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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/12/26 20:09:04」(JST)
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| SLC6A9 | |||||||||||||||||
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| Identifiers | |||||||||||||||||
| Aliases | SLC6A9, GLYT1, Glycine transporter 1, solute carrier family 6 member 9 | ||||||||||||||||
| External IDs | MGI: 95760 HomoloGene: 5050 GeneCards: SLC6A9 | ||||||||||||||||
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| Location (UCSC) | Chr 1: 43.99 – 44.03 Mb | Chr 4: 117.83 – 117.88 Mb | |||||||||||||||
| PubMed search | [1] | [2] | |||||||||||||||
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Sodium- and chloride-dependent glycine transporter 1 is a protein that in humans is encoded by the SLC6A9 gene.[3][4][5]
Contents
- 1 Selective inhibitors
- 2 See also
- 3 References
- 4 Further reading
Selective inhibitors
Elevation of extracellular synaptic glycine concentration by blockade of GlyT1 has been hypothesized to potentiate NMDA receptor function in vivo and to represent a rational approach for the treatment of schizophrenia and cognitive disorders. Several drug candidates have reached clinical trials.[6]
- ASP2535[7]
- Bitopertin (RG1678), which has entered phase II trials for the treatment of schizophrenia[8]
- Org 25935
- PF-03463275 (in phase II trial)
See also
- Sodium:neurotransmitter symporter
- Solute carrier family
References
- ^ "Human PubMed Reference:".
- ^ "Mouse PubMed Reference:".
- ^ Kim KM, Kingsmore SF, Han H, Yang-Feng TL, Godinot N, Seldin MF, Caron MG, Giros B (Jun 1994). "Cloning of the human glycine transporter type 1: molecular and pharmacological characterization of novel isoform variants and chromosomal localization of the gene in the human and mouse genomes". Mol Pharmacol. 45 (4): 608–17. PMID 8183239.
- ^ Jones EM, Fernald A, Bell GI, Le Beau MM (Nov 1995). "Assignment of SLC6A9 to human chromosome band 1p33 by in situ hybridization". Cytogenet Cell Genet. 71 (3): 211. doi:10.1159/000134110. PMID 7587377.
- ^ "Entrez Gene: SLC6A9 solute carrier family 6 (neurotransmitter transporter, glycine), member 9".
- ^ "Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain". Nature Reviews Drug Discovery. 12: 866–85. 31 October 2013. doi:10.1038/nrd3893. PMID 24172334.
- ^ Harada K, Nakato K, Yarimizu J, Yamazaki M, Morita M, Takahashi S, Aota M, Saita K, Doihara H, Sato Y, Yamaji T, Ni K, Matsuoka N (2012). "A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease". European Journal of Pharmacology. 685: 59–69. doi:10.1016/j.ejphar.2012.04.013. PMID 22542656.
- ^ Pinard E, Alanine A, Alberati D, Bender M, Borroni E, Bourdeaux P, Brom V, Burner S, Fischer H, Hainzl D, Halm R, Hauser N, Jolidon S, Lengyel J, Marty HP, Meyer T, Moreau JL, Mory R, Narquizian R, Nettekoven M, Norcross RD, Puellmann B, Schmid P, Schmitt S, Stalder H, Wermuth R, Wettstein JG, Zimmerli D (June 2010). "Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia". J. Med. Chem. 53 (12): 4603–14. doi:10.1021/jm100210p. PMID 20491477.
Further reading
- Olivares L, Aragón C, Giménez C, Zafra F (1995). "The role of N-glycosylation in the targeting and activity of the GLYT1 glycine transporter". J. Biol. Chem. 270 (16): 9437–42. doi:10.1074/jbc.270.16.9437. PMID 7721869.
- Borowsky B, Mezey E, Hoffman BJ (1993). "Two glycine transporter variants with distinct localization in the CNS and peripheral tissues are encoded by a common gene". Neuron. 10 (5): 851–63. doi:10.1016/0896-6273(93)90201-2. PMID 8494645.
- Evans J, Herdon H, Cairns W, et al. (2000). "Cloning, functional characterisation and population analysis of a variant form of the human glycine type 2 transporter". FEBS Lett. 463 (3): 301–6. doi:10.1016/S0014-5793(99)01636-1. PMID 10606742.
- Hanley JG, Jones EM, Moss SJ (2000). "GABA receptor rho1 subunit interacts with a novel splice variant of the glycine transporter, GLYT-1". J. Biol. Chem. 275 (2): 840–6. doi:10.1074/jbc.275.2.840. PMID 10625616.
- Geerlings A, López-Corcuera B, Aragón C (2000). "Characterization of the interactions between the glycine transporters GLYT1 and GLYT2 and the SNARE protein syntaxin 1A". FEBS Lett. 470 (1): 51–4. doi:10.1016/S0014-5793(00)01297-7. PMID 10722844.
- Christie GR, Ford D, Howard A, et al. (2001). "Glycine supply to human enterocytes mediated by high-affinity basolateral GLYT1". Gastroenterology. 120 (2): 439–48. doi:10.1053/gast.2001.21207. PMID 11159884.
- Reye P, Penfold P, Pow DV (2001). "Glyt-1 expression in cultured human Müller cells and intact retinae". Glia. 34 (4): 311–5. doi:10.1002/glia.1064. PMID 11360303.
- Geerlings A, Núñez E, Rodenstein L, et al. (2002). "Glycine transporter isoforms show differential subcellular localization in PC12 cells". J. Neurochem. 82 (1): 58–65. doi:10.1046/j.1471-4159.2002.00930.x. PMID 12091465.
- Brandenberger R, Wei H, Zhang S, et al. (2005). "Transcriptome characterization elucidates signaling networks that control human ES cell growth and differentiation". Nat. Biotechnol. 22 (6): 707–16. doi:10.1038/nbt971. PMID 15146197.
- Antonov SM, Brovtsyna NB, Mironova EV (2005). "The mechanism of allosteric interaction of cytoplasmic and extracellular Cl− in the glial glycine transporter (hGlyTlb)". Dokl. Biol. Sci. 402: 163–6. doi:10.1007/s10630-005-0076-z. PMID 16121932.
Membrane proteins, carrier proteins: membrane transport proteins solute carrier (TC 2A)
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see also solute carrier disorders
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Glycinergics
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See also: GABAergics • GHBergics • Glutamatergics
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Glutamatergics
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See also: GABAergics • GHBergics • Glycinergics
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This membrane protein–related article is a stub. You can help Wikipedia by expanding it.
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English Journal
- Na+/H+ exchange is inactivated during mouse oocyte meiosis, facilitating glycine accumulation that maintains embryo cell volume.
- Zhou C, Fitzharris G, Alper SL, Baltz JM.SourceOttawa Hospital Research Institute, Ottawa, Ontario, Canada.
- Journal of cellular physiology.J Cell Physiol.2013 Oct;228(10):2042-53. doi: 10.1002/jcp.24370.
- The coupled action of the Na(+)/H(+) exchanger NHE1 and the HCO3(-)/Cl(-) exchanger AE2 constitutes the principal mechanism for acute correction of decreased cell volume in mammalian somatic cells, while, when acting separately, they regulate intracellular pH. It was previously found that AE2 become
- PMID 23553550
- Inhibition of glycine transporter-1 reduces cue-induced nicotine-seeking, but does not promote extinction of conditioned nicotine cue responding in the rat.
- Cervo L, Di Clemente A, Orrù A, Moro F, Cassina C, Pich EM, Corsi M, Gozzi A, Bifone A.SourceIRCCS-Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.
- Addiction biology.Addict Biol.2013 Sep;18(5):800-11. doi: 10.1111/adb.12049. Epub 2013 Mar 14.
- Pharmacological stimulation of N-methyl-D-aspartate receptors (NMDAr) could enhance the outcome of cue-exposure therapy for smoking cessation. NMDAr stimulation can be achieved by increasing pharmacologically the synaptic levels of glycine, a necessary co-agonist. Here, we evaluate the effects of SS
- PMID 23490434
- Phencyclidine decreases tickling-induced 50-kHz ultrasound vocalizations in juvenile rats: a putative model of the negative symptoms of schizophrenia?
- Boulay D, Ho-Van S, Bergis O, Avenet P, Griebel G.SourceSanofi Research & Development, Exploratory Unit, Chilly-Mazarin, France.
- Behavioural pharmacology.Behav Pharmacol.2013 Aug 7. [Epub ahead of print]
- The objective of the present study was to examine the idea that the decrease in 50-kHz ultrasonic vocalizations elicited by tickling in juvenile rats following the administration of the psychotomimetic drug phencyclidine (PCP) may represent a valid model of the negative symptoms of schizophrenia. Fi
- PMID 23928693
Japanese Journal
- A Highly Selective Inhibitor of Glycine Transporter-1 Elevates the Threshold for Maximal Electroshock-Induced Tonic Seizure in Mice
- Biological and Pharmaceutical Bulletin 39(2), 174-180, 2016
- NAID 130005122358
- A highly selective inhibitor of glycine transporter-1 elevates the threshold for maximal electroshock-induced tonic seizure in mice
- Biological and Pharmaceutical Bulletin advpub(0), 2016
- NAID 130005112654
- Synthesis and evaluation of 2-chloro N-[(S)-{(S)-1-[11 C]methylpiperidin-2-yl} (phenyl)methyl]3- trifluoromethyl-benzamide ([11 C]N-methyl- SSR504734) as a PET radioligand for glycine transporter 1
- EJNMMI Research 2(1), 37, 2012-07-09
- NAID 120005231371
Related Links
- GlyT1トランスポーター阻害薬および神経学的および神経精神病学的障害の治療におけるその使用 ... （I） [式中：R 1 、R 2 、R 3 、R 4 、R 5 、R 6 、R 15 、R 7 、R 8 およびmは、明細書の記載と同義である]
- 2 meanings of GLYT1 acronym and GLYT1 abbreviation. Get the definition of GLYT1 by All Acronyms dictionary. Top Definition: Glycine Transporter 1 ... Skip to main content What does GLYT1 mean? The list of 2 meanings of
Related Pictures
★リンクテーブル★
| リンク元 | 「グリシン輸送体1」「glycine transporter 1」 |