5L1E
 
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor CP465022 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 3-(2-chlorophenyl)-2-(2-{6-[(diethylamino)methyl]pyridin-2-yl}ethyl)-6-fluoroquinazolin-4(3H)-one, Glutamate receptor 2 | | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | Deposit date: | 2016-07-29 | | Release date: | 2016-10-19 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (4.37 Å) | | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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5KUH
 | | GluK2EM with LY466195 | | Descriptor: | (3S,4aR,6S,8aR)-6-{[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl}decahydroisoquinoline-3-carboxylic acid, Glutamate receptor ionotropic, kainate 2 | | Authors: | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | | Deposit date: | 2016-07-13 | | Release date: | 2016-09-07 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (11.6 Å) | | Cite: | Structural basis of kainate subtype glutamate receptor desensitization.
Nature, 537, 2016
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5L1G
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with GYKI-Br | | Descriptor: | (8R)-5-(4-amino-3-bromophenyl)-N,8-dimethyl-8,9-dihydro-2H,7H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2 | | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | Deposit date: | 2016-07-29 | | Release date: | 2016-10-19 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (4.507 Å) | | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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1IIT
 | | GLUR0 LIGAND BINDING CORE COMPLEX WITH L-SERINE | | Descriptor: | SERINE, Slr1257 protein | | Authors: | Mayer, M.L, Olson, R, Gouaux, E. | | Deposit date: | 2001-04-24 | | Release date: | 2001-09-19 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Mechanisms for ligand binding to GluR0 ion channels: crystal structures of the glutamate and serine complexes and a closed apo state.
J.Mol.Biol., 311, 2001
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1IIW
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3IL1
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, IDRA-21 | | Descriptor: | (3S)-7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | Deposit date: | 2009-08-06 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (1.998 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3ILT
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, trichlormethiazide | | Descriptor: | 6-CHLORO-3-(DICHLOROMETHYL)-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE-7-SULFONAMIDE 1,1-DIOXIDE, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | Deposit date: | 2009-08-07 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.107 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IK6
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, chlorothiazide | | Descriptor: | 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | Deposit date: | 2009-08-05 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.101 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IJO
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, althiazide | | Descriptor: | (3S)-6-chloro-3-[(prop-2-en-1-ylsulfanyl)methyl]-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | Deposit date: | 2009-08-04 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.003 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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6YK3
 | | Structure of the AMPA receptor GluA2o ligand-binding domain (S1S2J) in complex with the compound ( S) - 1- [2'-Amino-2'-carboxyethyl]-5 ,7- dihydropyrrolo[3,4-d]pyrimidin-2,4(1H,3H)-dione at resolution 1.20A | | Descriptor: | (S)-1-[2'-Amino-2'-carboxyethyl]-5,7-dihydropyrrolo[3,4-d]pyrimidin-2,4(1H,3H)-dione, AMMONIUM ION, CHLORIDE ION, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2020-04-05 | | Release date: | 2020-06-03 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.2 Å) | | Cite: | Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.
Acs Chem Neurosci, 11, 2020
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5MFW
 | | Crystal structure of the GluK1 ligand-binding domain in complex with kainate and BPAM-121 at 2.10 A resolution | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, ... | | Authors: | Larsen, A.P, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2016-11-18 | | Release date: | 2017-04-12 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
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3IJX
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, hydrochlorothiazide | | Descriptor: | 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | Deposit date: | 2009-08-05 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.881 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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6YK4
 | | Structure of the AMPA receptor GluA2o ligand-binding domain (S1S2J) in complex with the compound ( S) - 1- [2'-Amino-2'-carboxyethyl]-6-methyl-5 ,7- dihydropyrrolo[3,4-d]pyrimidin-2,4(1H,3H)-dione at resolution 1.00A | | Descriptor: | (2~{S})-2-azanyl-3-[6-methyl-2,4-bis(oxidanylidene)-5,7-dihydropyrrolo[3,4-d]pyrimidin-1-yl]propanoic acid, CHLORIDE ION, GLYCEROL, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2020-04-05 | | Release date: | 2020-06-03 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (0.999 Å) | | Cite: | Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.
Acs Chem Neurosci, 11, 2020
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3ILU
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, hydroflumethiazide | | Descriptor: | 6-(trifluoromethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | Deposit date: | 2009-08-07 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.003 Å) | | Cite: | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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6YK2
 | | Structure of the AMPA receptor GluA2o ligand-binding domain (S1S2J) in complex with the compound (S)-1-[2'-Amino-2'-carboxyethyl]-5,7-dihydrothieno[3,4-d]pyrimidin- 2,4(1H,3H)-dione at resolution 1.60A | | Descriptor: | (2~{S})-2-azanyl-3-[2,4-bis(oxidanylidene)-5,7-dihydrothieno[3,4-d]pyrimidin-1-yl]propanoic acid, CHLORIDE ION, GLYCEROL, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2020-04-05 | | Release date: | 2020-06-03 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.612 Å) | | Cite: | Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.
Acs Chem Neurosci, 11, 2020
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6YK5
 | | Structure of the AMPA receptor GluA2o ligand-binding domain (S1S2J) in complex with the compound (S)-1-(2'-Amino-2'-carboxyethyl)-5,7-dihydrofuro[3,4-d]- pyrimidine-2,4(1H,3H)-dione at resolution 1.15A | | Descriptor: | (S)-1-(2'-Amino-2'-carboxyethyl)-5,7-dihydrofuro[3,4-d]-pyrimidine-2,4(1H,3H)-dione, CHLORIDE ION, GLYCEROL, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2020-04-05 | | Release date: | 2020-06-03 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.15 Å) | | Cite: | Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.
Acs Chem Neurosci, 11, 2020
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5MFQ
 | | Crystal structure of the GluK1 ligand-binding domain in complex with kainate and BPAM-344 at 1.90 A resolution | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ... | | Authors: | Larsen, A.P, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2016-11-18 | | Release date: | 2017-04-12 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
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7KS0
 | | GluK2/K5 with 6-Cyano-7-nitroquinoxaline-2,3-dione (CNQX) | | Descriptor: | Glutamate receptor ionotropic, kainate 2, kainate 5,Green fluorescent protein chimera | | Authors: | Khanra, N, Brown, P.M.G.E, Perozzo, A.M, Bowie, D, Meyerson, J.R. | | Deposit date: | 2020-11-20 | | Release date: | 2021-03-24 | | Last modified: | 2021-07-07 | | Method: | ELECTRON MICROSCOPY (5.3 Å) | | Cite: | Architecture and structural dynamics of the heteromeric GluK2/K5 kainate receptor.
Elife, 10, 2021
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7KS3
 | | GluK2/K5 with L-Glu | | Descriptor: | Glutamate receptor ionotropic, kainate 2, kainate 5,Green fluorescent protein chimera | | Authors: | Khanra, N, Brown, P.M.G.E, Perozzo, A.M, Bowie, D, Meyerson, J.R. | | Deposit date: | 2020-11-20 | | Release date: | 2021-03-24 | | Last modified: | 2021-07-07 | | Method: | ELECTRON MICROSCOPY (5.8 Å) | | Cite: | Architecture and structural dynamics of the heteromeric GluK2/K5 kainate receptor.
Elife, 10, 2021
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6YK6
 | | Structure of the AMPA receptor GluA2o ligand-binding domain (S1S2J) in complex with the compound (S)-1-(2'-Amino-2'-carboxyethyl)furo[3,4-d]pyrimidin-2,4-dione at resolution 1.47A | | Descriptor: | (S)-1-(2'-Amino-2'-carboxyethyl)furo[3,4-d]pyrimidin-2,4-dione, CHLORIDE ION, GLYCEROL, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2020-04-05 | | Release date: | 2020-06-03 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.469 Å) | | Cite: | Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.
Acs Chem Neurosci, 11, 2020
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5M2V
 | | Structure of GluK1 ligand-binding domain (S1S2) in complex with (2S,4R)-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid at 3.18 A resolution | | Descriptor: | (2~{S},4~{R})-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Frydenvang, K, Kastrup, J.S, Kristensen, C.M. | | Deposit date: | 2016-10-13 | | Release date: | 2017-01-11 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (3.18 Å) | | Cite: | Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid.
J. Med. Chem., 60, 2017
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6XSR
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6WHX
 | | GluN1b-GluN2B NMDA receptor in complex with GluN2B antagonist SDZ 220-040, class 2 | | Descriptor: | (2S)-2-amino-3-[2',4'-dichloro-4-hydroxy-5-(phosphonomethyl)biphenyl-3-yl]propanoic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Ionotropic glutamate receptor , ... | | Authors: | Chou, T, Tajima, N, Furukawa, H. | | Deposit date: | 2020-04-08 | | Release date: | 2020-07-15 | | Last modified: | 2020-08-05 | | Method: | ELECTRON MICROSCOPY (4.09 Å) | | Cite: | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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6WHW
 | | GluN1b-GluN2B NMDA receptor in complex with GluN2B antagonist SDZ 220-040, class 1 | | Descriptor: | (2S)-2-amino-3-[2',4'-dichloro-4-hydroxy-5-(phosphonomethyl)biphenyl-3-yl]propanoic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Ionotropic glutamate receptor , ... | | Authors: | Chou, T, Tajima, N, Furukawa, H. | | Deposit date: | 2020-04-08 | | Release date: | 2020-07-15 | | Last modified: | 2020-08-05 | | Method: | ELECTRON MICROSCOPY (4.09 Å) | | Cite: | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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6WHU
 | | GluN1b-GluN2B NMDA receptor in complex with SDZ 220-040 and L689,560, class 1 | | Descriptor: | (2R,4S)-5,7-dichloro-4-[(phenylcarbamoyl)amino]-1,2,3,4-tetrahydroquinoline-2-carboxylic acid, (2S)-2-amino-3-[2',4'-dichloro-4-hydroxy-5-(phosphonomethyl)biphenyl-3-yl]propanoic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Chou, T, Tajima, N, Furukawa, H. | | Deposit date: | 2020-04-08 | | Release date: | 2020-08-05 | | Method: | ELECTRON MICROSCOPY (3.93 Å) | | Cite: | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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