GluK2 | Ionotropic glutamate receptors | IUPHAR/BPS Guide to PHARMACOLOGY

GluK2

Target id: 451

Nomenclature: GluK2

Family: Ionotropic glutamate receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GluK2 in GtoImmuPdb

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 908 6q16.3-q21 GRIK2 glutamate ionotropic receptor kainate type subunit 2
Mouse 3 1 869 10 B3 Grik2 glutamate receptor, ionotropic, kainate 2 (beta 2)
Rat 3 1 908 20q13 Grik2 glutamate ionotropic receptor kainate type subunit 2
Previous and Unofficial Names
EAA4 | GLUK6 | GluR6 | MRT6 | glutamate receptor 6 | Glurbeta2 | glutamate receptor, ionotropic, kainate 2 | glutamate receptor, ionotropic, kainate 2 (beta 2) | glutamate receptor
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Electron density map of GluK2 desensitized state in complex with 2S,4R-4-methylglutamate
PDB Id:  4UQQ
Ligand:  SYM2081
Resolution:  0.0Å
Species:  Rat
References:  2
Natural/Endogenous Ligands
L-glutamic acid

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]kainate Rn Full agonist 8.2 pKd 7
pKd 8.2 (Kd 6.6x10-9 M) [7]
dysiherbaine Rn Full agonist 8.9 pKi 5
pKi 8.9 (Ki 1.2x10-9 M) [5]
kainate Rn Agonist 7.8 – 8.4 pKi 1,7
pKi 7.8 – 8.4 (Ki 1.43x10-8 – 3.7x10-9 M) [1,7]
Description: Measured using kainic acid in rat forebrain homogenate.
SYM2081 Hs Agonist 8.0 pKi 3
pKi 8.0 (Ki 1x10-8 M) [3]
SYM2081 Rn Agonist 7.8 – 8.0 pKi 4,7
pKi 7.8 – 8.0 (Ki 1.7x10-8 – 9.8x10-9 M) [4,7]
Description: Measuring displacement of [3H]kainate binding to recombinant rGluR6 receptors.
domoic acid Hs Full agonist 7.7 pKi 1
pKi 7.7 (Ki 1.83x10-8 M) [1]
Description: Measuring displacement of [3H]Kainate binding by domoate.
kainate Hs Full agonist 7.3 – 7.5 pKi 1,6
pKi 7.3 – 7.5 (Ki 5.3x10-8 – 3.2x10-8 M) [1,6]
Description: Measured using kainic acid.
LY339434 Hs Agonist 4.8 – 4.9 pKi 6
pKi 4.8 – 4.9 (Ki 1.541x10-5 – 1.204x10-5 M) [6]
SYM2081 Rn Full agonist 7.7 pIC50 7
pIC50 7.7 (IC50 1.9x10-8 M) [7]
[3H]SYM2081 Hs Full agonist - -
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
2,4-epi-neodysiherbaine Hs Antagonist - -
Allosteric Modulators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
concanavalin A Hs Positive - - - no

Not voltage dependent
Clinically-Relevant Mutations and Pathophysiology
Disease:  Mental retardation, autosomal recessive, 6; MRT6
Synonyms: Autosomal recessive non-syndromic intellectual disability [Orphanet: ORPHA88616]
OMIM: 611092
Orphanet: ORPHA88616

References

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1. Cantrell BE, Zimmerman DM, Monn JA, Kamboj RK, Hoo KH, Tizzano JP, Pullar IA, Farrell LN, Bleakman D. (1996) Synthesis of a series of aryl kainic acid analogs and evaluation in cells stably expressing the kainate receptor humGluR6. J. Med. Chem., 39 (19): 3617-24. [PMID:8809152]

2. Meyerson JR, Kumar J, Chittori S, Rao P, Pierson J, Bartesaghi A, Mayer ML, Subramaniam S. (2014) Structural mechanism of glutamate receptor activation and desensitization. Nature, 514 (7522): 328-34. [PMID:25119039]

3. Pedregal C, Collado I, Escribano A, Ezquerra J, Domínguez C, Mateo AI, Rubio A, Baker SR, Goldsworthy J, Kamboj RK et al.. (2000) 4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists. J. Med. Chem., 43 (10): 1958-68. [PMID:10821708]

4. Sagot E, Pickering DS, Pu X, Umberti M, Stensbøl TB, Nielsen B, Chapelet M, Bolte J, Gefflaut T, Bunch L. (2008) Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7. J. Med. Chem., 51 (14): 4093-103. [PMID:18578478]

5. Sakai R, Swanson GT, Shimamoto K, Green T, Contractor A, Ghetti A, Tamura-Horikawa Y, Oiwa C, Kamiya H. (2001) Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea. J. Pharmacol. Exp. Ther., 296 (2): 650-8. [PMID:11160654]

6. Small B, Thomas J, Kemp M, Hoo K, Ballyk B, Deverill M, Ogden AM, Rubio A, Pedregal C, Bleakman D. (1998) LY339434, a GluR5 kainate receptor agonist. Neuropharmacology, 37 (10-11): 1261-7. [PMID:9849663]

7. Zhou LM, Gu ZQ, Costa AM, Yamada KA, Mansson PE, Giordano T, Skolnick P, Jones KA. (1997) (2S,4R)-4-methylglutamic acid (SYM 2081): a selective, high-affinity ligand for kainate receptors. J. Pharmacol. Exp. Ther., 280 (1): 422-7. [PMID:8996224]

Contributors

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How to cite this page

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluK2. Last modified on 20/10/2015. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=451.