5KBS
 
 | | Cryo-EM structure of GluA2-0xSTZ at 8.7 Angstrom resolution | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | | 著者 | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | | 登録日 | 2016-06-03 | | 公開日 | 2016-07-13 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (8.7 Å) | | 主引用文献 | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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5KDT
 | | Structure of the human GluN1/GluN2A LBD in complex with GNE0723 | | 分子名称: | (1~{R},2~{R})-2-[7-[[5-chloranyl-3-(trifluoromethyl)pyrazol-1-yl]methyl]-5-oxidanylidene-2-(trifluoromethyl)-[1,3]thiazolo[3,2-a]pyrimidin-3-yl]cyclopropane-1-carbonitrile, ACETATE ION, GLUTAMIC ACID, ... | | 著者 | Wallweber, H.J.A, Lupardus, P.J. | | 登録日 | 2016-06-08 | | 公開日 | 2016-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.44 Å) | | 主引用文献 | Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
J. Med. Chem., 59, 2016
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5KBV
 | | Cryo-EM structure of GluA2 bound to antagonist ZK200775 at 6.8 Angstrom resolution | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | | 著者 | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.G, Frank, J, Sobolevsky, A.I. | | 登録日 | 2016-06-03 | | 公開日 | 2016-07-13 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (6.8 Å) | | 主引用文献 | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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3LSX
 | | Piracetam bound to the ligand binding domain of GluA3 | | 分子名称: | 2-(2-oxopyrrolidin-1-yl)acetamide, GLUTAMIC ACID, GluA3 S1S2 domain, ... | | 著者 | Ahmed, A.H, Oswald, R.E. | | 登録日 | 2010-02-13 | | 公開日 | 2011-03-16 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.006 Å) | | 主引用文献 | Piracetam Defines a New Binding Site for Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic Acid (AMPA) Receptors.
J.Med.Chem., 53, 2010
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3LSF
 | | Piracetam bound to the ligand binding domain of GluA2 | | 分子名称: | 2-(2-oxopyrrolidin-1-yl)acetamide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2010-02-12 | | 公開日 | 2010-03-16 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.851 Å) | | 主引用文献 | Piracetam Defines a New Binding Site for Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic Acid (AMPA) Receptors.
J.Med.Chem., 53, 2010
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3LSL
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5KBT
 | | Cryo-EM structure of GluA2-1xSTZ complex at 6.4 Angstrom resolution | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | | 著者 | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | | 登録日 | 2016-06-03 | | 公開日 | 2016-07-13 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (6.4 Å) | | 主引用文献 | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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3M3K
 | | Ligand binding domain (S1S2) of GluA3 (flop) | | 分子名称: | GLUTAMIC ACID, Glutamate receptor 3, ZINC ION | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2010-03-09 | | 公開日 | 2010-03-23 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.793 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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5KCJ
 | | Structure of the human GluN1/GluN2A LBD in complex with GNE6901 | | 分子名称: | 7-[(4-fluoranylphenoxy)methyl]-3-[(1~{R},2~{R})-2-(hydroxymethyl)cyclopropyl]-2-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one, ACETATE ION, GLUTAMIC ACID, ... | | 著者 | Wallweber, H.J.A, Lupardus, P.J. | | 登録日 | 2016-06-06 | | 公開日 | 2016-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.09 Å) | | 主引用文献 | Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function.
Neuron, 89, 2016
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5KK2
 | | Architecture of fully occupied GluA2 AMPA receptor - TARP complex elucidated by single particle cryo-electron microscopy | | 分子名称: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | | 著者 | Zhao, Y, Chen, S, Yoshioka, C, Baconguis, I, Gouaux, E. | | 登録日 | 2016-06-20 | | 公開日 | 2016-07-06 | | 最終更新日 | 2018-07-18 | | 実験手法 | ELECTRON MICROSCOPY (7.3 Å) | | 主引用文献 | Architecture of fully occupied GluA2 AMPA receptor-TARP complex elucidated by cryo-EM.
Nature, 536, 2016
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3O2A
 | | Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | | 分子名称: | GLUTAMIC ACID, GLYCEROL, Glutamate receptor 2, ... | | 著者 | Maclean, J.K.F, Basten, S, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Papakosta, M, Rankovic, Z, Smith, L. | | 登録日 | 2010-07-22 | | 公開日 | 2010-09-15 | | 最終更新日 | 2017-08-09 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.
Bioorg.Med.Chem.Lett., 20, 2010
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3OEM
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5L1H
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor GYKI53655 | | 分子名称: | (8R)-5-(4-aminophenyl)-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 | | 著者 | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | 登録日 | 2016-07-29 | | 公開日 | 2016-10-19 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.801 Å) | | 主引用文献 | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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5L2E
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5L1B
 | | AMPA subtype ionotropic glutamate receptor GluA2 in Apo state | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Glutamate receptor 2 | | 著者 | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | 登録日 | 2016-07-28 | | 公開日 | 2016-10-19 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (4 Å) | | 主引用文献 | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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3O6I
 | | Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | | 分子名称: | 2-[({3-tert-butyl-4-[(methylamino)methyl]-1H-pyrazol-1-yl}acetyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Maclean, J.K.F, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Martin, F, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L. | | 登録日 | 2010-07-29 | | 公開日 | 2010-09-15 | | 最終更新日 | 2017-08-09 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Bioorg.Med.Chem.Lett., 20, 2010
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5L1E
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor CP465022 | | 分子名称: | 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 | | 著者 | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | 登録日 | 2016-07-29 | | 公開日 | 2016-10-19 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (4.37 Å) | | 主引用文献 | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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5KUF
 | | GluK2EM with 2S,4R-4-methylglutamate | | 分子名称: | 2S,4R-4-METHYLGLUTAMATE, Glutamate receptor ionotropic, kainate 2 | | 著者 | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | | 登録日 | 2016-07-13 | | 公開日 | 2016-09-07 | | 最終更新日 | 2019-11-27 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Structural basis of kainate subtype glutamate receptor desensitization.
Nature, 537, 2016
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5L1F
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor Perampanel | | 分子名称: | 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2 | | 著者 | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | 登録日 | 2016-07-29 | | 公開日 | 2016-10-19 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (4 Å) | | 主引用文献 | 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 | | 分子名称: | (3S,4aR,6S,8aR)-6-{[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl}decahydroisoquinoline-3-carboxylic acid, Glutamate receptor ionotropic, kainate 2 | | 著者 | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | | 登録日 | 2016-07-13 | | 公開日 | 2016-09-07 | | 最終更新日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (11.6 Å) | | 主引用文献 | Structural basis of kainate subtype glutamate receptor desensitization.
Nature, 537, 2016
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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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5L1G
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with GYKI-Br | | 分子名称: | (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 | | 著者 | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | 登録日 | 2016-07-29 | | 公開日 | 2016-10-19 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (4.507 Å) | | 主引用文献 | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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3O6H
 | | Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | | 分子名称: | 1,2-ETHANEDIOL, 2-[({4-[(ethylamino)methyl]-3-(trifluoromethyl)-1H-pyrazol-1-yl}acetyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, DIMETHYL SULFOXIDE, ... | | 著者 | Maclean, J.K.F, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Martin, F, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L. | | 登録日 | 2010-07-29 | | 公開日 | 2010-09-15 | | 最終更新日 | 2017-08-09 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Bioorg.Med.Chem.Lett., 20, 2010
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3O6G
 | | Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | | 分子名称: | 1,2-ETHANEDIOL, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Maclean, J.K.F, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Martin, F, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L. | | 登録日 | 2010-07-29 | | 公開日 | 2010-09-15 | | 最終更新日 | 2017-08-09 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Bioorg.Med.Chem.Lett., 20, 2010
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3O29
 | | Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | | 分子名称: | GLUTAMIC ACID, GLYCEROL, Glutamate receptor 2, ... | | 著者 | Maclean, J.K.F, Basten, S, Campbell, R.A, Cumming, I.A, Gillen, K.J, Gillespie, J, Jamieson, C, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Papakosta, M, Rankovic, Z, Smith, L. | | 登録日 | 2010-07-22 | | 公開日 | 2010-09-15 | | 最終更新日 | 2017-08-09 | | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | | 主引用文献 | A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.
Bioorg.Med.Chem.Lett., 20, 2010
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