2CMO
 
 | | The structure of a mixed glur2 ligand-binding core dimer in complex with (s)-glutamate and the antagonist (s)-ns1209 | | Descriptor: | 2-({[(3E)-5-{4-[(DIMETHYLAMINO)(DIHYDROXY)-LAMBDA~4~-SULFANYL]PHENYL}-8-METHYL-2-OXO-6,7,8,9-TETRAHYDRO-1H-PYRROLO[3,2-H]ISOQUINOLIN-3(2H)-YLIDENE]AMINO}OXY)-4-HYDROXYBUTANOIC ACID, GLUTAMATE RECEPTOR 2, GLUTAMIC ACID, ... | | Authors: | Kasper, C, Pickering, D.S, Mirza, O, Olsen, L, Kristensen, A.S, Greenwood, J.R, Liljefors, T, Schousboe, A, Watjen, F, Gajhede, M, Sigurskjold, B.W, Kastrup, J.S. | | Deposit date: | 2006-05-11 | | Release date: | 2006-06-06 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | The Structure of a Mixed Glur2 Ligand-Binding Core Dimer in Complex with (S)-Glutamate and the Antagonist (S)-Ns1209.
J.Mol.Biol., 357, 2006
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1WVJ
 | | Exploring the GluR2 ligand-binding core in complex with the bicyclic AMPA analogue (S)-4-AHCP | | Descriptor: | 3-(3-HYDROXY-7,8-DIHYDRO-6H-CYCLOHEPTA[D]ISOXAZOL-4-YL)-L-ALANINE, GLYCEROL, SULFATE ION, ... | | Authors: | Nielsen, B.B, Pickering, D.S, Greenwood, J.R, Brehm, L, Gajhede, M, Schousboe, A, Kastrup, J.S. | | Deposit date: | 2004-12-15 | | Release date: | 2005-04-26 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Exploring the GluR2 ligand-binding core in complex with the bicyclical AMPA analogue (S)-4-AHCP
FEBS J., 272, 2005
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1XHY
 | | X-ray structure of the Y702F mutant of the GluR2 ligand-binding core (S1S2J) in complex with kainate at 1.85 A resolution | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, Glutamate receptor, SULFATE ION | | Authors: | Frandsen, A, Pickering, D.S, Vestergaard, B, Kasper, C, Nielsen, B.B, Greenwood, J.R, Campiani, G, Gajhede, M, Schousboe, A, Kastrup, J.S. | | Deposit date: | 2004-09-21 | | Release date: | 2005-03-22 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Tyr702 Is an Important Determinant of Agonist Binding and Domain Closure of the Ligand-Binding Core of GluR2.
Mol.Pharmacol., 67, 2005
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1SYH
 | | X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE (S1S2J) IN COMPLEX WITH (S)-CPW399 AT 1.85 A RESOLUTION. | | Descriptor: | (S)-2-AMINO-3-(1,3,5,7-PENTAHYDRO-2,4-DIOXO-CYCLOPENTA[E]PYRIMIDIN-1-YL) PROIONIC ACID, Glutamate receptor 2 | | Authors: | Frandsen, A, Pickering, D.S, Vestergaard, B, Kasper, C, Nielsen, B.B, Greenwood, J.R, Campiani, G, Gajhede, M, Schousboe, A, Kastrup, J.S. | | Deposit date: | 2004-04-01 | | Release date: | 2005-03-22 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Tyr702 Is an Important Determinant of Agonist Binding and Domain Closure of the Ligand-Binding Core of GluR2.
Mol.Pharmacol., 67, 2005
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1SYI
 | | X-RAY STRUCTURE OF THE Y702F MUTANT OF THE GLUR2 LIGAND-BINDING CORE (S1S2J) IN COMPLEX WITH (S)-CPW399 AT 2.1 A RESOLUTION. | | Descriptor: | (S)-2-AMINO-3-(1,3,5,7-PENTAHYDRO-2,4-DIOXO-CYCLOPENTA[E]PYRIMIDIN-1-YL) PROIONIC ACID, Glutamate receptor 2 | | Authors: | Frandsen, A, Pickering, D.S, Vestergaard, B, Kasper, C, Nielsen, B.B, Greenwood, J.R, Campiani, G, Gajhede, M, Schousboe, A, Kastrup, J.S. | | Deposit date: | 2004-04-01 | | Release date: | 2005-03-22 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Tyr702 Is an Important Determinant of Agonist Binding and Domain Closure of the Ligand-Binding Core of GluR2.
Mol.Pharmacol., 67, 2005
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4YMA
 | | Structure of the ligand-binding domain of GluA2 in complex with the antagonist CNG10109 | | Descriptor: | (3R)-3-(3-carboxy-5-hydroxyphenyl)-L-proline, 1,2-ETHANEDIOL, ACETATE ION, ... | | Authors: | Moller, C, Tapken, D, Kastrup, J.S, Frydenvang, K. | | Deposit date: | 2015-03-06 | | Release date: | 2015-08-05 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.895 Å) | | Cite: | Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.
J.Med.Chem., 58, 2015
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4NWD
 | | Crystal structure of the kainate receptor GluK3 ligand-binding domain in complex with the agonist (2S,4R)-4-(3-Methylamino-3-oxopropyl)glutamic acid at 2.6 A resolution | | Descriptor: | (4R)-4-[3-(methylamino)-3-oxopropyl]-L-glutamic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Venskutonyte, R, Larsen, A.P, Frydenvang, K, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2013-12-06 | | Release date: | 2014-08-06 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Molecular Recognition of Two 2,4-syn-Functionalized (S)-Glutamate Analogues by the Kainate Receptor GluK3 Ligand Binding Domain.
Chemmedchem, 9, 2014
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4NWC
 | | Crystal structure of the GluK3 ligand-binding domain (S1S2) in complex with the agonist (2S,4R)-4-(3-Methoxy-3-oxopropyl)glutamic acid at 2.01 A resolution. | | Descriptor: | (2S,4R)-4-(3-Methoxy-3-oxopropyl) glutamic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Larsen, A.P, Venskutonyte, R, Frydenvang, K, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2013-12-06 | | Release date: | 2014-08-06 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.012 Å) | | Cite: | Molecular Recognition of Two 2,4-syn-Functionalized (S)-Glutamate Analogues by the Kainate Receptor GluK3 Ligand Binding Domain.
Chemmedchem, 9, 2014
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1VSO
 | | Crystal Structure of the Ligand-Binding Core of iGluR5 in Complex With the Antagonist (S)-ATPO at 1.85 A resolution | | Descriptor: | (S)-2-AMINO-3-(5-TERT-BUTYL-3-(PHOSPHONOMETHOXY)-4-ISOXAZOLYL)PROPIONIC ACID, GLYCEROL, Glutamate receptor, ... | | Authors: | Hald, H, Naur, P, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2007-03-29 | | Release date: | 2007-07-03 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Partial agonism and antagonism of the ionotropic glutamate receptor iGLuR5: structures of the ligand-binding core in complex with domoic acid and 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid.
J.Biol.Chem., 282, 2007
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5FHO
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with (S)-2-Amino-3-(5-(2-(3-chlorobenzyl)-2H-tetrazol-5-yl)-3-hydroxyisoxazol-4-yl)propanoic acid at 2.3 A resolution | | Descriptor: | (1S)-1-carboxy-2-(5-{2-[(3-chlorophenyl)methyl]-2H-tetrazol-5-yl}-3-oxo-2,3-dihydro-1,2-oxazol-4-yl)ethan-1-aminium, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2015-12-22 | | Release date: | 2016-03-02 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.
J.Med.Chem., 59, 2016
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5FHM
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with (S)-2-Amino-3-(5-(2-(3-(aminomethyl)benzyl)-2H-tetrazol-5-yl)-3-hydroxyisoxazol-4-yl)propanoic acid at resolution 1.55 A resolution | | Descriptor: | (2~{S})-3-[5-[2-[[3-(aminomethyl)phenyl]methyl]-1,2,3,4-tetrazol-5-yl]-3-oxidanyl-1,2-oxazol-4-yl]-2-azanyl-propanoic acid, 1,2-ETHANEDIOL, ACETATE ION, ... | | Authors: | Kastrup, J.S, Frydenvang, K, Al-musaed, A. | | Deposit date: | 2015-12-22 | | Release date: | 2016-03-02 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.
J.Med.Chem., 59, 2016
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5FHN
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6Q54
 | | Structure of GluA2 ligand-binding domain (S1S2J) in complex with the agonist (S)-2-Amino-3-(1-ethyl-4-hydroxy-1H-1,2,3-triazol-5-yl)propanoic acid at 1.4 A resolution | | Descriptor: | (2~{S})-2-azanyl-3-(3-ethyl-5-oxidanyl-1,2,3-triazol-4-yl)propanoic acid, CHLORIDE ION, CITRIC ACID, ... | | Authors: | Moellerud, S, Temperini, P, Kastrup, J.S. | | Deposit date: | 2018-12-07 | | Release date: | 2019-04-17 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
J.Med.Chem., 62, 2019
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6Q60
 | | Structure of GluA2 ligand-binding domain (S1S2J) in complex with the agonist (S)-2-Amino-3-(2-methyl-5-hydroxy-2H-1,2,3-triazol-4-yl)propanoic acid at 1.55 A resolution | | Descriptor: | (2~{S})-2-azanyl-3-(2-methyl-5-oxidanyl-1,2,3-triazol-4-yl)propanoic acid, CHLORIDE ION, GLYCEROL, ... | | Authors: | Moellerud, S, Temperini, P, Kastrup, J.S. | | Deposit date: | 2018-12-10 | | Release date: | 2019-04-17 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
J.Med.Chem., 62, 2019
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4G8N
 | | Crystal structure of the kainate receptor GluK3 ligand-binding domain in complex with the agonist G8M | | Descriptor: | (1S,2R)-2-[(S)-amino(carboxy)methyl]cyclobutanecarboxylic acid, CHLORIDE ION, Glutamate receptor, ... | | Authors: | Venskutonyte, R, Kastrup, J.S, Frydenvang, K, Gajhede, M. | | Deposit date: | 2012-07-23 | | Release date: | 2012-08-29 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors.
J.Struct.Biol., 180, 2012
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4IGR
 | | Crystal structure of the kainate receptor GluK3 ligand-binding domain in complex with the agonist ZA302 | | Descriptor: | (4R)-4-{3-[hydroxy(methyl)amino]-3-oxopropyl}-L-glutamic acid, CHLORIDE ION, Glutamate receptor, ... | | Authors: | Larsen, A.P, Venskutonyte, R, Gajhede, M, Kastrup, J.S, Frydenvang, K. | | Deposit date: | 2012-12-18 | | Release date: | 2013-03-06 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.
J.Med.Chem., 56, 2013
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3GBB
 | | X-ray structure of iGluR5 ligand-binding core (S1S2) in complex with MSVIII-19 at 2.10A resolution | | Descriptor: | (2R,3aR,7aR)-2-[(2S)-2-amino-3-hydroxy-3-oxo-propyl]-3,3a,5,6,7,7a-hexahydrofuro[4,5-b]pyran-2-carboxylic acid, Glutamate receptor, ionotropic kainate 1 | | Authors: | Frydenvang, K, Naur, P, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2009-02-19 | | Release date: | 2009-03-17 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Full Domain Closure of the Ligand-binding Core of the Ionotropic Glutamate Receptor iGluR5 Induced by the High Affinity Agonist Dysiherbaine and the Functional Antagonist 8,9-Dideoxyneodysiherbaine
J.Biol.Chem., 284, 2009
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4YMB
 | | Structure of the ligand-binding domain of GluK1 in complex with the antagonist CNG10111 | | Descriptor: | (3R,4S)-3-(3-carboxyphenyl)-4-propyl-L-proline, 1,2-ETHANEDIOL, ACETATE ION, ... | | Authors: | Moller, C, Tapken, D, Kastrup, J.S, Frydenvang, K. | | Deposit date: | 2015-03-06 | | Release date: | 2015-08-05 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.93 Å) | | Cite: | Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.
J.Med.Chem., 58, 2015
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4QF9
 | | Structure of GluK1 ligand-binding domain (S1S2) in complex with (S)-2-amino-4-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-6-yl)butanoic acid at 2.28 A resolution | | Descriptor: | (2S)-2-amino-4-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-6-yl)butanoic acid, ACETATE ION, CHLORIDE ION, ... | | Authors: | Kristensen, C.M, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2014-05-20 | | Release date: | 2015-04-22 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Binding Mode of an alpha-Amino Acid-Linked Quinoxaline-2,3-dione Analogue at Glutamate Receptor Subtype GluK1.
ACS Chem Neurosci, 6, 2015
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5IKB
 | | Crystal structure of the kainate receptor GluK4 ligand binding domain in complex with kainate | | Descriptor: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, GLYCEROL, Glutamate receptor ionotropic, ... | | Authors: | Kristensen, O, Kristensen, L.B, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2016-03-03 | | Release date: | 2016-08-24 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | The Structure of a High-Affinity Kainate Receptor: GluK4 Ligand-Binding Domain Crystallized with Kainate.
Structure, 24, 2016
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4O3A
 | | Crystal structure of the glua2 ligand-binding domain in complex with L-aspartate at 1.80 a resolution | | Descriptor: | ACETATE ION, ASPARTIC ACID, CHLORIDE ION, ... | | Authors: | Krintel, C, Frydenvang, F, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2013-12-18 | | Release date: | 2014-04-16 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | L-Asp is a useful tool in the purification of the ionotropic glutamate receptor A2 ligand-binding domain.
Febs J., 281, 2014
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4O3B
 | | Crystal structure of an open/closed glua2 ligand-binding domain dimer at 1.91 A resolution | | Descriptor: | ACETATE ION, CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Krintel, C, de Rabassa, A.C, Frydenvang, K, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2013-12-18 | | Release date: | 2014-04-16 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.906 Å) | | Cite: | L-Asp is a useful tool in the purification of the ionotropic glutamate receptor A2 ligand-binding domain.
Febs J., 281, 2014
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4O3C
 | | Crystal structure of the GLUA2 ligand-binding domain in complex with L-aspartate at 1.50 A resolution | | Descriptor: | ACETATE ION, ASPARTIC ACID, CHLORIDE ION, ... | | Authors: | Krintel, C, Frydenvang, K, Kaern, A.M, Gajhede, M, Kastrup, J.S. | | Deposit date: | 2013-12-18 | | Release date: | 2014-04-16 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | L-Asp is a useful tool in the purification of the ionotropic glutamate receptor A2 ligand-binding domain.
Febs J., 281, 2014
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5M2V
 | | Structure of GluK1 ligand-binding domain (S1S2) in complex with (2S,4R)-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid at 3.18 A resolution | | Descriptor: | (2~{S},4~{R})-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Frydenvang, K, Kastrup, J.S, Kristensen, C.M. | | Deposit date: | 2016-10-13 | | Release date: | 2017-01-11 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (3.18 Å) | | Cite: | Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid.
J. Med. Chem., 60, 2017
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5NF6
 | | Structure of GluK3 ligand-binding domain (S1S2) in complex with CIP-AS at 2.55 A resolution | | Descriptor: | (3~{a}~{S},4~{S},6~{a}~{R})-4,5,6,6~{a}-tetrahydro-3~{a}~{H}-pyrrolo[3,4-d][1,2]oxazole-3,4-dicarboxylic acid, ACETATE ION, CHLORIDE ION, ... | | Authors: | Frydenvang, K, Venskutonyte, R, Thorsen, T.S, Kastrup, J.S. | | Deposit date: | 2017-03-13 | | Release date: | 2017-07-26 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Structure and Affinity of Two Bicyclic Glutamate Analogues at AMPA and Kainate Receptors.
ACS Chem Neurosci, 8, 2017
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