8P3Y
 
 | | Homomeric GluA2 flip R/G-edited Q/R-edited F231A mutant in tandem with TARP gamma-2, desensitized conformation 3 | | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | | Authors: | Krieger, J.M, Zhang, D, Yamashita, K, Greger, I.H. | | Deposit date: | 2023-05-18 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3.55 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8P3S
 | | Homomeric GluA2 flip R/G-unedited Q/R-edited F231A mutant in tandem with TARP gamma-2, desensitized conformation 2 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 2, ... | | Authors: | Zhang, D, Krieger, J.M, Yamashita, K, Greger, I. | | Deposit date: | 2023-05-18 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.95 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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5YBG
 | | Crystal structure of the GluA2o LBD in complex with glutamate and LY451395 | | Descriptor: | ACETATE ION, GLUTAMIC ACID, GLYCEROL, ... | | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | | Deposit date: | 2017-09-04 | | Release date: | 2018-01-17 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.52 Å) | | Cite: | HBT1, a Novel AMPA Receptor Potentiator with Lower Agonistic Effect, Avoided Bell-Shaped Response in In Vitro BDNF Production.
J. Pharmacol. Exp. Ther., 364, 2018
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8C2H
 | | Transmembrane domain of active state homomeric GluA1 AMPA receptor in tandem with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 1 flip isoform, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-22 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.64 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1P
 | | Active state homomeric GluA1 AMPA receptor in complex with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, CYCLOTHIAZIDE, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C2I
 | | Transmembrane domain of resting state homomeric GluA1 AMPA receptor in complex with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 1 flip isoform, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-22 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1S
 | | Transmembrane domain of resting state homomeric GluA2 F231A mutant AMPA receptor in complex with TARP gamma 2 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 2, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1R
 | | Resting state homomeric GluA2 F231A mutant AMPA receptor in complex with TARP gamma-2 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 2, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1Q
 | | Resting state homomeric GluA1 AMPA receptor in complex with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 1 flip isoform, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.82 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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6CNA
 | | GluN1-GluN2B NMDA receptors with exon 5 | | 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 ionotropic, ... | | Authors: | Furukawa, H, Grant, T, Grigorieff, N. | | Deposit date: | 2018-03-07 | | Release date: | 2018-10-03 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (4.6 Å) | | Cite: | Structural Mechanism of Functional Modulation by Gene Splicing in NMDA Receptors.
Neuron, 98, 2018
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5ZG3
 | | Crystal structure of the GluA2o LBD in complex with glutamate and TAK-137 | | Descriptor: | 9-(4-phenoxyphenyl)-3,4-dihydro-2H-2lambda~6~-pyrido[2,1-c][1,2,4]thiadiazine-2,2-dione, ACETATE ION, GLUTAMIC ACID, ... | | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | | Deposit date: | 2018-03-07 | | Release date: | 2019-01-16 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window.
Neuropsychopharmacology, 44, 2019
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6DM0
 | | Open state GluA2 in complex with STZ and blocked by IEM-1460, after micelle signal subtraction | | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, ... | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Vassilevski, A.A, Sobolevsky, A.I. | | Deposit date: | 2018-06-04 | | Release date: | 2018-08-22 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (4.4 Å) | | Cite: | Mechanisms of Channel Block in Calcium-Permeable AMPA Receptors.
Neuron, 99, 2018
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6DLZ
 | | Open state GluA2 in complex with STZ after micelle signal subtraction | | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Vassilevski, A.A, Sobolevsky, A.I. | | Deposit date: | 2018-06-04 | | Release date: | 2018-08-22 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Mechanisms of Channel Block in Calcium-Permeable AMPA Receptors.
Neuron, 99, 2018
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5ZG1
 | | Crystal structure of the GluA2o LBD in complex with glutamate and Compound-2 | | Descriptor: | 9-(4-~{tert}-butylphenyl)-3,4-dihydropyrido[2,1-c][1,2,4]thiadiazine 2,2-dioxide, GLUTAMIC ACID, GLYCEROL, ... | | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | | Deposit date: | 2018-03-07 | | Release date: | 2019-01-16 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.32 Å) | | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window.
Neuropsychopharmacology, 44, 2019
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5ZG2
 | | Crystal structure of the GluA2o LBD in complex with ZK200775 and Compound-2 | | Descriptor: | 9-(4-~{tert}-butylphenyl)-3,4-dihydropyrido[2,1-c][1,2,4]thiadiazine 2,2-dioxide, ACETATE ION, GLYCEROL, ... | | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | | Deposit date: | 2018-03-07 | | Release date: | 2019-01-16 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.25 Å) | | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window.
Neuropsychopharmacology, 44, 2019
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5ZG0
 | | Crystal structure of the GluA2o LBD in complex with glutamate and Compound-1 | | Descriptor: | 9-{4-[(propan-2-yl)oxy]phenyl}-3,4-dihydro-2H-2lambda~6~-pyrido[2,1-c][1,2,4]thiadiazine-2,2-dione, ACETATE ION, GLUTAMIC ACID, ... | | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | | Deposit date: | 2018-03-07 | | Release date: | 2019-01-16 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.58 Å) | | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window.
Neuropsychopharmacology, 44, 2019
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6DM1
 | | Open state GluA2 in complex with STZ and blocked by NASPM, after micelle signal subtraction | | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, ... | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Vassilevski, A.A, Sobolevsky, A.I. | | Deposit date: | 2018-06-04 | | Release date: | 2018-08-22 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (4.2 Å) | | Cite: | Mechanisms of Channel Block in Calcium-Permeable AMPA Receptors.
Neuron, 99, 2018
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5YBF
 | | Crystal structure of the GluA2o LBD in complex with glutamate and HBT1 | | Descriptor: | 2-[2-[5-methyl-3-(trifluoromethyl)pyrazol-1-yl]ethanoylamino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, ACETATE ION, GLUTAMIC ACID, ... | | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | | Deposit date: | 2017-09-04 | | Release date: | 2018-01-17 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | HBT1, a Novel AMPA Receptor Potentiator with Lower Agonistic Effect, Avoided Bell-Shaped Response in In Vitro BDNF Production.
J. Pharmacol. Exp. Ther., 364, 2018
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6FAZ
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with the positive allosteric modulator TDPAM01 at 1.4 A resolution. | | Descriptor: | 1,2-ETHANEDIOL, 6,6'-(Ethane-1,2-diyl)bis(4-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide), ACETATE ION, ... | | Authors: | Nielsen, L, Laulumaa, S, Kastrup, J.S. | | Deposit date: | 2017-12-18 | | Release date: | 2018-11-21 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds.
J. Med. Chem., 61, 2018
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6F29
 | | Crystal structure of the kainate receptor GluK3 ligand binding domain in complex with (S)-1-[2-Amino-2-carboxyethyl]-5,7-dihydrothieno[3,4-d]pyrimidin-2,4(1H,3H)-dione at resolution 2.6A | | Descriptor: | (2~{S})-2-azanyl-3-[2,4-bis(oxidanylidene)-5,7-dihydrothieno[3,4-d]pyrimidin-1-yl]propanoic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2017-11-23 | | Release date: | 2018-02-28 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | ( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
J. Med. Chem., 61, 2018
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1FTJ
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1FTM
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1FTK
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1FW0
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1FTO
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