3KFM
 
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6HC9
 | | STRUCTURE OF GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L504Y-N775S) IN COMPLEX WITH GLUTAMATE AND TDPAM02 AT 2.4 A RESOLUTION. | | 分子名称: | 6,6'-(ETHANE-1,2-DIYL)BIS(4-CYCLOPROPYL-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE 1,1-DIOXIDE), CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | 著者 | Laulumaa, S, Hansen, K.V, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2018-08-14 | | 公開日 | 2019-04-03 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor.
Acs Med.Chem.Lett., 10, 2019
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6IRA
 | | Structure of the human GluN1/GluN2A NMDA receptor in the glutamate/glycine-bound state at pH 7.8 | | 分子名称: | Glutamate receptor ionotropic, NMDA 1, NMDA 2A | | 著者 | Zhang, J, Chang, S, Zhang, X, Zhu, S. | | 登録日 | 2018-11-12 | | 公開日 | 2019-01-16 | | 最終更新日 | 2019-06-05 | | 実験手法 | ELECTRON MICROSCOPY (4.5 Å) | | 主引用文献 | Structural Basis of the Proton Sensitivity of Human GluN1-GluN2A NMDA Receptors
Cell Rep, 25, 2018
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8BN2
 | | Crystal structure of the ligand-binding domain (LBD) of human iGluR Delta-1 (GluD1) in complex with D-Serine | | 分子名称: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | 著者 | Heroven, C, Malinauskas, T, Aricescu, A.R. | | 登録日 | 2022-11-11 | | 公開日 | 2023-11-22 | | 最終更新日 | 2024-01-03 | | 実験手法 | X-RAY DIFFRACTION (1.63 Å) | | 主引用文献 | GluD1 binds GABA and controls inhibitory plasticity.
Science, 382, 2023
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8BN5
 | | Crystal structure of the ligand-binding domain (LBD) of human iGluR Delta-1 (GluD1) in complex with GABA | | 分子名称: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | 著者 | Heroven, C, Malinauskas, T, Aricescu, A.R. | | 登録日 | 2022-11-12 | | 公開日 | 2023-11-22 | | 最終更新日 | 2024-01-03 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | GluD1 binds GABA and controls inhibitory plasticity.
Science, 382, 2023
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8BLJ
 | | Crystal structure of the ligand-binding domain (LBD) of human iGluR Delta-1 (GluD1), apo state | | 分子名称: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | 著者 | Heroven, C, Malinauskas, T, Aricescu, A.R. | | 登録日 | 2022-11-09 | | 公開日 | 2023-11-22 | | 最終更新日 | 2024-01-03 | | 実験手法 | X-RAY DIFFRACTION (2.18 Å) | | 主引用文献 | GluD1 binds GABA and controls inhibitory plasticity.
Science, 382, 2023
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8BSU
 | | Crystal structure of the kainate receptor GluK3-H523A ligand binding domain in complex with kainate and the positive allosteric modulator BPAM344 at 2.9A resolution | | 分子名称: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, ... | | 著者 | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2022-11-26 | | 公開日 | 2023-12-13 | | 最終更新日 | 2024-07-03 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure.
Febs J., 291, 2024
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8BST
 | | Crystal structure of the kainate receptor GluK3-H523A ligand binding domain in complex with kainate at 2.7A resolution | | 分子名称: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, ACETATE ION, CHLORIDE ION, ... | | 著者 | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2022-11-26 | | 公開日 | 2023-12-13 | | 最終更新日 | 2024-04-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure.
Febs J., 291, 2024
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3M3L
 | | PEPA bound to the ligand binding domain of GluA2 (flop form) | | 分子名称: | 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | 登録日 | 2010-03-09 | | 公開日 | 2010-03-23 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA.
Biochemistry, 49, 2010
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8PIV
 | | Homomeric GluA2 flip R/G-unedited Q/R-edited F231A mutant in tandem with TARP gamma-2, desensitized conformation 1 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor, ... | | 著者 | Zhang, D, Krieger, J.M, Yamashita, K, Greger, I.H. | | 登録日 | 2023-06-22 | | 公開日 | 2023-08-30 | | 最終更新日 | 2023-10-11 | | 実験手法 | ELECTRON MICROSCOPY (3.46 Å) | | 主引用文献 | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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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 | | 分子名称: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, ... | | 著者 | Larsen, A.P, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2016-11-18 | | 公開日 | 2017-04-12 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
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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 | | 分子名称: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ... | | 著者 | Larsen, A.P, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2016-11-18 | | 公開日 | 2017-04-12 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
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6WI1
 | | GluN1b-GluN2B NMDA receptor in active conformation stabilized by inter-GluN1b-GluN2B subunit cross-linking | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Ionotropic glutamate receptor , ... | | 著者 | Chou, T, Tajima, N, Furukawa, H. | | 登録日 | 2020-04-08 | | 公開日 | 2020-07-15 | | 最終更新日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (3.62 Å) | | 主引用文献 | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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6WHR
 | | GluN1b-GluN2B NMDA receptor in non-active 2 conformation at 4 angstrom resolution | | 分子名称: | 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, ... | | 著者 | Chou, T, Tajima, N, Furukawa, H. | | 登録日 | 2020-04-08 | | 公開日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (3.99 Å) | | 主引用文献 | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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8QEZ
 | | Crystal structure of the AMPA receptor GluA2-L504Y-N775S ligand binding domain in complex with L-glutamate and positive allosteric modulator BPAM395 at 1.55A resolution | | 分子名称: | 6-chloranyl-4-cyclopropyl-2,3-dihydrothieno[3,2-e][1,2,4]thiadiazine 1,1-dioxide, ACETATE ION, CACODYLATE ION, ... | | 著者 | Dorosz, J, Laulumaa, S, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2023-09-01 | | 公開日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators.
Eur.J.Med.Chem., 264, 2023
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6WHX
 | | GluN1b-GluN2B NMDA receptor in complex with GluN2B antagonist SDZ 220-040, class 2 | | 分子名称: | (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 , ... | | 著者 | Chou, T, Tajima, N, Furukawa, H. | | 登録日 | 2020-04-08 | | 公開日 | 2020-07-15 | | 最終更新日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (4.09 Å) | | 主引用文献 | 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 | | 分子名称: | (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, ... | | 著者 | Chou, T, Tajima, N, Furukawa, H. | | 登録日 | 2020-04-08 | | 公開日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (3.93 Å) | | 主引用文献 | 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 | | 分子名称: | (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 , ... | | 著者 | Chou, T, Tajima, N, Furukawa, H. | | 登録日 | 2020-04-08 | | 公開日 | 2020-07-15 | | 最終更新日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (4.09 Å) | | 主引用文献 | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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6WHY
 | | GluN1b-GluN2B NMDA receptor in complex with GluN1 antagonist L689,560, class 1 | | 分子名称: | (2R,4S)-5,7-dichloro-4-[(phenylcarbamoyl)amino]-1,2,3,4-tetrahydroquinoline-2-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Chou, T, Tajima, N, Furukawa, H. | | 登録日 | 2020-04-08 | | 公開日 | 2020-07-15 | | 最終更新日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (4.03 Å) | | 主引用文献 | Structural Basis of Functional Transitions in Mammalian NMDA Receptors.
Cell, 182, 2020
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5O4F
 | | Structure of GluK3 ligand-binding domain (S1S2) in complex with the agonist LM-12b at 2.10 A resolution | | 分子名称: | (3~{a}~{R},4~{S},6~{a}~{R})-1-methyl-4,5,6,6~{a}-tetrahydro-3~{a}~{H}-pyrrolo[3,4-c]pyrazole-3,4-dicarboxylic acid, ACETATE ION, CHLORIDE ION, ... | | 著者 | Moellerud, S, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2017-05-29 | | 公開日 | 2017-07-26 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Structure and Affinity of Two Bicyclic Glutamate Analogues at AMPA and Kainate Receptors.
ACS Chem Neurosci, 8, 2017
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5NS9
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8SS4
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunits TARP gamma-5 and cornichon-2 (apo state) | | 分子名称: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-5 subunit chimera, Protein cornichon homolog 2, ... | | 著者 | Yen, L.Y, Gangwar, S.P, Yelshanskaya, M.V, Sobolevsky, A.I. | | 登録日 | 2023-05-08 | | 公開日 | 2023-09-06 | | 最終更新日 | 2023-11-01 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS8
 | | Structure of AMPA receptor GluA2 complex with auxiliary subunit TARP gamma-5 bound to competitive antagonist ZK and antiepileptic drug perampanel (closed state) | | 分子名称: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, CHOLESTEROL, ... | | 著者 | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | 登録日 | 2023-05-08 | | 公開日 | 2023-09-06 | | 最終更新日 | 2023-10-25 | | 実験手法 | ELECTRON MICROSCOPY (2.81 Å) | | 主引用文献 | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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5O9A
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J-L504Y-N775S) in complex with glutamate and BPAM121 at 1.78 A resolution | | 分子名称: | 1,2-ETHANEDIOL, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ... | | 著者 | Laulumaa, S, Rovinskaja, K, Frydenvang, K.A, Kastrup, J.S. | | 登録日 | 2017-06-16 | | 公開日 | 2018-01-03 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.78 Å) | | 主引用文献 | 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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8SS5
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunit TARP gamma-5 (apo state) | | 分子名称: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-5 subunit chimera, SODIUM ION | | 著者 | Yen, L.Y, Gangwar, S.P, Yelshanskaya, M.V, Sobolevsky, A.I. | | 登録日 | 2023-05-08 | | 公開日 | 2023-09-06 | | 最終更新日 | 2023-10-25 | | 実験手法 | ELECTRON MICROSCOPY (3.56 Å) | | 主引用文献 | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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