5O9A
 
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J-L504Y-N775S) in complex with glutamate and BPAM121 at 1.78 A resolution | | Descriptor: | 1,2-ETHANEDIOL, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ... | | Authors: | Laulumaa, S, Rovinskaja, K, Frydenvang, K.A, Kastrup, J.S. | | Deposit date: | 2017-06-16 | | Release date: | 2018-01-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.
J. Med. Chem., 61, 2018
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5OEW
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with glutamate and positive allosteric modulator BPAM538 | | Descriptor: | 4-cyclopropyl-7-(3-methoxyphenoxy)-2,3-dihydro-1$l^{6},2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, GLUTAMIC ACID, ... | | Authors: | Larsen, A.P, Frydenvang, K.A, Kastrup, J.S. | | Deposit date: | 2017-07-10 | | Release date: | 2018-01-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.
J. Med. Chem., 61, 2018
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1GR2
 | | STRUCTURE OF A GLUTAMATE RECEPTOR LIGAND BINDING CORE (GLUR2) COMPLEXED WITH KAINATE | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, PROTEIN (GLUTAMATE RECEPTOR 2) | | Authors: | Armstrong, N, Sun, Y, Chen, G.Q, Gouaux, E. | | Deposit date: | 1998-09-17 | | Release date: | 1998-12-09 | | Last modified: | 2017-08-16 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structure of a glutamate-receptor ligand-binding core in complex with kainate.
Nature, 395, 1998
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1II5
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5NS9
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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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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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1FTK
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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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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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3U92
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1FTM
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1FW0
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1FTO
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3TZA
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with the antagonist (S)-2-amino-3-(2-(2-carboxyethyl)-5-chloro-4-nitrophenyl)propionic acid at 1.9A resolution | | Descriptor: | (S)-2-amino-3-(2-(2-carboxyethyl)-5-chloro-4-nitrophenyl)propionic acid, Glutamate receptor 2,Glutamate receptor 2, SULFATE ION | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2011-09-27 | | Release date: | 2011-10-26 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | A new phenylalanine derivative acts as an antagonist at the AMPA receptor GluA2 and introduces partial domain closure: synthesis, resolution, pharmacology, and crystal structure
J.Med.Chem., 54, 2011
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3U94
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3U93
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1FTL
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7OCA
 | | Resting state full-length GluA1/A2 heterotertramer in complex with TARP gamma 8 and CNIH2 | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Zhang, D, Watson, J.F, Matthews, P.M, Cais, O, Greger, I.H. | | Deposit date: | 2021-04-26 | | Release date: | 2021-06-09 | | Last modified: | 2021-06-30 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Gating and modulation of a hetero-octameric AMPA glutamate receptor.
Nature, 594, 2021
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7OCC
 | | NTD of resting state GluA1/A2 heterotertramer | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 1, ... | | Authors: | Zhang, D, Watson, J.F, Matthews, P.M, Cais, O, Greger, I.H. | | Deposit date: | 2021-04-26 | | Release date: | 2021-06-09 | | Last modified: | 2021-06-30 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Gating and modulation of a hetero-octameric AMPA glutamate receptor.
Nature, 594, 2021
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7OCD
 | | Resting state GluA1/A2 heterotetramer in complex with auxiliary subunit TARP gamma 8 (LBD-TMD) | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 6-nitro-2,3-bis(oxidanylidene)-1,4-dihydrobenzo[f]quinoxaline-7-sulfonamide, Glutamate receptor 2, ... | | Authors: | Zhang, D, Watson, J.F, Matthews, P.M, Cais, O, Greger, I.H. | | Deposit date: | 2021-04-26 | | Release date: | 2021-06-09 | | Last modified: | 2021-06-30 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Gating and modulation of a hetero-octameric AMPA glutamate receptor.
Nature, 594, 2021
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7OCE
 | | Resting state GluA1/A2 AMPA receptor in complex with TARP gamma 8 and CNIH2 (LBD-TMD) | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 6-nitro-2,3-bis(oxidanylidene)-1,4-dihydrobenzo[f]quinoxaline-7-sulfonamide, CHOLESTEROL, ... | | Authors: | Zhang, D, Watson, J.F, Matthews, P.M, Cais, O, Greger, I.H. | | Deposit date: | 2021-04-26 | | Release date: | 2021-06-09 | | Last modified: | 2021-06-30 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Gating and modulation of a hetero-octameric AMPA glutamate receptor.
Nature, 594, 2021
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7OCF
 | | Active state GluA1/A2 AMPA receptor in complex with TARP gamma 8 and CNIH2 (LBD-TMD) | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, CYCLOTHIAZIDE, GLUTAMIC ACID, ... | | Authors: | Zhang, D, Watson, J.F, Matthews, P.M, Cais, O, Greger, I.H. | | Deposit date: | 2021-04-26 | | Release date: | 2021-06-09 | | Last modified: | 2021-06-30 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Gating and modulation of a hetero-octameric AMPA glutamate receptor.
Nature, 594, 2021
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3TKD
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and cyclothiazide at 1.45 A resolution | | Descriptor: | CYCLOTHIAZIDE, GLUTAMATE RECEPTOR 2, GLUTAMIC ACID, ... | | Authors: | Krintel, C, Frydenvang, K, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2011-08-26 | | Release date: | 2011-09-21 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | Thermodynamics and structural analysis of positive allosteric modulation of the ionotropic glutamate receptor GluA2.
Biochem.J., 441, 2012
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