- Glycine receptor
The glycine receptor, or GlyR, is the receptor for the
amino acid neurotransmitter glycine . It is one of the most widely distributed inhibitory receptors in thecentral nervous system .Activation and inactivation
The receptor can be activated by a range of simple
amino acid s includingglycine , β-alanine andtaurine , and can be selectively blocked by the high-affinity competitive antagoniststrychnine . cite journal | last =Rajendra | first =S | authorlink = | coauthors =Lynch JW, Schofield PR | title =The glycine receptor | journal =Pharmacology and Therapeutics | volume =73 | issue =2 | pages =121–146 | publisher = | date =1997 | url =http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=9131721 | doi = 10.1016/S0163-7258(96)00163-5| pmid =9131721 | accessdate =2007-01-16 ]Arrangement of subunits
Strychnine-sensitive glycine receptors are members of a family of
Ligand-gated ion channel s. Receptors of this family are arranged as fivesubunit s surrounding a central pore, with each subunit composed of four α helical transmembrane segments.cite journal | last =Miyazawa | first =A | authorlink = | coauthors =Fujiyoshi Y, Unwin N | title =Structure and gating mechanism of the acetylcholine receptor pore | journal = Nature| volume =423 | issue =6943 | pages = 949–955| publisher = | date =2003 | url = | doi = 10.1038/nature01748| pmid =12827192 | accessdate = ]There are presently four known isoforms of the α-subunit (α1-4) of GlyR that are essential to bind
ligand s (Gene|GLRA1, Gene|GLRA2, Gene|GLRA3, Gene|GLRA4) and a single β-subunit (Gene|GLRB).The adult form of the GlyR is the heteromeric α1β receptor, which is believed to have a stoichiometry (proportion) of three α1 subunits and two β subunitscite journal | last =Kuhse | first = J| authorlink = | coauthors = Laube B, Magalei D, Betz H| title =Assembly of the inhibitory glycine receptor: identification of amino acid sequence motifs governing subunit stoichiometry | journal =Neuron | volume =11 | issue =6 | pages =1049–1056 | publisher = | date =1993 | url = | doi = 10.1016/0896-6273(93)90218-G| pmid =8274276 | accessdate = ] or four α1 subunits and one β subunit.cite journal | last =Kuhse | first =J | authorlink = | coauthors =Betz H, Kirsch J | title =The inhibitory glycine receptor: architecture, synaptic localization and molecular pathology of a postsynaptic ion-channel complex | journal =Current Opinion in Neurobiology | volume =5 | issue =3 | pages =318–323 | publisher = | date =1995 | url = | doi = 10.1016/0959-4388(95)80044-1| pmid =7580154 | accessdate = ] The α-subunits are also able to form functional homo-
pentamer ic receptors in heterologous expression systems in African clawed frog'soocyte s or mammaliancell line s, and the α1 homomeric receptor is essential for studies of channelpharmacokinetics andpharmacodynamics .cite journal | last = Lewis | first =TM | authorlink = | coauthors =Schofield PR, McClellan AM | title =Kinetic determinants of agonist action at the recombinant human glycine receptor | journal =Journal of Physiology | volume =549 | issue =Part 2 | pages =361–374 | publisher = | date =2003 | url =http://jp.physoc.org/cgi/content/full/549/2/361 | doi = 10.1113/jphysiol.2002.037796| pmid =12679369 | accessdate =2007-01-16 ]Pathology
A mutation in GLRA1 is responsible for some cases of
stiff person syndrome . [OMIM|184850|STIFF-PERSON SYNDROME; SPS]Research
Quantum dots have been used to track the diffusion of glycine receptors into thesynapse of neurons. [cite journal |author=Dahan M, Lévi S, Luccardini C, Rostaing P, Riveau B, Triller A |title=Diffusion dynamics of glycine receptors revealed by single-quantum dot tracking |journal=Science |volume=302 |issue=5644 |pages=442–5 |year=2003 |pmid=14564008 |doi=10.1126/science.1088525]References
External links
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