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Glycine receptor

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https://www.readbyqxmd.com/read/28528670/glycine-receptor-drug-discovery
#1
Joseph W Lynch, Yan Zhang, Sahil Talwar, Argel Estrada-Mondragon
Postsynaptic glycine receptor (GlyR) chloride channels mediate inhibitory neurotransmission in the spinal cord and brain stem, although presynaptic and extrasynaptic GlyRs are expressed more widely throughout the brain. In humans, GlyRs are assembled as homo- or heteromeric pentamers of α1-3 and β subunits. GlyR malfunctions have been linked to a range of neurological disorders including hyperekplexia, temporal lobe epilepsy, autism, breathing disorders, and chronic inflammatory pain. Although it is possible that GlyRs may eventually be clinically targeted for a variety of neurological disorders, most research to date has focused on developing GlyR-targeted treatments for chronic pain...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28524260/presence-of-ethanol-sensitive-glycine-receptors-in-medium-spiny-neurons-in-the-mouse-nucleus-accumbens
#2
B Förstera, B Muñoz, M K Lobo, R Chandra, D M Lovinger, L G Aguayo
Alcohol abuse causes major social, economic and health-related problems worldwide. Alcohol, like other drugs of abuse, increases levels of dopamine in the nucleus accumbens, facilitating behavioural reinforcement and substance abuse. Previous studies suggested that glycine receptors (GlyRs) are involved in the regulation of accumbal dopamine levels. Here, we investigated the presence of GlyRs in accumbal dopamine receptor medium spiny neurons (MSNs) of C57BL/6J mice, analyzing mRNA expression-levels and immunoreactivity of GlyR subunits, as well as ethanol sensitivity...
May 19, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28515681/the-activity-induced-long-non-coding-rna-meg3-modulates-ampa-receptor-surface-expression-in-primary-cortical-neurons
#3
Men C Tan, Jocelyn Widagdo, Yu Q Chau, Tianyi Zhu, Justin J-L Wong, Allen Cheung, Victor Anggono
Transcription of new RNA is crucial for maintaining synaptic plasticity, learning and memory. Although the importance of synaptic plasticity-related messenger RNAs (mRNAs) is well established, the role of a large group of long non-coding RNAs (lncRNAs) in long-term potentiation (LTP) is not known. In this study, we demonstrated the expression of a lncRNA cluster, namely maternally expressed gene 3 (Meg3), retrotransposon-like gene 1-anti-sense (Rtl1-AS), Meg8 and Meg9, which is located in the maternally imprinted Dlk1-Dio3 region on mouse chromosome 12qF1, in primary cortical neurons following glycine stimulation in an N-Methyl-D-aspartate receptor (NMDAR)-dependent manner...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28514338/-a-comparative-chemoreactome-analysis-of-mexidol
#4
I Yu Torshin, O A Gromova, I S Sardaryan, L E Fedotova
AIM: To compare mexidol with control molecules (choline alfoscerate, piracetam, glycine, semax) using chemoreactome analysis. MATERIAL AND METHODS: The chemical structure of mexidol was compared to molecule metabolites extracted from the Human Metabolome Database (HMDB) and a drug database. More than 40 000 of metabolites from HMDB were used as a model of human metabolome. RESULTS AND CONCLUSION: The chemoreactome analysis showed that mexidol may be (1) an agonist of acetylcholine and GABA-A receptors; (2) an anti-inflammatory agent, the effects of which are carried out by inhibiting the synthesis of pro-inflammatory prostaglandins; (3) a neurotrophic agent with neuroprotective properties; (4) a coagulation inhibitor; (5) a diabetes medication and (6) a hypolipidemic agent...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/28514141/subtype-specific-agonists-for-nmda-receptor-glycine-binding-sites
#5
Alex Maolanon, Rune Risgaard, Shuang-Yan Wang, Yoran Snoep, Athanasios Papangelis, Feng Yi, David Holley, Anne F Barslund, Niels Svenstrup, Kasper B Hansen, Rasmus Prætorius Clausen
A series of analogues based on serine as lead structure were designed and their agonist activities were evaluated at recombinant NMDA receptor subtypes (GluN1/2A-D) using two-electrode voltage-clamp (TEVC) electrophysiology. Pronounced variation in subunit-selectivity, potency, and agonist efficacy was observed in a manner that was dependent on the GluN2 subunit in the NMDA receptor. In particular, compounds 15a and 16a are potent GluN2C-specific superagonists at the GluN1 subunit with agonist efficacies of 398% and 308% compared to glycine...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28510303/cucurbit-8-uril-and-14-3-3-based-binary-bivalent-supramolecular-protein-assembly-platform-and-co-crystal-structure
#6
Pim de Vink, Jeroen Briels, Thomas Schrader, Lech Milroy, Luc Brunsveld, Christian Ottmann
Interactions between proteins frequently employ recognition sequences that engage in multivalent binding events. Dimeric 14-3-3 adapter proteins represent a prominent example, typically binding partner proteins in a phosphorylation-dependent mono- or bivalent manner. Here we describe the development of a cucurbit[8]uril (Q8)-based supramolecular system, which in conjunction with the 14-3-3 protein dimer acts as a binary and bivalent protein assembly platform. We fused the phenylalanine-glycine-glycine (FGG) tripeptide motif to the N-terminus of the 14-3-3-binding epitope of the estrogen receptor α (ERα), for selective binding to Q8...
May 16, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28501123/attenuation-of-intestinal-ischemia-reperfusion-injury%C3%A2-by-%C3%AE-alanine-a-potentially-glycine-receptor-mediated-effect
#7
Lisa Brencher, Rabea Verhaegh, Michael Kirsch
BACKGROUND: Acute mesenteric ischemia is often caused by embolization of the mesenteric arterial circulation. Coherent intestinal injury due to ischemia and following reperfusion get visible on macroscopic and histologic level. In previous studies, application of glycine caused an ameliorated intestinal damage after ischemia-reperfusion in rats. Because we speculated that glycine acted here as a signal molecule, we investigated whether the glycine-receptor agonist β-alanine evokes the same beneficial effect in intestinal ischemia-reperfusion...
May 1, 2017: Journal of Surgical Research
https://www.readbyqxmd.com/read/28489663/use-dependent-inhibition-of-glycine-activated-chloride-current-in-rat-neurons-by-%C3%AE-amyloid-peptide-pretreated-with-hexafluoroisopropanol
#8
Elena I Solntseva, Julia V Bukanova
Hexafluoroisopropanol (HFIP) is a nonpolar organic solvent that is often used to prepare β-amyloid peptide (Aβ) samples. In this work, we compare the effects of two different species derived from synthetic Aβ1-42 and prepared without HFIP (Aβ) or using HFIP (Aβ/HFIP) on the glycine-activated chloride current (IGly). The experiments were conducted on the pyramidal neurons isolated from CA3 region of rat hippocampus. Transmembrane currents were recorded using a conventional patch-clamp technique in the whole-cell configuration...
May 5, 2017: Neuroreport
https://www.readbyqxmd.com/read/28481020/activation-of-ryanodine-receptors-is-required-for-pka-mediated-downregulation-of-a-type-k-channels-in-rat-hippocampal-neurons
#9
Yoon-Sil Yang, Sang-Chan Jeon, Moon-Suk Kang, Seon-Hee Kim, Su-Yong Eun, Soo-Hee Jin, Sung-Cherl Jung
A-type K(+) channels (IA channels) contribute to learning and memory mechanisms by regulating neuronal excitabilities in the CNS, and their expression level is targeted by Ca(2+) influx via synaptic NMDA receptors (NMDARs) during long-term potentiation (LTP). However, it is not clear how local synaptic Ca(2+) changes induce IA downregulation throughout the neuron, extending from the active synapse to the soma. In this study, we tested if two major receptors of endoplasmic reticulum (ER), ryanodine (RyRs), and IP3 (IP3 R) receptors, are involved in Ca(2+) -mediated IA downregulation in cultured hippocampal neurons of rats...
May 8, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28480032/neuroprotection-provided-by-isoflurane-pre-conditioning-and-post-conditioning
#10
REVIEW
Ming Jiang, Liang Sun, Dong-Xia Feng, Zheng-Quan Yu, Rong Gao, Yuan-Zhao Sun, Gang Chen
Isoflurane, a volatile and inhalational anesthetic, has been extensively used in perioperative period for several decades. A large amount of experimental studies have indicated that isoflurane exhibits neuroprotective properties when it is administrated before or after (pre-conditioning and post-conditioning) neurodegenerative diseases (e.g., hypoxic ischemia, stroke and trauma). Multiple mechanisms are involved in isoflurane induced neuroprotection, including activation of glycine and γ-aminobutyric acid receptors, antagonism of ionic channels and alteration of the function and activity of other cellular proteins...
January 2017: Medical Gas Research
https://www.readbyqxmd.com/read/28479061/crystal-structures-of-human-glyr%C3%AE-3-bound-to-ivermectin
#11
Xin Huang, Hao Chen, Paul L Shaffer
Ivermectin acts as a positive allosteric modulator of several Cys-loop receptors including the glutamate-gated chloride channels (GluCls), γ-aminobutyric acid receptors (GABAARs), glycine receptors (GlyRs), and neuronal α7-nicotinic receptors (α7 nAChRs). The crystal structure of Caenorhabditis elegans GluCl complexed with ivermectin revealed the details of its ivermectin binding site. Although the electron microscopy structure of zebrafish GlyRα1 complexed with ivermectin demonstrated a similar binding orientation, detailed structural information on the ivermectin binding and pore opening for Cys-loop receptors in vertebrates has been elusive...
May 4, 2017: Structure
https://www.readbyqxmd.com/read/28475556/high-concentrations-of-tranexamic-acid-inhibit-ionotropic-glutamate-receptors
#12
Irene Lecker, Dian-Shi Wang, Kirusanthy Kaneshwaran, C David Mazer, Beverley A Orser
BACKGROUND: The antifibrinolytic drug tranexamic acid is structurally similar to the amino acid glycine and may cause seizures and myoclonus by acting as a competitive antagonist of glycine receptors. Glycine is an obligatory co-agonist of the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors. Thus, it is plausible that tranexamic acid inhibits NMDA receptors by acting as a competitive antagonist at the glycine binding site. The aim of this study was to determine whether tranexamic acid inhibits NMDA receptors, as well as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and kainate subtypes of ionotropic glutamate receptors...
May 5, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28470528/phenotyping-cellular-viability-by-functional-analysis-of-ion-channels-glyr-targeted-screening-in-nt2-n-cells
#13
Katharina Kuenzel, Sepideh Abolpour Mofrad, Daniel F Gilbert
Glycine receptor chloride channels (GlyRs) are attractive drug targets for therapeutic intervention and are also more and more recognized in the context of in vitro neurotoxicity and developmental neurotoxicity testing. Assaying the functional properties of GlyR can serve as an indicator of cellular viability and the integrity of the developing and mature central nervous system. Human pluripotent NTERA-2 (NT2) stem cells undergo neuronal differentiation upon stimulation with retinoic acid and express a large variety of neuronal proteins-including GlyR...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28468946/novel-mode-of-antagonist-binding-in-nmda-receptors-revealed-by-the-crystal-structure-of-the-glun1-glun2a-ligand-binding-domain-complexed-to-nvp-aam077
#14
Annabel Romero-Hernandez, Hiro Furukawa
Competitive antagonists against N-methyl-D-aspartate (NMDA) receptors have played critical roles throughout the history of neuropharmacology and basic neuroscience. There are currently numerous NMDA receptor antagonists containing a variety of chemical groups. Among those compounds, a GluN2-specific antagonist, (R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-methyl]-phosphonic acid (NVP-AAM077), contains a unique combination of a dioxoquinoxalinyl ring, a bromophenyl group, and a phosphono group...
May 3, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28464209/alanine-scan-of-the-opioid-peptide-dynorphin-b-amide
#15
Anand A Joshi, Thomas F Murray, Jane V Aldrich
To date structure-activity relationship (SAR) studies of the dynorphins (Dyn), endogenous peptides for kappa opioid receptors (KOR), have focused almost exclusively on Dyn A with minimal studies on Dyn B. While both Dyn A and Dyn B have identical N-terminal sequences, their C-terminal sequences differ which could result in differences in pharmacological activity. We performed an alanine scan of the non-glycine residues up through residue 11 of Dyn B amide to explore the role of these side chains in the activity of Dyn B...
May 2, 2017: Biopolymers
https://www.readbyqxmd.com/read/28461116/anti-neuronal-anti-bodies-in-patients-with-early-psychosis
#16
O Mantere, M Saarela, T Kieseppä, T Raij, T Mäntylä, M Lindgren, E Rikandi, W Stoecker, B Teegen, J Suvisaari
It may be challenging to distinguish autoimmune encephalitis associated with anti-neuronal autoantibodies from primary psychiatric disorders. Here, serum was drawn from patients with a first-episode psychosis (n=70) or a clinical high-risk for psychosis (n=6) and controls (n=34). We investigated the serum prevalence of 24 anti-neuronal autoantibodies: IgG antibodies for anti-N-methyl-d-aspartate-type glutamate receptor (anti-NMDAR), glutamate and γ-aminobutyric acid alpha and beta receptors (GABA-a, GABA-b), alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA), glycine receptor (GlyR), metabotropic glutamate receptor 1 and 5 (mGluR1, mGluR5), anti-Tr/Delta/notch-like epidermal growth factor-related receptor (DNER), contactin-associated protein-like 2 (CASPR2), myelin oligodendrocyte glycoprotein (MOG), glutamic acid decarboxylase-65 (GAD65), collapsin response mediator protein 5/crossveinless-2 (CV2), aquaporin-4 (AQP4), anti-dipeptidyl-peptidase-like protein-6 (DPPX), type 1 anti-neuronal nuclear antibody (ANNA-1, Hu), Ri, Yo, IgLON5, Ma2, zinc finger protein 4 (ZIC4), Rho GTPase-activating protein 26, amphiphysin, and recoverin, as well as IgA and IgM for dopamine-2-receptor (DRD2)...
April 28, 2017: Schizophrenia Research
https://www.readbyqxmd.com/read/28453266/metabolomics-approach-to-investigate-estrogen-receptor-dependent-and-independent-effects-of-o-p-ddt-in-the-uterus-and-brain-of-immature-mice
#17
Dezhen Wang, Wentao Zhu, Yao Wang, Jin Yan, Miaomiao Teng, Jiyan Miao, Zhiqiang Zhou
Previous studies have demonstrated the endocrine disruption of o,p'-DDT. In this study, we used a (1)H NMR based metabolomics approach to investigate the estrogenic effects of o,p'-DDT (300 mg/kg) on the uterus and brain after 3 days of oral gavage administration, and ethynylestradiol (EE, 100 μg/kg) was used as a positive control. A supervised statistical analysis (PLS-DA) indicated that o,p'-DDT exerted both estrogenic receptor-(ER)-dependent and independent effects on the uterus but mainly ER-independent effects on the brain at metabolome levels, which was verified by coexposing with the antiestrogenic ICI 182,780...
May 2, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28445975/functional-fgfr4-gly388arg-polymorphism-contributes-to-cancer-susceptibility-evidence-from-meta-analysis
#18
Si-Wei Xiong, Jianqun Ma, Fen Feng, Wen Fu, Shan-Rong Shu, Tianjiao Ma, Caixia Wu, Guo-Chang Liu, Jinhong Zhu
Fibroblast growth factor receptor 4 (FGFR4) is a member of receptor tyrosine kinase family. A functional Gly388Arg (rs351855 G>A) polymorphism in FGFR4 gene causes a glycine-to-arginine change at codon 388 within the transmembrane domain of the receptor. Although the FGFR4 rs351855 G>A polymorphism has been implicated in cancer development, its association with cancer risk remains controversial. Here, we have systematically analyzed the association between the rs351855 G>A polymorphism and cancer risk by performing a meta-analysis of 27 studies consisting of 8,682 cases and 9,731 controls...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28437460/an-aggregation-removal-model-for-the-formation-and-size-determination-of-post-synaptic-scaffold-domains
#19
Jonas Ranft, Leandro G Almeida, Pamela C Rodriguez, Antoine Triller, Vincent Hakim
The formation and stability of synapses are key questions in neuroscience. Post-synaptic domains have been classically conceived as resulting from local insertion and turnover of proteins at the synapse. However, insertion is likely to occur outside the post-synaptic domains and advances in single-molecule imaging have shown that proteins diffuse in the plane of the membrane prior to their accumulation at synapses. We quantitatively investigated this scenario using computer simulations and mathematical analysis, taking for definiteness the specific case of inhibitory synapse components, i...
April 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/28429370/the-role-of-charged-residues-in-independent-glycine-receptor-folding-domains-for-intermolecular-interactions-and-ion-channel-function
#20
Georg Langlhofer, Carmen Villmann
Glycine receptor (GlyR) truncations in the intracellular TM3-4 loop, documented in patients suffering from hyperekplexia and in the mouse mutant oscillator, lead to non-functionality of GlyRs. The missing part that contains the TM3-4 loop, TM4, and C-terminal sequences is essential for pentameric receptor arrangements. In vitro coexpressions of GlyRα1 truncated N-domains and C- domains were able to restore ion channel function. An ionic interaction between both domains was hypothesised as the underlying mechanism...
April 21, 2017: Journal of Neurochemistry
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