Glycine receptor

From Wikipedia, the free encyclopedia

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 the central nervous system.

1 Activation and inactivation
2 Arrangement of subunits
3 Pathology
4 References
5 External links

[edit] Activation and inactivation

The receptor can be activated by a range of simple amino acids including glycine, β-alanine and taurine, and can be selectively blocked by the high-affinity competitive antagonist strychnine.^[1]

[edit] Arrangement of subunits

Strychnine-sensitive glycine receptors are members of a family of Ligand-gated ion channels. Receptors of this family are arranged as five subunits surrounding a central pore, with each subunit composed of four α helical transmembrane segments.^[2]

There are presently four known isoforms of the α-subunit (α_1-4) of GlyR that are essential to bind ligands (GLRA1, GLRA2, GLRA3, GLRA4) and a single β-subunit (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 subunits ^[3] or four α₁ subunits and one β subunit.^[4] The α-subunits are also able to form functional homo-pentameric receptors in heterologous expression systems in African clawed frog's oocytes or mammalian cell lines,^[4] and the α₁ homomeric receptor is essential for studies of channel pharmacokinetics and pharmacodynamics.^[5]

[edit] Pathology

A mutation in GLRA1 is responsible for some cases of stiff person syndrome.^[6]

[edit] References

^ Rajendra, S; Lynch JW, Schofield PR (1997). "The glycine receptor". Pharmacology and Therapeutics 73 (2): 121-146. PMID 9131721. Retrieved on 2007-01-16.
^ Miyazawa, A; Fujiyoshi Y, Unwin N (2003). "Structure and gating mechanism of the acetylcholine receptor pore". Nature 423 (6943): 949-955. PMID 12827192. Retrieved on 2007-01-16.
^ Kuhse, J; Laube B, Magalei D, Betz H (1993). "Assembly of the inhibitory glycine receptor: identification of amino acid sequence motifs governing subunit stoichiometry". Neuron 11 (6): 1049-1056. PMID 8274276. Retrieved on 2007-01-16.
^ ^a ^b Kuhse, J; Betz H, Kirsch J (1995). "The inhibitory glycine receptor: architecture, synaptic localization and molecular pathology of a postsynaptic ion-channel complex". Current Opinion in Neurobiology 5 (3): 318-323. PMID 7580154. Retrieved on 2007-01-16.
^ Lewis, TM; Schofield PR, McClellan AM (2003). "Kinetic determinants of agonist action at the recombinant human glycine receptor". Journal of Physiology 549 (Part 2): 361-374. PMID 12679369. Retrieved on 2007-01-16.
^ http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=184850