5KBV
 
 | | Cryo-EM structure of GluA2 bound to antagonist ZK200775 at 6.8 Angstrom resolution | | Descriptor: | 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 | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.G, Frank, J, Sobolevsky, A.I. | | Deposit date: | 2016-06-03 | | Release date: | 2016-07-13 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (6.8 Å) | | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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5KBT
 | | Cryo-EM structure of GluA2-1xSTZ complex at 6.4 Angstrom resolution | | Descriptor: | 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 | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | | Deposit date: | 2016-06-03 | | Release date: | 2016-07-13 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (6.4 Å) | | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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5KCJ
 | | Structure of the human GluN1/GluN2A LBD in complex with GNE6901 | | Descriptor: | 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, ... | | Authors: | Wallweber, H.J.A, Lupardus, P.J. | | Deposit date: | 2016-06-06 | | Release date: | 2016-07-13 | | Method: | X-RAY DIFFRACTION (2.09 Å) | | Cite: | Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function.
Neuron, 89, 2016
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5IPS
 | | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 4 | | Descriptor: | Ionotropic glutamate receptor subunit NR2B, N-methyl-D-aspartate receptor subunit NR1-8a | | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | | Deposit date: | 2016-03-09 | | Release date: | 2016-04-20 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (13.5 Å) | | Cite: | Mechanism of NMDA Receptor Inhibition and Activation.
Cell, 165, 2016
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5I2N
 | | Structure of the human GluN1/GluN2A LBD in complex with N-ethyl-7-{[2-fluoro-3-(trifluoromethyl)phenyl]methyl}-2-methyl-5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidine-3-carboxamide (compound 29) | | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CALCIUM ION, GLUTAMIC ACID, ... | | Authors: | Wallweber, H.J.A, Lupardus, P.J. | | Deposit date: | 2016-02-09 | | Release date: | 2016-03-16 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.12 Å) | | Cite: | 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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5ICT
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5KK2
 | | Architecture of fully occupied GluA2 AMPA receptor - TARP complex elucidated by single particle cryo-electron microscopy | | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-2 subunit | | Authors: | Zhao, Y, Chen, S, Yoshioka, C, Baconguis, I, Gouaux, E. | | Deposit date: | 2016-06-20 | | Release date: | 2016-07-06 | | Last modified: | 2018-07-18 | | Method: | ELECTRON MICROSCOPY (7.3 Å) | | Cite: | Architecture of fully occupied GluA2 AMPA receptor-TARP complex elucidated by cryo-EM.
Nature, 536, 2016
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5L1H
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor GYKI53655 | | Descriptor: | (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 | | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | Deposit date: | 2016-07-29 | | Release date: | 2016-10-19 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.801 Å) | | Cite: | 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 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Glutamate receptor 2 | | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | Deposit date: | 2016-07-28 | | Release date: | 2016-10-19 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (4 Å) | | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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5JTY
 | | Glutamate- and DCKA-bound GluN1/GluN2A agonist binding domains with MPX-007 | | Descriptor: | 4-hydroxy-5,7-dimethylquinoline-2-carboxylic acid, 5-({[(3,4-difluorophenyl)sulfonyl]amino}methyl)-6-methyl-N-[(2-methyl-1,3-thiazol-5-yl)methyl]pyrazine-2-carboxamide, GLUTAMIC ACID, ... | | Authors: | Mou, T.-C, Sprang, S.R, Hansen, K.B. | | Deposit date: | 2016-05-10 | | Release date: | 2016-09-21 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.72 Å) | | Cite: | Structural Basis for Negative Allosteric Modulation of GluN2A-Containing NMDA Receptors.
Neuron, 91, 2016
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5KUF
 | | GluK2EM with 2S,4R-4-methylglutamate | | Descriptor: | 2S,4R-4-METHYLGLUTAMATE, Glutamate receptor ionotropic, kainate 2 | | Authors: | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | | Deposit date: | 2016-07-13 | | Release date: | 2016-09-07 | | Last modified: | 2019-11-27 | | Method: | ELECTRON MICROSCOPY (3.8 Å) | | Cite: | 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 | | Descriptor: | 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2 | | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | Deposit date: | 2016-07-29 | | Release date: | 2016-10-19 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (4 Å) | | Cite: | Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.
Neuron, 91, 2016
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5L1E
 | | AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor CP465022 | | Descriptor: | 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 | | Authors: | Yelshanskaya, M.V, Singh, A.K, Sampson, J.M, Sobolevsky, A.I. | | Deposit date: | 2016-07-29 | | Release date: | 2016-10-19 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (4.37 Å) | | Cite: | 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 | | Descriptor: | (3S,4aR,6S,8aR)-6-{[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl}decahydroisoquinoline-3-carboxylic acid, Glutamate receptor ionotropic, kainate 2 | | Authors: | Meyerson, J.R, Chittori, S, Merk, A, Rao, P, Han, T.H, Serpe, M, Mayer, M.L, Subramaniam, S. | | Deposit date: | 2016-07-13 | | Release date: | 2016-09-07 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (11.6 Å) | | Cite: | Structural basis of kainate subtype glutamate receptor desensitization.
Nature, 537, 2016
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1MQJ
 | | Crystal structure of the GluR2 ligand binding core (S1S2J) in complex with willardiine at 1.65 angstroms resolution | | Descriptor: | 2-AMINO-3-(2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, ZINC ION, glutamate receptor 2 | | Authors: | Jin, R, Banke, T.G, Mayer, M.L, Traynelis, S.F, Gouaux, E. | | Deposit date: | 2002-09-16 | | Release date: | 2003-08-05 | | Last modified: | 2017-08-02 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Structural basis for partial agonist action at ionotropic glutamate receptors
Nat.Neurosci., 6, 2003
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1M5D
 | | X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J-Y702F) IN COMPLEX WITH Br-HIBO AT 1.73 A RESOLUTION | | Descriptor: | (S)-2-AMINO-3-(4-BROMO-3-HYDROXY-ISOXAZOL-5-YL)PROPIONIC ACID, Glutamate receptor 2, SULFATE ION | | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | | Deposit date: | 2002-07-09 | | Release date: | 2002-09-18 | | Last modified: | 2021-10-27 | | Method: | X-RAY DIFFRACTION (1.73 Å) | | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core
J.Mol.Biol., 322, 2002
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1MQD
 | | X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.46 A resolution. Crystallization in the presence of lithium sulfate. | | Descriptor: | (S)-2-AMINO-3-(3-HYDROXY-ISOXAZOL-4-YL)PROPIONIC ACID, GLYCEROL, Glutamate receptor subunit 2, ... | | Authors: | Kasper, C, Lunn, M.-L, Liljefors, T, Gouaux, E, Egebjerg, J, Kastrup, J.S. | | Deposit date: | 2002-09-16 | | Release date: | 2003-07-01 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.46 Å) | | Cite: | GluR2 ligand-binding core complexes: Importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists.
FEBS Lett., 531, 2002
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1M5F
 | | X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J-Y702F) IN COMPLEX WITH ACPA AT 1.95 A RESOLUTION | | Descriptor: | (S)-2-AMINO-3-(3-CARBOXY-5-METHYLISOXAZOL-4-YL)PROPIONIC ACID, ACETATE ION, Glutamate receptor 2, ... | | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | | Deposit date: | 2002-07-09 | | Release date: | 2002-09-18 | | Last modified: | 2021-10-27 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core
J.Mol.Biol., 322, 2002
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1M5B
 | | X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) IN COMPLEX WITH 2-Me-Tet-AMPA AT 1.85 A RESOLUTION. | | Descriptor: | (S)-2-AMINO-3-[3-HYDROXY-5-(2-METHYL-2H-TETRAZOL-5-YL)ISOXAZOL-4-YL]PROPIONIC ACID, Glutamate receptor 2, ZINC ION | | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | | Deposit date: | 2002-07-09 | | Release date: | 2002-09-18 | | Last modified: | 2017-08-16 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core
J.Mol.Biol., 322, 2002
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1MXU
 | | CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) in complex with bromo-willardiine (Control for the crystal titration experiments) | | Descriptor: | 2-AMINO-3-(5-BROMO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, GLUTAMATE RECEPTOR 2, ZINC ION | | Authors: | Jin, R, Gouaux, E. | | Deposit date: | 2002-10-03 | | Release date: | 2003-06-10 | | Last modified: | 2017-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Probing the Function, Conformational Plasticity, and Dimer-Dimer Contacts of the GluR2 Ligand-Binding Core: Studies of 5-Substituted Willardiines and GluR2 S1S2 in the Crystal
Biochemistry, 42, 2003
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1MXV
 | | crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW) | | Descriptor: | GLUTAMATE RECEPTOR 2, ZINC ION | | Authors: | Jin, R, Gouaux, E. | | Deposit date: | 2002-10-03 | | Release date: | 2003-06-10 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Probing the Function, Conformational Plasticity, and Dimer-Dimer Contacts of the GluR2 Ligand-Binding Core: Studies of 5-Substituted Willardiines and GluR2 S1S2 in the Crystal
Biochemistry, 42, 2003
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1MY2
 | | crystal titration experiment (AMPA complex control) | | Descriptor: | (S)-ALPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID, GLUTAMATE RECEPTOR 2, ZINC ION | | Authors: | Jin, R, Gouaux, E. | | Deposit date: | 2002-10-03 | | Release date: | 2003-06-10 | | Last modified: | 2017-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal.
Biochemistry, 42, 2003
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1MXY
 | | crystal titration experiments (AMPA co-crystals soaked in 10 uM BrW) | | Descriptor: | GLUTAMATE RECEPTOR 2, ZINC ION | | Authors: | Jin, R, Gouaux, E. | | Deposit date: | 2002-10-03 | | Release date: | 2003-06-10 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal.
Biochemistry, 42, 2003
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1N0T
 | | X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with the antagonist (S)-ATPO at 2.1 A resolution. | | Descriptor: | (S)-2-AMINO-3-(5-TERT-BUTYL-3-(PHOSPHONOMETHOXY)-4-ISOXAZOLYL)PROPIONIC ACID, ACETATE ION, Glutamate receptor 2, ... | | Authors: | Hogner, A, Greenwood, J.R, Liljefors, T, Lunn, M.-L, Egebjerg, J, Larsen, I.K, Gouaux, E, Kastrup, J.S. | | Deposit date: | 2002-10-15 | | Release date: | 2003-03-04 | | Last modified: | 2017-08-16 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Competitive antagonism of AMPA receptors by ligands of
different classes: crystal structure of ATPO bound to the
GluR2 ligand-binding core, in comparison with DNQX.
J.Med.Chem., 46, 2003
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