2PBW
 
 | | Crystal Structure of the Ligand-Binding Core of iGluR5 in Complex with the Partial agonist Domoic Acid at 2.5 A Resolution | | Descriptor: | (2S,3S,4S)-2-CARBOXY-4-[(1Z,3E,5R)-5-CARBOXY-1-METHYL-1,3-HEXADIENYL]-3-PYRROLIDINEACETIC ACID, Glutamate receptor, ionotropic kainate 1 | | Authors: | Hald, H, Naur, P, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2007-03-29 | | Release date: | 2007-07-03 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Partial agonism and antagonism of the ionotropic glutamate receptor iGLuR5: structures of the ligand-binding core in complex with domoic acid and 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid.
J.Biol.Chem., 282, 2007
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4BDO
 | | Crystal structure of the GluK2 K531A-T779G LBD dimer in complex with kainate | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, GLUTAMATE RECEPTOR, IONOTROPIC KAINATE 2, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2012-10-05 | | Release date: | 2013-04-10 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Correlating Efficacy and Desensitization with Gluk2 Ligand-Binding Domain Movements.
Open Biol., 3, 2013
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4BDR
 | | Crystal structure of the GluK2 R775A LBD dimer in complex with kainate | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, CHLORIDE ION, GLUTAMATE RECEPTOR, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2012-10-05 | | Release date: | 2013-04-10 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Correlating Efficacy and Desensitization with Gluk2 Ligand-Binding Domain Movements.
Open Biol., 3, 2013
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4BDM
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4BDQ
 | | Crystal structure of the GluK2 R775A LBD dimer in complex with glutamate | | Descriptor: | GLUTAMATE RECEPTOR, IONOTROPIC KAINATE 2, GLUTAMIC ACID, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2012-10-05 | | Release date: | 2013-04-10 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Correlating Efficacy and Desensitization with Gluk2 Ligand-Binding Domain Movements.
Open Biol., 3, 2013
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4BDN
 | | Crystal structure of the GluK2 K531A-T779G LBD dimer in complex with glutamate | | Descriptor: | GLUTAMATE RECEPTOR, IONOTROPIC KAINATE 2, GLUTAMIC ACID, ... | | Authors: | Nayeem, N, Mayans, O, Green, T. | | Deposit date: | 2012-10-05 | | Release date: | 2013-04-10 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Correlating Efficacy and Desensitization with Gluk2 Ligand-Binding Domain Movements.
Open Biol., 3, 2013
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2AL4
 | | CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) IN COMPLEX WITH quisqualate and CX614. | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, 2,3,6A,7,8,9-HEXAHYDRO-11H-[1,4]DIOXINO[2,3-G]PYRROLO[2,1-B][1,3]BENZOXAZIN-11-ONE, Glutamate receptor 2, ... | | Authors: | Jin, R, Clark, S, Weeks, A.M, Dudman, J.T, Gouaux, E, Partin, K.M. | | Deposit date: | 2005-08-04 | | Release date: | 2005-10-25 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Mechanism of positive allosteric modulators acting on AMPA receptors.
J.Neurosci., 25, 2005
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2F36
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2F34
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2F35
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2QS4
 | | Crystal structure of the GluR5 ligand binding core dimer in complex with LY466195 at 1.58 Angstroms resolution | | Descriptor: | (3S,4aR,6S,8aR)-6-{[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl}decahydroisoquinoline-3-carboxylic acid, AMMONIUM ION, GLYCEROL, ... | | Authors: | Alushin, G.M, Jane, D.E, Mayer, M.L. | | Deposit date: | 2007-07-30 | | Release date: | 2008-08-05 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.58 Å) | | Cite: | Binding site and ligand flexibility revealed by high resolution crystal structures of GluK1 competitive antagonists.
Neuropharmacology, 60, 2011
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2QS1
 | | Crystal structure of the GluR5 ligand binding core dimer in complex with UBP315 at 1.80 Angstroms resolution | | Descriptor: | 3-({3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl}methyl)-4,5-dibromothiophene-2-carboxylic acid, CHLORIDE ION, Glutamate receptor, ... | | Authors: | Alushin, G.M, Jane, D.E, Mayer, M.L. | | Deposit date: | 2007-07-30 | | Release date: | 2008-08-05 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Binding site and ligand flexibility revealed by high resolution crystal structures of GluK1 competitive antagonists.
Neuropharmacology, 60, 2011
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2QS3
 | | Crystal structure of the GluR5 ligand binding core dimer in complex with UBP316 at 1.76 Angstroms resolution | | Descriptor: | 3-({3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl}methyl)-5-phenylthiophene-2-carboxylic acid, CHLORIDE ION, Glutamate receptor, ... | | Authors: | Alushin, G.M, Jane, D.E, Mayer, M.L. | | Deposit date: | 2007-07-30 | | Release date: | 2008-08-05 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.76 Å) | | Cite: | ACET is a highly potent and specific kainate receptor antagonist: characterisation and effects on hippocampal mossy fibre function.
Neuropharmacology, 56, 2009
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6QKZ
 | | Full length GluA1/2-gamma8 complex | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 6-nitro-2,3-bis(oxidanylidene)-1,4-dihydrobenzo[f]quinoxaline-7-sulfonamide, ... | | Authors: | Herguedas, B, Garcia-Nafria, J, Greger, I.G. | | Deposit date: | 2019-01-30 | | Release date: | 2019-03-27 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (6.3 Å) | | Cite: | Architecture of the heteromeric GluA1/2 AMPA receptor in complex with the auxiliary subunit TARP gamma 8.
Science, 364, 2019
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8VJ7
 | | GluA2 bound to GYKI-52466 and Glutamate, Inhibited State 2 | | Descriptor: | 4-[(5S,8R)-8-methyl-6,7,8,9-tetrahydro-2H,5H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl]aniline, GLUTAMIC ACID, Isoform Flip of Glutamate receptor 2 | | Authors: | Hale, W.D, Montano Romero, A, Huganir, R.L, Twomey, E.C. | | Deposit date: | 2024-01-05 | | Release date: | 2024-06-05 | | Last modified: | 2024-06-19 | | Method: | ELECTRON MICROSCOPY (4.85 Å) | | Cite: | Allosteric competition and inhibition in AMPA receptors.
Nat.Struct.Mol.Biol., 2024
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9B37
 | | Open state of kainate receptor GluK2 in complex with agonist glutamate and positive allosteric modulator BPAM344 bound to one concanavalin A dimer. Composite map. | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-3)-[2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-6)]beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Nadezhdin, K.D, Gangwar, S.P, Sobolevsky, A.I. | | Deposit date: | 2024-03-18 | | Release date: | 2024-05-22 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (6.66 Å) | | Cite: | Kainate receptor channel opening and gating mechanism.
Nature, 630, 2024
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9B36
 | | Open state of kainate receptor GluK2 in complex with agonist glutamate and positive allosteric modulator BPAM344 bound to two concanavalin A dimers. Composite map. | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-3)-[2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-6)]beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Nadezhdin, K.D, Gangwar, S.P, Sobolevsky, A.I. | | Deposit date: | 2024-03-18 | | Release date: | 2024-05-22 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (4.29 Å) | | Cite: | Kainate receptor channel opening and gating mechanism.
Nature, 630, 2024
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8VJ6
 | | GluA2 bound to GYKI-52466 and Glutamate, Inhibited State 1 | | Descriptor: | 4-[(5S,8R)-8-methyl-6,7,8,9-tetrahydro-2H,5H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl]aniline, Isoform Flip of Glutamate receptor 2 | | Authors: | Hale, W.D, Montano Romero, A, Huganir, R.L, Twomey, E.C. | | Deposit date: | 2024-01-05 | | Release date: | 2024-06-05 | | Last modified: | 2024-06-19 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Allosteric competition and inhibition in AMPA receptors.
Nat.Struct.Mol.Biol., 2024
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9B38
 | | Kainate receptor GluK2 in complex with agonist glutamate with pseudo 4-fold symmetrical ligand-binding domain layer | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, GLUTAMIC ACID, ... | | Authors: | Nadezhdin, K.D, Gangwar, S.P, Sobolevsky, A.I. | | Deposit date: | 2024-03-18 | | Release date: | 2024-05-22 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (3.36 Å) | | Cite: | Kainate receptor channel opening and gating mechanism.
Nature, 630, 2024
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9B39
 | | Kainate receptor GluK2 in complex with agonist glutamate with asymmetric ligand-binding domain layer | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, GLUTAMIC ACID, ... | | Authors: | Nadezhdin, K.D, Gangwar, S.P, Sobolevsky, A.I. | | Deposit date: | 2024-03-18 | | Release date: | 2024-05-22 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (3.84 Å) | | Cite: | Kainate receptor channel opening and gating mechanism.
Nature, 630, 2024
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5WEN
 | | GluA2 bound to GSG1L in digitonin, state 2 | | Descriptor: | Digitonin, Glutamate receptor 2,Germ cell-specific gene 1-like protein | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | | Deposit date: | 2017-07-10 | | Release date: | 2017-08-02 | | Last modified: | 2021-08-25 | | Method: | ELECTRON MICROSCOPY (6.8 Å) | | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors.
Nature, 549, 2017
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9B35
 | | Ligand-binding and transmembrane domains of kainate receptor GluK2 in the open state, a complex with agonist glutamate and positive allosteric modulator BPAM344 | | Descriptor: | GLUTAMIC ACID, Glutamate receptor ionotropic, kainate 2 | | Authors: | Nadezhdin, K.D, Gangwar, S.P, Sobolevsky, A.I. | | Deposit date: | 2024-03-18 | | Release date: | 2024-05-22 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Kainate receptor channel opening and gating mechanism.
Nature, 630, 2024
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6OVE
 | | Crystal structure of GluN1/GluN2A NMDA receptor agonist binding domains with glycine and antagonist, 4-propylphenyl-ACEPC | | Descriptor: | (3R,5S)-5-[(2R)-2-amino-2-carboxyethyl]-1-(4-propylphenyl)pyrazolidine-3-carboxylic acid, GLYCINE, Glutamate receptor ionotropic, ... | | Authors: | Syrenne, J.T, Mou, T.C, Tamborini, L, Pinto, A, Sprang, S.R, Hansen, K.B. | | Deposit date: | 2019-05-07 | | Release date: | 2020-05-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structure of GluN1/GluN2A NMDA receptor agonist binding domains with glycine and antagonist, 3-ethylphenyl-ACEPC
To Be Published
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6PEQ
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6SBT
 | | Structure of GluK1 ligand-binding domain (S1S2) in complex with N-(7-(1H-imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl benzamide at 2.3 A resolution | | Descriptor: | CHLORIDE ION, GLYCEROL, Glutamate receptor ionotropic, ... | | Authors: | Moellerud, S, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2019-07-22 | | Release date: | 2019-10-30 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | N-(7-(1H-Imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)benzamide, a New Kainate Receptor Selective Antagonist and Analgesic: Synthesis, X-ray Crystallography, Structure-Affinity Relationships, and in Vitro and in Vivo Pharmacology.
Acs Chem Neurosci, 10, 2019
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