Biology:Glycine transporter 1

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A representation of the 3D structure of the protein myoglobin showing turquoise α-helices.
Generic protein structure example

Sodium- and chloride-dependent glycine transporter 1 is a protein that in humans is encoded by the SLC6A9 gene.[1][2][3]

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.[4]

  • ASP2535[5]
  • Bitopertin (RG1678), which has entered phase II trials for the treatment of schizophrenia[6]
  • Org 25935
  • PF-03463275 (in phase II trial)

See also

References

  1. ↑ "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. Jun 1994. PMID 8183239. 
  2. ↑ "Assignment of SLC6A9 to human chromosome band 1p33 by in situ hybridization". Cytogenet Cell Genet 71 (3): 211. Nov 1995. doi:10.1159/000134110. PMID 7587377. 
  3. ↑ "Entrez Gene: SLC6A9 solute carrier family 6 (neurotransmitter transporter, glycine), member 9". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6536. 
  4. ↑ "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. http://www.nature.com/nrd/journal/v12/n11/full/nrd3893.html. 
  5. ↑ "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. 2012. doi:10.1016/j.ejphar.2012.04.013. PMID 22542656. 
  6. ↑ "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. June 2010. doi:10.1021/jm100210p. PMID 20491477. 

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