3O28
| Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator | Descriptor: | 2-({[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetyl}amino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, DIMETHYL SULFOXIDE, GLUTAMIC ACID, ... | Authors: | 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. | Deposit date: | 2010-07-22 | Release date: | 2010-09-15 | Last modified: | 2017-08-09 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | 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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3OEL
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3OEK
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3OEN
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3M3F
| PEPA bound to the ligand binding domain of GluA3 (flop form) | Descriptor: | 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide, GLUTAMIC ACID, Glutamate receptor 3, ... | Authors: | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | Deposit date: | 2010-03-09 | Release date: | 2010-03-23 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | 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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5TPA
| Structure of the human GluN1/GluN2A LBD in complex with compound 9 (GNE3500) | Descriptor: | (1R,2R)-2-(2-{[5-chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl}-7-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-6-yl)cyclopropane-1-carbonitrile, GLUTAMIC ACID, GLYCINE, ... | Authors: | Wallweber, H.J.A, Lupardus, P.J. | Deposit date: | 2016-10-20 | Release date: | 2016-11-30 | Last modified: | 2017-02-01 | Method: | X-RAY DIFFRACTION (2.48 Å) | Cite: | GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile. ACS Med Chem Lett, 8, 2017
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5UN1
| Crystal structure of GluN1/GluN2B delta-ATD NMDA receptor | Descriptor: | (5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | Authors: | Song, X, Gouaux, E. | Deposit date: | 2017-01-30 | Release date: | 2018-02-07 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (3.6 Å) | Cite: | Mechanism of NMDA receptor channel block by MK-801 and memantine. Nature, 556, 2018
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5VHW
| GluA2-0xGSG1L bound to ZK | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Germ cell-specific gene 1-like protein, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-04-13 | Release date: | 2017-05-03 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (7.8 Å) | Cite: | Structural Bases of Desensitization in AMPA Receptor-Auxiliary Subunit Complexes. Neuron, 94, 2017
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5VHZ
| GluA2-2xGSG1L bound to L-Quisqualate | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, Glutamate receptor 2,Germ cell-specific gene 1-like protein | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-04-13 | Release date: | 2017-05-03 | Last modified: | 2017-11-08 | Method: | ELECTRON MICROSCOPY (8.4 Å) | Cite: | Structural Bases of Desensitization in AMPA Receptor-Auxiliary Subunit Complexes. Neuron, 94, 2017
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5TP9
| Structure of the human GluN1/GluN2A LBD in complex with compound 2 (GNE9178) | Descriptor: | 7-{[5-chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl}-N-ethyl-2-methyl-5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidine-3-carboxamide, ACETATE ION, CALCIUM ION, ... | Authors: | Wallweber, H.J.A, Lupardus, P.J. | Deposit date: | 2016-10-20 | Release date: | 2016-11-30 | Last modified: | 2017-02-08 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile. ACS Med Chem Lett, 8, 2017
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5VHY
| GluA2-2xGSG1L bound to ZK | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Germ cell-specific gene 1-like protein, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-04-13 | Release date: | 2017-05-03 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (4.6 Å) | Cite: | Structural Bases of Desensitization in AMPA Receptor-Auxiliary Subunit Complexes. Neuron, 94, 2017
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5VOU
| Structure of AMPA receptor-TARP complex | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | Authors: | Chen, S, Zhao, Y, Wang, Y.S, Shekhar, M, Tajkhorshid, E, Gouaux, E. | Deposit date: | 2017-05-03 | Release date: | 2017-07-12 | Last modified: | 2019-12-18 | Method: | ELECTRON MICROSCOPY (6.4 Å) | Cite: | Activation and Desensitization Mechanism of AMPA Receptor-TARP Complex by Cryo-EM. Cell, 170, 2017
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5VOV
| Structure of AMPA receptor-TARP complex | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | Authors: | Zhao, Y, Chen, S, Wang, Y.S, Shekhar, M, Tajkhorshid, E, Gouaux, E. | Deposit date: | 2017-05-03 | Release date: | 2017-07-12 | Last modified: | 2019-12-18 | Method: | ELECTRON MICROSCOPY (7.7 Å) | Cite: | Activation and Desensitization Mechanism of AMPA Receptor-TARP Complex by Cryo-EM. Cell, 170, 2017
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5UOW
| Triheteromeric NMDA receptor GluN1/GluN2A/GluN2B in complex with glycine, glutamate, MK-801 and a GluN2B-specific Fab, at pH 6.5 | Descriptor: | (5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, GLUTAMIC ACID, ... | Authors: | Lu, W, Du, J, Goehring, A, Gouaux, E. | Deposit date: | 2017-02-01 | Release date: | 2017-03-22 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (4.5 Å) | Cite: | Cryo-EM structures of the triheteromeric NMDA receptor and its allosteric modulation. Science, 355, 2017
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5U8C
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5VIH
| Crystal structure of GluN1/GluN2A NMDA receptor agonist binding domains with glycine and antagonist, 4-fluorophenyl-ACEPC | Descriptor: | 5-[(2R)-2-amino-2-carboxyethyl]-1-(4-fluorophenyl)-1H-pyrazole-3-carboxylic acid, DI(HYDROXYETHYL)ETHER, GLYCINE, ... | Authors: | Mou, T.-C, Conti, P, Pinto, A, Tamborini, L, Sprang, S.R, Hansen, K.B. | Deposit date: | 2017-04-16 | Release date: | 2017-04-26 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structural basis of subunit selectivity for competitive NMDA receptor antagonists with preference for GluN2A over GluN2B subunits. Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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5VIJ
| Crystal structure of GluN1/GluN2A NMDA receptor agonist binding domains with glycine and antagonist, 4-bromophenyl-ACEPC | Descriptor: | 5-[(2R)-2-amino-2-carboxyethyl]-1-(4-bromophenyl)-1H-pyrazole-3-carboxylic acid, GLYCINE, Glutamate receptor ionotropic, ... | Authors: | Mou, T.-C, Conti, P, Pinto, A, Tamborini, L, Sprang, S.R, Hansen, K.B. | Deposit date: | 2017-04-16 | Release date: | 2017-04-26 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.105 Å) | Cite: | Structural basis of subunit selectivity for competitive NMDA receptor antagonists with preference for GluN2A over GluN2B subunits. Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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5VHX
| GluA2-1xGSG1L bound to ZK | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Germ cell-specific gene 1-like protein, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-04-13 | Release date: | 2017-05-03 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (8.3 Å) | Cite: | Structural Bases of Desensitization in AMPA Receptor-Auxiliary Subunit Complexes. Neuron, 94, 2017
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5VII
| Crystal structure of GluN1/GluN2A NMDA receptor agonist binding domains with glycine and antagonist, 4-(3-fluoropropyl)phenyl-ACEPC | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 5-[(2R)-2-amino-2-carboxyethyl]-1-[4-(3-fluoropropyl)phenyl]-1H-pyrazole-3-carboxylic acid, DI(HYDROXYETHYL)ETHER, ... | Authors: | Mou, T.-C, Conti, P, Pinto, A, Tamborini, L, Sprang, S.R, Hansen, K.B. | Deposit date: | 2017-04-16 | Release date: | 2017-04-26 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.951 Å) | Cite: | Structural basis of subunit selectivity for competitive NMDA receptor antagonists with preference for GluN2A over GluN2B subunits. Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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5UP2
| Triheteromeric NMDA receptor GluN1/GluN2A/GluN2B in complex with glycine, glutamate, Ro 25-6981, MK-801 and a GluN2B-specific Fab, at pH 6.5 | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, GluN2B-specific Fab, ... | Authors: | Lu, W, Du, J, Goehring, A, Gouaux, E. | Deposit date: | 2017-02-01 | Release date: | 2017-03-22 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (6 Å) | Cite: | Cryo-EM structures of the triheteromeric NMDA receptor and its allosteric modulation. Science, 355, 2017
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5WEK
| GluA2 bound to antagonist ZK and GSG1L in digitonin, state 1 | Descriptor: | Chimera of Glutamate receptor 2,Germ cell-specific gene 1-like protein, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2019-11-20 | Method: | ELECTRON MICROSCOPY (4.6 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
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5WEM
| GluA2 bound to GSG1L in digitonin, state 1 | Descriptor: | Chimera of Glutamate receptor 2,Germ cell-specific gene 1-like protein | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2019-11-20 | Method: | ELECTRON MICROSCOPY (6.1 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
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5VOT
| Structure of AMPA receptor-TARP complex | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | Authors: | Chen, S, Zhao, Y, Wang, Y.S, Shekhar, M, Tajkhorshid, E, Gouaux, E. | Deposit date: | 2017-05-03 | Release date: | 2017-07-12 | Last modified: | 2019-12-18 | Method: | ELECTRON MICROSCOPY (4.9 Å) | Cite: | Activation and Desensitization Mechanism of AMPA Receptor-TARP Complex by Cryo-EM. Cell, 170, 2017
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5WEO
| Activated GluA2 complex bound to glutamate, cyclothiazide, and STZ in digitonin | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit chimera | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2019-11-20 | Method: | ELECTRON MICROSCOPY (4.2 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
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5WEL
| GluA2 bound to antagonist ZK and GSG1L in digitonin, state 2 | Descriptor: | Chimera of Glutamate receptor 2, Germ cell-specific gene 1-like protein, Digitonin, ... | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (4.4 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
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