Glutamate receptor 2

Details

Name
Glutamate receptor 2
Synonyms
  • AMPA-selective glutamate receptor 2
  • GluA2
  • GluR-2
  • GluR-B
  • GluR-K2
  • GLUR2
  • Glutamate receptor ionotropic, AMPA 2
Gene Name
GRIA2
Organism
Humans
Amino acid sequence
>lcl|BSEQ0001654|Glutamate receptor 2
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
Number of residues
883
Molecular Weight
98820.32
Theoretical pI
7.66
GO Classification
Functions
AMPA glutamate receptor activity / extracellular-glutamate-gated ion channel activity / ionotropic glutamate receptor activity
Processes
ion transmembrane transport / ionotropic glutamate receptor signaling pathway / signal transduction / synaptic transmission / synaptic transmission, glutamatergic
Components
AMPA glutamate receptor complex / cell junction / dendrite / endocytic vesicle membrane / endoplasmic reticulum membrane / integral component of plasma membrane / plasma membrane / postsynaptic membrane / synaptic vesicle
General Function
Ionotropic glutamate receptor activity
Specific Function
Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.
Pfam Domain Function
Transmembrane Regions
544-564 617-637 813-833
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0016219|Glutamate receptor 2 (GRIA2)
ATGCAAAAGATTATGCATATTTCTGTCCTCCTTTCTCCTGTTTTATGGGGACTGATTTTT
GGTGTCTCTTCTAACAGCATACAGATAGGGGGGCTATTTCCTAGGGGCGCCGATCAAGAA
TACAGTGCATTTCGAGTAGGGATGGTTCAGTTTTCCACTTCGGAGTTCAGACTGACACCC
CACATCGACAATTTGGAGGTGGCAAACAGCTTCGCAGTCACTAATGCTTTCTGCTCCCAG
TTTTCGAGAGGAGTCTATGCTATTTTTGGATTTTATGACAAGAAGTCTGTAAATACCATC
ACATCATTTTGCGGAACACTCCACGTCTCCTTCATCACTCCCAGCTTCCCAACAGATGGC
ACACATCCATTTGTCATTCAGATGAGACCCGACCTCAAAGGAGCTCTCCTTAGCTTGATT
GAATACTATCAATGGGACAAGTTTGCATACCTCTATGACAGTGACAGAGGCTTATCAACA
CTGCAAGCTGTGCTGGATTCTGCTGCTGAAAAGAAATGGCAAGTGACTGCTATCAATGTG
GGAAACATTAACAATGACAAGAAAGATGAGATGTACCGATCACTTTTTCAAGATCTGGAG
TTAAAAAAGGAACGGCGTGTAATTCTGGACTGTGAAAGGGATAAAGTAAACGACATTGTA
GACCAGGTTATTACCATTGGAAAACATGTTAAAGGGTACCACTACATCATTGCAAATCTG
GGATTTACTGATGGAGACCTATTAAAAATCCAGTTTGGAGGTGCAAATGTCTCTGGATTT
CAGATAGTGGACTATGATGATTCGTTGGTATCTAAATTTATAGAAAGATGGTCAACACTG
GAAGAAAAAGAATACCCTGGAGCTCACACAACAACAATTAAGTATACTTCTGCTCTGACC
TATGATGCCGTTCAAGTGATGACTGAAGCCTTCCGCAACCTAAGGAAGCAAAGAATTGAA
ATCTCCCGAAGGGGGAATGCAGGAGACTGTCTGGCAAACCCAGCAGTGCCCTGGGGACAA
GGTGTAGAAATAGAAAGGGCCCTCAAACAGGTTCAGGTTGAAGGTCTCTCAGGAAATATA
AAGTTTGACCAGAATGGAAAAAGAATAAACTATACAATTAACATCATGGAGCTCAAAACT
AATGGGCCCCGGAAGATTGGCTACTGGAGTGAAGTGGACAAAATGGTTGTTACCCTTACT
GAGCTCCCTTCTGGAAATGACACCTCTGGGCTTGAGAATAAGACTGTTGTTGTCACCACA
ATTTTGGAATCTCCGTATGTTATGATGAAGAAAAATCATGAAATGCTTGAAGGCAATGAG
CGCTATGAGGGCTACTGTGTTGACCTGGCTGCAGAAATCGCCAAACATTGTGGGTTCAAG
TACAAGTTGACAATTGTTGGTGATGGCAAGTATGGGGCCAGGGATGCAGACACGAAAATT
TGGAATGGGATGGTTGGAGAACTTGTATATGGGAAAGCTGATATTGCAATTGCTCCATTA
ACTATTACCCTTGTGAGAGAAGAGGTGATTGACTTCTCAAAGCCCTTCATGAGCCTCGGG
ATATCTATCATGATCAAGAAGCCTCAGAAGTCCAAACCAGGAGTGTTTTCCTTTCTTGAT
CCTTTAGCCTATGAGATCTGGATGTGCATTGTTTTTGCCTACATTGGGGTCAGTGTAGTT
TTATTCCTGGTCAGCAGATTTAGCCCCTACGAGTGGCACACTGAGGAGTTTGAAGATGGA
AGAGAAACACAAAGTAGTGAATCAACTAATGAATTTGGGATTTTTAATAGTCTCTGGTTT
TCCTTGGGTGCCTTTATGCGGCAAGGATGCGATATTTCGCCAAGATCCCTCTCTGGGCGC
ATTGTTGGAGGTGTGTGGTGGTTCTTTACCCTGATCATAATCTCCTCCTACACGGCTAAC
TTAGCTGCCTTCCTGACTGTAGAGAGGATGGTGTCTCCCATCGAAAGTGCTGAGGATCTT
TCTAAGCAAACAGAAATTGCTTATGGAACATTAGACTCTGGCTCCACTAAAGAGTTTTTC
AGGAGATCTAAAATTGCAGTGTTTGATAAAATGTGGACCTACATGCGGAGTGCGGAGCCC
TCTGTGTTTGTGAGGACTACGGCCGAAGGGGTGGCTAGAGTGCGGAAGTCCAAAGGGAAA
TATGCCTACTTGTTGGAGTCCACGATGAACGAGTACATTGAGCAAAGGAAGCCTTGCGAC
ACCATGAAAGTTGGTGGAAACCTGGATTCCAAAGGCTATGGCATCGCAACACCTAAAGGA
TCCTCATTAAGAACCCCAGTAAATCTTGCAGTATTGAAACTCAGTGAGCAAGGCGTCTTA
GACAAGCTGAAAAACAAATGGTGGTACGATAAAGGTGAATGTGGAGCCAAGGACTCTGGA
AGTAAGGAAAAGACCAGTGCCCTCAGTCTGAGCAACGTTGCTGGAGTATTCTACATCCTT
GTCGGGGGCCTTGGTTTGGCAATGCTGGTGGCTTTGATTGAGTTCTGTTACAAGTCAAGG
GCCGAGGCGAAACGAATGAAGGTGGCAAAGAATGCACAGAATATTAACCCATCTTCCTCG
CAGAATTCACAGAATTTTGCAACTTATAAGGAAGGTTACAACGTATATGGCATCGAAAGT
GTTAAAATTTAG
Chromosome Location
4
Locus
4q32-q33
External Identifiers
ResourceLink
UniProtKB IDP42262
UniProtKB Entry NameGRIA2_HUMAN
GenBank Protein ID493134
GenBank Gene IDL20814
GenAtlas IDGRIA2
HGNC IDHGNC:4572
General References
  1. Sun W, Ferrer-Montiel AV, Montal M: Primary structure and functional expression of the AMPA/kainate receptor subunit 2 from human brain. Neuroreport. 1994 Jan 12;5(4):441-4. [PubMed:8003671]
  2. Hillier LW, Graves TA, Fulton RS, Fulton LA, Pepin KH, Minx P, Wagner-McPherson C, Layman D, Wylie K, Sekhon M, Becker MC, Fewell GA, Delehaunty KD, Miner TL, Nash WE, Kremitzki C, Oddy L, Du H, Sun H, Bradshaw-Cordum H, Ali J, Carter J, Cordes M, Harris A, Isak A, van Brunt A, Nguyen C, Du F, Courtney L, Kalicki J, Ozersky P, Abbott S, Armstrong J, Belter EA, Caruso L, Cedroni M, Cotton M, Davidson T, Desai A, Elliott G, Erb T, Fronick C, Gaige T, Haakenson W, Haglund K, Holmes A, Harkins R, Kim K, Kruchowski SS, Strong CM, Grewal N, Goyea E, Hou S, Levy A, Martinka S, Mead K, McLellan MD, Meyer R, Randall-Maher J, Tomlinson C, Dauphin-Kohlberg S, Kozlowicz-Reilly A, Shah N, Swearengen-Shahid S, Snider J, Strong JT, Thompson J, Yoakum M, Leonard S, Pearman C, Trani L, Radionenko M, Waligorski JE, Wang C, Rock SM, Tin-Wollam AM, Maupin R, Latreille P, Wendl MC, Yang SP, Pohl C, Wallis JW, Spieth J, Bieri TA, Berkowicz N, Nelson JO, Osborne J, Ding L, Meyer R, Sabo A, Shotland Y, Sinha P, Wohldmann PE, Cook LL, Hickenbotham MT, Eldred J, Williams D, Jones TA, She X, Ciccarelli FD, Izaurralde E, Taylor J, Schmutz J, Myers RM, Cox DR, Huang X, McPherson JD, Mardis ER, Clifton SW, Warren WC, Chinwalla AT, Eddy SR, Marra MA, Ovcharenko I, Furey TS, Miller W, Eichler EE, Bork P, Suyama M, Torrents D, Waterston RH, Wilson RK: Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature. 2005 Apr 7;434(7034):724-31. [PubMed:15815621]
  3. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [PubMed:15489334]
  4. Paschen W, Hedreen JC, Ross CA: RNA editing of the glutamate receptor subunits GluR2 and GluR6 in human brain tissue. J Neurochem. 1994 Nov;63(5):1596-602. [PubMed:7523595]
  5. Kolleker A, Zhu JJ, Schupp BJ, Qin Y, Mack V, Borchardt T, Kohr G, Malinow R, Seeburg PH, Osten P: Glutamatergic plasticity by synaptic delivery of GluR-B(long)-containing AMPA receptors. Neuron. 2003 Dec 18;40(6):1199-212. [PubMed:14687553]
  6. Dev KK, Nakanishi S, Henley JM: The PDZ domain of PICK1 differentially accepts protein kinase C-alpha and GluR2 as interacting ligands. J Biol Chem. 2004 Oct 1;279(40):41393-7. Epub 2004 Jul 9. [PubMed:15247289]
  7. Salussolia CL, Gan Q, Kazi R, Singh P, Allopenna J, Furukawa H, Wollmuth LP: A eukaryotic specific transmembrane segment is required for tetramerization in AMPA receptors. J Neurosci. 2013 Jun 5;33(23):9840-5. doi: 10.1523/JNEUROSCI.2626-12.2013. [PubMed:23739980]
  8. Clayton A, Siebold C, Gilbert RJ, Sutton GC, Harlos K, McIlhinney RA, Jones EY, Aricescu AR: Crystal structure of the GluR2 amino-terminal domain provides insights into the architecture and assembly of ionotropic glutamate receptors. J Mol Biol. 2009 Oct 9;392(5):1125-32. doi: 10.1016/j.jmb.2009.07.082. Epub 2009 Aug 3. [PubMed:19651138]
  9. Ward SE, Harries M, Aldegheri L, Andreotti D, Ballantine S, Bax BD, Harris AJ, Harker AJ, Lund J, Melarange R, Mingardi A, Mookherjee C, Mosley J, Neve M, Oliosi B, Profeta R, Smith KJ, Smith PW, Spada S, Thewlis KM, Yusaf SP: Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator. J Med Chem. 2010 Aug 12;53(15):5801-12. doi: 10.1021/jm1005429. [PubMed:20614889]
  10. Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, Urwyler S: Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3358-61. doi: 10.1016/j.bmcl.2011.04.017. Epub 2011 Apr 8. [PubMed:21531559]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00142Glutamic Acidapproved, nutraceuticalunknownDetails
DB01664(S)-DES-ME-AMPAexperimentalunknownDetails
DB02057(S)-AMPAexperimentalunknownDetails
DB023472-Amino-3-(5-Tert-Butyl-3-(Phosphonomethoxy)-4-Isoxazolyl)Propionic AcidexperimentalunknownDetails
DB02818Iodo-WillardiineexperimentalunknownDetails
DB02966Fluoro-WillardiineexperimentalunknownDetails
DB02999QuisqualateexperimentalunknownDetails
DB03240(S)-2-Amino-3-(1,3,5,7-Pentahydro-2,4-Dioxo-Cyclopenta[E]Pyrimidin-1-Yl) Proionic AcidexperimentalunknownDetails
DB03319(2S)-2-Ammonio-3-[5-(2-methyl-2-propanyl)-3-oxido-1,2-oxazol-4-yl]propanoateexperimentalunknownDetails
DB03759FG-9041experimentalunknownDetails
DB04000Bromo-WillardiineexperimentalunknownDetails
DB04129WillardiineexperimentalunknownDetails
DB041522-Amino-3-(3-Hydroxy-7,8-Dihydro-6h-Cyclohepta[D]-4-Isoxazolyl)Propionic AcidexperimentalunknownDetails
DB04982TalampanelinvestigationalunknownDetails
DB05047CX717illicit, investigationalunknownDetails
DB04599AniracetamexperimentalunknownDetails
DB07455N,N'-[biphenyl-4,4'-diyldi(2R)propane-2,1-diyl]dimethanesulfonamideexperimentalunknownDetails
DB075982,3,6A,7,8,9-HEXAHYDRO-11H-[1,4]DIOXINO[2,3-G]PYRROLO[2,1-B][1,3]BENZOXAZIN-11-ONEexperimentalunknownDetails
DB08303(3S)-3-cyclopentyl-6-methyl-7-[(4-methylpiperazin-1-yl)sulfonyl]-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxideexperimentalunknownDetails
DB08304(3R)-3-cyclopentyl-7-[(4-methylpiperazin-1-yl)sulfonyl]-3,4-dihydro-2H-1,2-benzothiazine 1,1-dioxideexperimentalunknownDetails
DB08305(3R)-3-cyclopentyl-6-methyl-7-[(4-methylpiperazin-1-yl)sulfonyl]-3,4-dihydro-2H-1,2-benzothiazine 1,1-dioxideexperimentalunknownDetails
DB04798THIO-ATPAexperimentalunknownDetails
DB01351Amobarbitalapproved, illicitunknownantagonistDetails
DB00312Pentobarbitalapproved, investigational, vet_approvedunknownantagonistDetails
DB00237Butabarbitalapproved, illicitunknownantagonistDetails
DB00241Butalbitalapproved, illicitunknownantagonistDetails
DB00306Talbutalapproved, illicitunknownantagonistDetails
DB00418Secobarbitalapproved, vet_approvedunknownantagonistDetails
DB00463MetharbitalwithdrawnunknownantagonistDetails
DB00599Thiopentalapproved, vet_approvedunknownantagonistDetails
DB00794Primidoneapproved, vet_approvedunknownantagonistDetails
DB00849MethylphenobarbitalapprovedunknownantagonistDetails
DB01174Phenobarbitalapproved, investigationalunknownantagonistDetails
DB01352Aprobarbitalexperimental, illicitunknownantagonistDetails
DB01353Butobarbitalapproved, illicitunknownantagonistDetails
DB01354HeptabarbitalexperimentalunknownantagonistDetails
DB01355HexobarbitalexperimentalunknownantagonistDetails
DB01483BarbitalillicitunknownantagonistDetails
DB01496Barbituric acid derivativeexperimental, illicitunknownantagonistDetails
DB01346Quinidine barbiturateapprovedunknownantagonistDetails
DB00898EthanolapprovedunknownDetails
DB13146Fluciclovine (18F)approvednoinhibitorDetails