Metabotropic glutamate receptor 8
Metabotropic glutamate receptor 8 is a protein that in humans is encoded by the GRM8 gene.[5][6]
Function
[edit]L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions. The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group I includes GRM1 and GRM5 and these receptors have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. Alternative splice variants of GRM8 have been described but their full-length nature has not been determined.[6]
Ligands
[edit]- (S)-3,4-DCPG: agonist[7]
- AZ12216052: positive allosteric modulator[8]
See also
[edit]References
[edit]- ^ a b c GRCh38: Ensembl release 89: ENSG00000179603 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000024211 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ Scherer SW, Duvoisin RM, Kuhn R, Heng HH, Belloni E, Tsui LC (January 1996). "Localization of two metabotropic glutamate receptor genes, GRM3 and GRM8, to human chromosome 7q". Genomics. 31 (2): 230–233. doi:10.1006/geno.1996.0036. PMID 8824806.
- ^ a b "Entrez Gene: GRM8 glutamate receptor, metabotropic 8".
- ^ Thomas NK, Wright RA, Howson PA, Kingston AE, Schoepp DD, Jane DE (March 2001). "(S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord". Neuropharmacology. 40 (3): 311–318. doi:10.1016/S0028-3908(00)00169-6. PMID 11166323. S2CID 2872874.
- ^ Duvoisin RM, Pfankuch T, Wilson JM, Grabell J, Chhajlani V, Brown DG, et al. (October 2010). "Acute pharmacological modulation of mGluR8 reduces measures of anxiety". Behavioural Brain Research. 212 (2): 168–173. doi:10.1016/j.bbr.2010.04.006. PMC 2892883. PMID 20385173.
Further reading
[edit]- Scherer SW, Soder S, Duvoisin RM, Huizenga JJ, Tsui LC (September 1997). "The human metabotropic glutamate receptor 8 (GRM8) gene: a disproportionately large gene located at 7q31.3-q32.1". Genomics. 44 (2): 232–236. doi:10.1006/geno.1997.4842. PMID 9299241.
- Wu S, Wright RA, Rockey PK, Burgett SG, Arnold JS, Rosteck PR, et al. (January 1998). "Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells". Brain Research. Molecular Brain Research. 53 (1–2): 88–97. doi:10.1016/S0169-328X(97)00277-5. PMID 9473604.
- Malherbe P, Kratzeisen C, Lundstrom K, Richards JG, Faull RL, Mutel V (April 1999). "Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8". Brain Research. Molecular Brain Research. 67 (2): 201–210. doi:10.1016/S0169-328X(99)00050-9. PMID 10216218.
- Thomas NK, Wright RA, Howson PA, Kingston AE, Schoepp DD, Jane DE (March 2001). "(S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord". Neuropharmacology. 40 (3): 311–318. doi:10.1016/S0028-3908(00)00169-6. PMID 11166323. S2CID 2872874.
- Enz R (March 2002). "The actin-binding protein Filamin-A interacts with the metabotropic glutamate receptor type 7". FEBS Letters. 514 (2–3): 184–188. doi:10.1016/S0014-5793(02)02361-X. PMID 11943148. S2CID 44474808.
- Tang Z, El Far O, Betz H, Scheschonka A (November 2005). "Pias1 interaction and sumoylation of metabotropic glutamate receptor 8". The Journal of Biological Chemistry. 280 (46): 38153–38159. doi:10.1074/jbc.M508168200. PMID 16144832.
- Kobayashi Y, Akiyoshi J, Kanehisa M, Ichioka S, Tanaka Y, Tsuru J, et al. (February 2007). "Lack of polymorphism in genes encoding mGluR 7, mGluR 8, GABA(A) receptor alfa-6 subunit and nociceptin/orphanin FQ receptor and panic disorder". Psychiatric Genetics. 17 (1): 9. doi:10.1097/YPG.0b013e32801118bc. PMID 17167337.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.