor. Micron. 2017;92:19-24 pubmed publisher..Here we present our results on the formation and improvement of diffracting 2D crystals of the mouse 5-HT3A by limited proteolysis and addition of conformational nanobodies. ..
- Dahlström E, Sandholm N. Progress in Defining the Genetic Basis of Diabetic Complications. Curr Diab Rep. 2017;17:80 pubmed publisher..Variants in or near AFF3, RGMA-MCTP2, SP3-CDCA7, GLRA3, CNKSR3, and UMOD have reached genome-wide significance (p value <5 × 10-8) for association with ..
- Basak S, Chatterjee S, Chakrapani S. Site Directed Spin Labeling and EPR Spectroscopic Studies of Pentameric Ligand-Gated Ion Channels. J Vis Exp. 2016;: pubmed publisher..A combination of steady-state Continuous Wave (CW) and Pulsed (Double Electron Electron Resonance-DEER) EPR approaches will be described that will enable a complete quantitative characterization of channel dynamics. ..
- Cappelli A, Butini S, Brizzi A, Gemma S, Valenti S, Giuliani G, et al. The interactions of the 5-HT3 receptor with quipazine-like arylpiperazine ligands: the journey track at the end of the first decade of the third millennium. Curr Top Med Chem. 2010;10:504-26 pubmed..The discussion is focused mainly on the most significant structure-affinity relationships emerged in the progress of the work and shows how the original ideas have evolved in the recent years. ..
- Barrantes F. Phylogenetic conservation of protein-lipid motifs in pentameric ligand-gated ion channels. Biochim Biophys Acta. 2015;1848:1796-805 pubmed publisher..This article is part of a Special Issue entitled: Lipid-protein interactions. ..
- Regan M, Romero Hernandez A, Furukawa H. A structural biology perspective on NMDA receptor pharmacology and function. Curr Opin Struct Biol. 2015;33:68-75 pubmed publisher..Structural analysis of the isolated extracellular domains in combination with the intact heterotetrameric NMDAR structure provides important insights into how this sophisticated ligand-gated ion channel may function. ..
- Lyu G, Han Y. [Research advances in hereditary epilepsy and precision drug therapy]. Zhongguo Dang Dai Er Ke Za Zhi. 2017;19:1118-1123 pubmed..With the application of next-generation sequencing technology, more and more genes will be determined, which helps to further study the pathogenic mechanism of mutant genes and provides a basis for precision drug therapy for epilepsy. ..
- Vacchelli E, Semeraro M, Enot D, Chaba K, Poirier Colame V, Dartigues P, et al. Negative prognostic impact of regulatory T cell infiltration in surgically resected esophageal cancer post-radiochemotherapy. Oncotarget. 2015;6:20840-50 pubmed..Altogether, these results corroborate the notion that the immunosurveillance seals the fate of patients with esophageal carcinomas treated with conventional radiochemotherapy. ..
- Murail S. Simulation of Ligand Binding to Membrane Proteins. Methods Mol Biol. 2017;1635:359-381 pubmed publisher..As an illustration, the simulation of the ligand-gated ion channel ?-aminobutyric acid type A receptor (GABAAR) surrounded by one of its allosteric potentiators, bromoform, will be presented and discussed. ..
- Clausen R, Mohr A, Riise E, Jensen A, Gill A, Madden D, et al. A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain. Int J Biol Macromol. 2016;92:779-787 pubmed publisher..Furthermore, we present for the first time a GluA4 subtype-specific murine Fab fragment targeting the LBD of the receptor. ..
- Olofsson P, Katz D, Rosas Ballina M, Levine Y, Ochani M, Valdés Ferrer S, et al. ?7 nicotinic acetylcholine receptor (?7nAChR) expression in bone marrow-derived non-T cells is required for the inflammatory reflex. Mol Med. 2012;18:539-43 pubmed publisher..Together, these results indicate that ?7nAChR expression in bone marrow-derived non-T cells is required for the integrity of the inflammatory reflex. ..
- Wang T, Si F, He Z, Chen B. Genome-wide identification, characterization and classification of ionotropic glutamate receptor genes (iGluRs) in the malaria vector Anopheles sinensis (Diptera: Culicidae). Parasit Vectors. 2018;11:34 pubmed publisher..sinensis, and generated the classification of iGluRs by feature and bioinformatics analyses. The work lays the foundation for further functional study of these genes. ..
- Haas A, Le Page Y, Zhadobov M, Boriskin A, Sauleau R, Le Drean Y. Impact of 60-GHz millimeter waves on stress and pain-related protein expression in differentiating neuron-like cells. Bioelectromagnetics. 2016;37:444-54 pubmed publisher..Bioelectromagnetics. 37:444-454, 2016. © 2016 Wiley Periodicals, Inc. ..
- Kaltwasser S, Schmitz L, Michel Schmidt R, Anspach L, Kirkpatrick C, Wessler I. Murine embryonic stem cell line CGR8 expresses all subtypes of muscarinic receptors and multiple nicotinic receptor subunits: Down-regulation of Î±4- and Î²4-subunits during early differentiation. Int Immunopharmacol. 2015;29:110-4 pubmed publisher..Thus, the so-called neuronal Î±4 nicotine receptor composed of these subunits may be involved in the regulation of pluripotency in this murine stem cell line. ..
- Kinde M, Chen Q, Lawless M, Mowrey D, Xu J, Saxena S, et al. Conformational Changes Underlying Desensitization of the Pentameric Ligand-Gated Ion Channel ELIC. Structure. 2015;23:995-1004 pubmed publisher..This work also revealed the co-existence of multiple conformations for a given state and suggested asymmetric conformational arrangements in a homomeric pLGIC. ..
- Mehta P, Srivastava S, Sharma M, Singh I, Malik R. Identification of chemically diverse GABAA agonists as potential anti-epileptic agents using structure-guided virtual screening, ADMET, quantum mechanics and clinical validation through off-target analysis. Int J Biol Macromol. 2018;119:1113-1128 pubmed publisher..The best hit was also analyzed using Quantum mechanical studies, off-target analysis and hit modification. The off-target analysis emphasized that these agents did not have any other predicted side-effects. ..
- Carswell C, Sun J, Baenziger J. Intramembrane aromatic interactions influence the lipid sensitivities of pentameric ligand-gated ion channels. J Biol Chem. 2015;290:2496-507 pubmed publisher..Aromatic residues strengthen M4 interactions with M1/M3 to reduce the sensitivities of pentameric ligand-gated ion channels to their surrounding membrane environment. ..
- Marabelli A, Lape R, Sivilotti L. Mechanism of activation of the prokaryotic channel ELIC by propylamine: a single-channel study. J Gen Physiol. 2015;145:23-45 pubmed publisher..The microscopic affinity for the agonist increased as the channel activated, from 7 mM for the resting state to 0.15 mM for the partially activated intermediate state. ..
- BÃ¡ez PagÃ¡n C, Delgado VÃ©lez M, Lasalde Dominicci J. Activation of the Macrophage Î±7 Nicotinic Acetylcholine Receptor and Control of Inflammation. J Neuroimmune Pharmacol. 2015;10:468-76 pubmed publisher..Whether this ion-translocating activity is relevant for the proper operation of the CAP or other important physiological processes remains obscure. ..
- Tewari M, Monika -, Varghse R, Menon M, Seth P. Astrocytes mediate HIV-1 Tat-induced neuronal damage via ligand-gated ion channel P2X7R. J Neurochem. 2015;132:464-76 pubmed..We believe that these finding should provide new insights into the role of astrocytes in HIV-1 Tat-mediated neurotoxicity. ..
- Hannan S, Mortensen M, Smart T. Snake neurotoxin Î±-bungarotoxin is an antagonist at native GABA(A) receptors. Neuropharmacology. 2015;93:28-40 pubmed publisher..In conclusion, Î±-Bgtx can act as an inhibitor at recombinant and native GABAARs and may be used as a selective tool to inhibit phasic but not tonic currents in the hippocampus. ..
- Xia J, Yu X, Tang L, Li G, He T. P2X7 receptor stimulates breast cancer cell invasion and migration via the AKT pathway. Oncol Rep. 2015;34:103-10 pubmed publisher..Therefore, the P2X7 receptor may be a useful therapeutic target for the treatment of breast cancer. ..
- Lee D, Cho P, Lee H, Lee S, Jung S, Oh S. Trans-activation of TRPV1 by D1R in mouse dorsal root ganglion neurons. Biochem Biophys Res Commun. 2015;465:832-7 pubmed publisher..These results provide evidence that the trans-activation of TRPV1 following D1R activation may contribute to the modulation of pain signaling in nociceptive sensory neurons. ..
- Heusser S, Yoluk O, Klement G, Riederer E, Lindahl E, Howard R. Functional characterization of neurotransmitter activation and modulation in a nematode model ligand-gated ion channel. J Neurochem. 2016;138:243-53 pubmed publisher..The modified channel is also sensitive to allosteric modulators associated with human GABAA receptors, and to site-directed mutations predicted to alter channel opening. ..
- Yuan S, Filipek S, Vogel H. A Gating Mechanism of the Serotonin 5-HT3 Receptor. Structure. 2016;24:816-825 pubmed publisher..The structural transitions in the receptor's transmembrane part finally couple to the intracellular MA helix bundle, opening lateral ports for ion passage. ..
- Mukherjee A. [Computational analysis of a cys-loop ligand gated ion channel from the green alga Chlamydomonas reinhardtii]. Mol Biol (Mosk). 2015;49:832-45 pubmed publisher..This is the first report on a detailed characterization of a cys-loop receptor from the plant kingdom. ..
- Hénault C, Baenziger J. Functional characterization of two prokaryotic pentameric ligand-gated ion channel chimeras - role of the GLIC transmembrane domain in proton sensing. Biochim Biophys Acta Biomembr. 2017;1859:218-227 pubmed publisher..A structural basis for the impaired function of GE is suggested. ..
- Zhang K, Liu J, You X, Kong P, Song Y, Cao L, et al. P2X7 as a new target for chrysophanol to treat lipopolysaccharide-induced depression in mice. Neurosci Lett. 2016;613:60-5 pubmed publisherP2X7 receptor is a ligand gated ion channel found peripheral macrophages and microglia in the nervous system. The current study investigated the relationship between the activated P2X7 and depression for the first time...
- Laurent B, Murail S, Shahsavar A, Sauguet L, Delarue M, Baaden M. Sites of Anesthetic Inhibitory Action on a Cationic Ligand-Gated Ion Channel. Structure. 2016;24:595-605 pubmed publisher..GAs predominantly access the receptor from the lipid bilayer in all cases. Differential binding affinity among the channel forms is observed; the pore site markedly stabilizes the inactive versus active state. ..
- Ziemba P, Schreiner B, Flegel C, Herbrechter R, Stark T, Hofmann T, et al. Activation and modulation of recombinantly expressed serotonin receptor type 3A by terpenes and pungent substances. Biochem Biophys Res Commun. 2015;467:1090-6 pubmed publisher..In our study, we identified new modulators of 5-HT3A receptors out of the classes of monoterpenes and vanilloid substances that frequently occur in various plants. ..
- Kono Y, HÃ¼lsmann S. Presynaptic facilitation of glycinergic mIPSC is reduced in mice lacking Î±3 glycine receptor subunits. Neuroscience. 2016;320:1-7 pubmed publisher..In this study we analyzed the role of GlyR Î±3 in synaptic inhibition to the hypoglossal nucleus using Glra3 (the gene encoding the glycine receptor Î±3 subunit) knockout mice...
- Cheng W, Chen Z, Bracamontes J, Budelier M, Krishnan K, Shin D, et al. Mapping two neurosteroid-modulatory sites in the prototypic pentameric ligand-gated ion channel GLIC. J Biol Chem. 2018;293:3013-3027 pubmed publisher..These results provide a detailed molecular model of multisite neurosteroid modulation of GLIC, which may be applicable to other mammalian pLGICs. ..
- Jia Y, Yang B, Dong W, Liu Z, Lv Z, Jia Z, et al. A serotonin receptor (Cg5-HTR-1) mediating immune response in oyster Crassostrea gigas. Dev Comp Immunol. 2018;82:83-93 pubmed publisher..05). These results suggested that Cg5-HTR-1 was a novel member of 5-HT1 receptor family and it mediated serotonergic immunomodulation on both cellular and humoral immune responses. ..
- Rienzo M, Rocchi A, Threatt S, Dougherty D, Lummis S. Perturbation of Critical Prolines in Gloeobacter violaceus Ligand-gated Ion Channel (GLIC) Supports Conserved Gating Motions among Cys-loop Receptors. J Biol Chem. 2016;291:6272-80 pubmed publisher..However, the Pro-198 site displays a unique phenotype that gives evidence of the importance of the region surrounding this residue for the correct functioning of GLIC. ..
- Feingold D, Starc T, O Donnell M, Nilson L, Dent J. The orphan pentameric ligand-gated ion channel pHCl-2 is gated by pH and regulates fluid secretion in Drosophila Malpighian tubules. J Exp Biol. 2016;219:2629-38 pubmed publisher..Our data implicate pHCl-2 as an important source of chloride conductance required for proper urine production, highlighting a novel role for pLGICs in epithelial tissues regulating fluid secretion and osmotic homeostasis. ..
- Zhang H, Hu J, Zhou Y, Qin X, Song Z, Yang P, et al. Promoted Interaction of Nuclear Factor-ÎºB With Demethylated Purinergic P2X3 Receptor Gene Contributes to Neuropathic Pain in Rats With Diabetes. Diabetes. 2015;64:4272-84 pubmed publisher..Our findings suggest that the p2x3r gene promoter DNA demethylation and enhanced interaction with p65 contributes to P2X3R sensitization and diabetic pain hypersensitivity. ..
- Shafaat O, Winkler J, Gray H, Dougherty D. Photoactivation of an Acid-Sensitive Ion Channel Associated with Vision and Pain. Chembiochem. 2016;17:1323-7 pubmed publisher..100??s) after excitation of 1. These results demonstrate that irradiation of 1 can induce rapid, local pH changes that can be used to investigate both biological and chemical proton transfer reactions. ..
- Olsen R. GABAA receptor: Positive and negative allosteric modulators. Neuropharmacology. 2018;136:10-22 pubmed publisher..This article is part of the "Special Issue Dedicated to Norman G. Bowery". ..
- Burgos C, Yevenes G, Aguayo L. Structure and Pharmacologic Modulation of Inhibitory Glycine Receptors. Mol Pharmacol. 2016;90:318-25 pubmed publisher..In this review, we summarize how the new information obtained in functional, mutagenesis, and structural studies have contributed to a better understanding of the function and regulation of GlyR. ..
- Lev B, Murail S, Poitevin F, Cromer B, Baaden M, Delarue M, et al. String method solution of the gating pathways for a pentameric ligand-gated ion channel. Proc Natl Acad Sci U S A. 2017;114:E4158-E4167 pubmed publisher..These results provide molecular details of GLIC gating and insight into the allosteric mechanisms for the superfamily of pentameric ligand-gated channels. ..
- Elberson B, Whisenant T, Cortes D, Cuello L. A cost-effective protocol for the over-expression and purification of fully-functional and more stable Erwinia chrysanthemi ligand-gated ion channel. Protein Expr Purif. 2017;133:177-186 pubmed publisher..The use of an autoinduction media and inexpensive detergents during ELIC extraction, in addition to the high-quality and large quantity of the purified channel, are the highlights of this improved biochemical protocol. ..
- Blanc E, Wagner P, Plaisier F, Schmitt M, Durroux T, Bourguignon J, et al. Design and validation of a homogeneous time-resolved fluorescence cell-based assay targeting the ligand-gated ion channel 5-HT3A. Anal Biochem. 2015;484:105-12 pubmed publisher..This interesting result was confirmed with electrophysiological experiments. The method described here is easy to implement and could be applicable for other LGICs, opening new ways for the screening of chemical libraries. ..
- Yu J, Chen Y, Li M, Gao Q, Peng Y, Gong Q, et al. Paeoniflorin down-regulates ATP-induced inflammatory cytokine production and P2X7R expression on peripheral blood mononuclear cells from patients with primary SjÃ¶gren's syndrome. Int Immunopharmacol. 2015;28:115-20 pubmed publisher..Thus, PF may provide a new therapeutic approach to regulate P2X7R-mediated pathologic responses of pSS. ..
- Ion B, Wells M, Chen Q, Xu Y, Tang P. Ketamine Inhibition of the Pentameric Ligand-Gated Ion Channel GLIC. Biophys J. 2017;113:605-612 pubmed publisher..Both signaling pathways have been predicted previously using the perturbation-based Markovian transmission model. The study provides a structural and dynamics basis for the inhibitory modulation of ketamine on pLGICs. ..
- Mesuret G, Dannenberg J, Arnoldt M, Grützner A, Niebert M, Hülsmann S. Breathing disturbances in a model of Rett syndrome: A potential involvement of the glycine receptor ?3 subunit?. Respir Physiol Neurobiol. 2018;248:43-47 pubmed publisher..Therefore, we generated a double knock-out mouse line that lacks both the Mecp2 gene as well as the gene (Glra3) for the ?3 subunit of the ionotropic glycine receptor...
- Kingsmore S, Suh D, Seldin M. Genetic mapping of the glycine receptor alpha 3 subunit on mouse chromosome 8. Mamm Genome. 1994;5:831-2 pubmed
- WELSH B, Todorovic J, Kirson D, Allen H, BAYLY M, Mihic S. Disruption of a putative intersubunit electrostatic bond enhances agonist efficacy at the human Î±1 glycine receptor. Brain Res. 2017;1657:148-155 pubmed publisher..Our findings suggest that the determination of efficacy following ligand binding to the glycine receptor may involve the disruption of an intersubunit electrostatic interaction occurring near the agonist binding site. ..
- Sandholm N, Forsblom C, Mäkinen V, McKnight A, Osterholm A, He B, et al. Genome-wide association study of urinary albumin excretion rate in patients with type 1 diabetes. Diabetologia. 2014;57:1143-53 pubmed publisher..6% after adjustment for covariates. In the discovery stage, five single nucleotide polymorphisms in the GLRA3 gene were strongly associated with albuminuria (p?<?5?×?10(-8))...
- Martin N, Malik S, Calimet N, Changeux J, Cecchini M. Un-gating and allosteric modulation of a pentameric ligand-gated ion channel captured by molecular dynamics. PLoS Comput Biol. 2017;13:e1005784 pubmed publisher..The simulated un-gating converges to the X-ray structure of GluCl resting state both globally and locally, demonstrating the predictive character of state-of-art MD simulations...
- Leffler A, Kuryatov A, Zebroski H, Powell S, Filipenko P, Hussein A, et al. Discovery of peptide ligands through docking and virtual screening at nicotinic acetylcholine receptor homology models. Proc Natl Acad Sci U S A. 2017;114:E8100-E8109 pubmed publisher..ToxDock is freely available at rosie.rosettacommons.org/tox_dock. ..
- Ding S, Zhu L, Tian Y, Zhu T, Huang X, Zhang X. P2X3 receptor involvement in endometriosis pain via ERK signaling pathway. PLoS ONE. 2017;12:e0184647 pubmed publisher..Additionally, P2X3 and calcitonin gene related peptide (CGRP) were co-expressed in endometriotic lesions. These obtained results suggest that P2X3 might be involved in endometriosis pain signal transduction via ERK signal pathway. ..
- Swanger S, Chen W, Wells G, Burger P, Tankovic A, Bhattacharya S, et al. Mechanistic Insight into NMDA Receptor Dysregulation by Rare Variants in the GluN2A and GluN2B Agonist Binding Domains. Am J Hum Genet. 2016;99:1261-1280 pubmed publisher..Finally, discerning the mechanisms underlying NMDAR dysregulation by these rare variants allowed investigations of pharmacologic strategies to correct NMDAR function. ..