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3H06
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Crystal structure of the binding domain of the AMPA subunit GluR2 bound to the willardiine antagonist, UBP282
Descriptor: 4-({3-[(2R)-2-amino-2-carboxyethyl]-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl}methyl)benzoic acid, Glutamate receptor 2
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2009-04-08
Release date:2009-05-05
Last modified:2017-08-23
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Mechanisms of antagonism of the GluR2 AMPA receptor: structure and dynamics of the complex of two willardiine antagonists with the glutamate binding domain.
Biochemistry, 48, 2009
3H03
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BU of 3h03 by Molmil
Crystal structure of the binding domain of the AMPA subunit GluR2 bound to UBP277
Descriptor: 3-[3-(2-carboxyethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]-L-alanine, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2009-04-08
Release date:2009-05-05
Last modified:2023-09-06
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Mechanisms of antagonism of the GluR2 AMPA receptor: structure and dynamics of the complex of two willardiine antagonists with the glutamate binding domain.
Biochemistry, 48, 2009
3H6W
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BU of 3h6w by Molmil
Crystal structure of the iGluR2 ligand-binding core (S1S2J-N754S) in complex with glutamate and NS5217 at 1.50 A resolution
Descriptor: (3R)-3-cyclopentyl-6-methyl-7-[(4-methylpiperazin-1-yl)sulfonyl]-3,4-dihydro-2H-1,2-benzothiazine 1,1-dioxide, DIMETHYL SULFOXIDE, GLUTAMIC ACID, ...
Authors:Hald, H, Gajhede, M, Kastrup, J.S.
Deposit date:2009-04-24
Release date:2009-07-28
Last modified:2023-09-06
Method:X-RAY DIFFRACTION (1.49 Å)
Cite:Distinct structural features of cyclothiazide are responsible for effects on peak current amplitude and desensitization kinetics at iGluR2.
J.Mol.Biol., 391, 2009
3QXM
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BU of 3qxm by Molmil
Crystal Structure of Human GluK2 Ligand-Binding Core in Complex with Novel Marine-Derived Toxins, Neodysiherbaine A
Descriptor: (2R,3aR,6R,7R,7aR)-2-[(2S)-2-amino-2-carboxyethyl]-6,7-dihydroxyhexahydro-2H-furo[3,2-b]pyran-2-carboxylic acid, Glutamate receptor ionotropic, kainate 2
Authors:Unno, M, Sasaki, M, Ikeda-Saito, M.
Deposit date:2011-03-02
Release date:2011-10-26
Last modified:2023-11-01
Method:X-RAY DIFFRACTION (1.65 Å)
Cite:Binding and Selectivity of the Marine Toxin Neodysiherbaine A and Its Synthetic Analogues to GluK1 and GluK2 Kainate Receptors.
J.Mol.Biol., 413, 2011
3PMV
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BU of 3pmv by Molmil
Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator
Descriptor: GLUTAMIC ACID, GLYCEROL, Glutamate receptor 2, ...
Authors:Maclean, J.K.F, Jamieson, C, Brown, C.I, Campbell, R.A, Gillen, K.J, Gillespie, J, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L.
Deposit date:2010-11-18
Release date:2011-01-12
Last modified:2023-09-20
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:Structure based evolution of a novel series of positive modulators of the AMPA receptor.
Bioorg.Med.Chem.Lett., 21, 2011
3RTW
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BU of 3rtw by Molmil
Nitrowillardiine bound to the ligand binding domain of GluA2
Descriptor: 3-(5-nitro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-L-alanine, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-05-04
Release date:2011-05-18
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.095 Å)
Cite:Mechanisms of Modal Activation of GluA3 Receptors.
Mol.Pharmacol., 80, 2011
3S9E
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BU of 3s9e by Molmil
Crystal structure of the kainate receptor GluK3 ligand binding domain in complex with (S)-glutamate
Descriptor: CHLORIDE ION, GLUTAMIC ACID, GLYCEROL, ...
Authors:Venskutonyte, R, Frydenvang, K, Gajhede, M, Kastrup, J.S.
Deposit date:2011-06-01
Release date:2011-09-28
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.6 Å)
Cite:Binding site and interlobe interactions of the ionotropic glutamate receptor GluK3 ligand binding domain revealed by high resolution crystal structure in complex with (S)-glutamate.
J.Struct.Biol., 176, 2011
3RT6
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BU of 3rt6 by Molmil
Fluorowillardiine bound to the ligand binding domain of GluA3
Descriptor: 2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, Glutamate receptor 3, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-05-03
Release date:2011-05-18
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.836 Å)
Cite:Mechanisms of Modal Activation of GluA3 Receptors.
Mol.Pharmacol., 80, 2011
3RT8
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BU of 3rt8 by Molmil
Chlorowillardiine bound to the ligand binding domain of GluA3
Descriptor: 3-(5-chloro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-L-alanine, Glutamate receptor 3, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-05-03
Release date:2011-05-18
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.426 Å)
Cite:Mechanisms of Modal Activation of GluA3 Receptors.
Mol.Pharmacol., 80, 2011
3R7X
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BU of 3r7x by Molmil
Crystal Structure Analysis of a Quinazolinedione sulfonamide bound to human GluR2: A Novel Class of Competitive AMPA Receptor Antagonists with Oral Activity
Descriptor: GLUTAMIC ACID, Glutamate receptor 2, N-[6-(1H-imidazol-1-yl)-7-nitro-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]methanesulfonamide
Authors:Kallen, J.
Deposit date:2011-03-23
Release date:2011-05-18
Last modified:2017-07-26
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity.
Bioorg.Med.Chem.Lett., 21, 2011
3RNN
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BU of 3rnn by Molmil
Crystal Structure of iGluR2 Ligand Binding Domain with Symmetric Sulfonamide Containing Potentiator
Descriptor: GLUTAMIC ACID, Glutamate receptor 2, N,N'-(benzene-1,4-diyldiethane-2,1-diyl)dipropane-2-sulfonamide, ...
Authors:Timm, D.E.
Deposit date:2011-04-22
Release date:2011-05-25
Last modified:2019-07-17
Method:X-RAY DIFFRACTION (1.75 Å)
Cite:Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.
Mol.Pharmacol., 80, 2011
3RTF
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BU of 3rtf by Molmil
Chlorowillardiine bound to the ligand binding domain of GluA2
Descriptor: 3-(5-chloro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-L-alanine, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-05-03
Release date:2011-05-18
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.7 Å)
Cite:Mechanisms of Modal Activation of GluA3 Receptors.
Mol.Pharmacol., 80, 2011
3S2V
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BU of 3s2v by Molmil
Crystal Structure of the Ligand Binding Domain of GluK1 in Complex with an Antagonist (S)-1-(2'-Amino-2'-carboxyethyl)-3-[(2-carboxythien-3-yl)methyl]thieno[3,4-d]pyrimidin-2,4-dione at 2.5 A Resolution
Descriptor: (S)-1-(2'-AMINO-2'-CARBOXYETHYL)-3-[(2-CARBOXYTHIEN-3-YL)METHYL]THIENO[3,4-D]PYRIMIDIN-2,4-DIONE, CHLORIDE ION, GLYCEROL, ...
Authors:Venskutonyte, R, Frydenvang, K, Kastrup, J.S.
Deposit date:2011-05-17
Release date:2011-06-22
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
J.Med.Chem., 54, 2011
3T96
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BU of 3t96 by Molmil
Iodowillardiine bound to a double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2
Descriptor: 2-AMINO-3-(5-IODO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Wang, S, Chuang, H.H, Oswald, R.E.
Deposit date:2011-08-02
Release date:2011-08-17
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.872 Å)
Cite:Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
3T9H
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BU of 3t9h by Molmil
Kainate bound to a double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Wang, S, Chuang, H.H, Oswald, R.E.
Deposit date:2011-08-02
Release date:2011-08-17
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.015 Å)
Cite:Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
3PMW
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BU of 3pmw by Molmil
Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator
Descriptor: DIMETHYL SULFOXIDE, GLUTAMIC ACID, GLYCEROL, ...
Authors:Maclean, J.K.F, Jamieson, C, Brown, C.I, Campbell, R.A, Gillen, K.J, Gillespie, J, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L.
Deposit date:2010-11-18
Release date:2011-01-12
Last modified:2023-05-31
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Structure based evolution of a novel series of positive modulators of the AMPA receptor.
Bioorg.Med.Chem.Lett., 21, 2011
3T93
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BU of 3t93 by Molmil
Glutamate bound to a double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2
Descriptor: GLUTAMIC ACID, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-08-02
Release date:2011-08-17
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.907 Å)
Cite:Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
3TDJ
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BU of 3tdj by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and BPAM-97 at 1.95 A resolution
Descriptor: 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, GLUTAMIC ACID, ...
Authors:Krintel, C, Frydenvang, K, Gajhede, M, Kastrup, J.S.
Deposit date:2011-08-11
Release date:2011-09-21
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.95 Å)
Cite:Thermodynamics and structural analysis of positive allosteric modulation of the ionotropic glutamate receptor GluA2.
Biochem.J., 441, 2012
3T9U
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BU of 3t9u by Molmil
CNQX bound to an oxidized double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2
Descriptor: 7-nitro-2,3-dioxo-2,3-dihydroquinoxaline-6-carbonitrile, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-08-03
Release date:2011-08-17
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.97 Å)
Cite:Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
3RN8
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BU of 3rn8 by Molmil
Crystal Structure of iGluR2 Ligand Binding Domain and Symmetrical Carboxyl Containing Potentiator
Descriptor: 3,3'-benzene-1,4-diylbis(4-cyano-5-ethylthiophene-2-carboxylic acid), ACETATE ION, GLUTAMIC ACID, ...
Authors:Timm, D.E.
Deposit date:2011-04-22
Release date:2011-05-25
Last modified:2017-08-23
Method:X-RAY DIFFRACTION (1.7 Å)
Cite:Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.
Mol.Pharmacol., 80, 2011
3UA8
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BU of 3ua8 by Molmil
Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2
Descriptor: Glutamate receptor 2, N-methyl-1-{3-[(methylsulfonyl)amino]-2,4-dioxo-7-(trifluoromethyl)-1,2,3,4-tetrahydroquinazolin-6-yl}-1H-imidazole-4-carboxamide
Authors:Kallen, J.
Deposit date:2011-10-21
Release date:2012-01-11
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.
Bioorg.Med.Chem.Lett., 22, 2012
3T9V
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BU of 3t9v by Molmil
CNQX bound to a reduced double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2
Descriptor: 7-nitro-2,3-dioxo-2,3-dihydroquinoxaline-6-carbonitrile, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-08-03
Release date:2011-08-17
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.975 Å)
Cite:Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
3T9X
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Glutamate bound to a double cysteine mutant (V484C/E657C) of the ligand binding domain of GluA2
Descriptor: GLUTAMIC ACID, Glutamate receptor 2, ZINC ION
Authors:Ahmed, A.H, Oswald, R.E.
Deposit date:2011-08-03
Release date:2011-08-17
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.823 Å)
Cite:Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
3PMX
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BU of 3pmx by Molmil
Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator
Descriptor: 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, GLUTAMIC ACID, ...
Authors:Maclean, J.K.F, Jamieson, C, Brown, C.I, Campbell, R.A, Gillen, K.J, Gillespie, J, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, A.J, Moir, E.M, Morrow, J.A, Pantling, J, Rankovic, Z, Smith, L.
Deposit date:2010-11-18
Release date:2011-01-12
Last modified:2017-08-09
Method:X-RAY DIFFRACTION (1.87 Å)
Cite:Structure based evolution of a novel series of positive modulators of the AMPA receptor.
Bioorg.Med.Chem.Lett., 21, 2011
3TKD
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BU of 3tkd by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and cyclothiazide at 1.45 A resolution
Descriptor: CYCLOTHIAZIDE, GLUTAMATE RECEPTOR 2, GLUTAMIC ACID, ...
Authors:Krintel, C, Frydenvang, K, Gajhede, M, Kastrup, J.S.
Deposit date:2011-08-26
Release date:2011-09-21
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (1.45 Å)
Cite:Thermodynamics and structural analysis of positive allosteric modulation of the ionotropic glutamate receptor GluA2.
Biochem.J., 441, 2012

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