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1YCJ
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BU of 1ycj by Molmil
Crystal structure of the kainate receptor GluR5 ligand-binding core in complex with (S)-glutamate
Descriptor: GLUTAMIC ACID, Ionotropic glutamate receptor 5, SULFATE ION
Authors:Naur, P, Vestergaard, B, Skov, L.K, Egebjerg, J, Gajhede, M, Kastrup, J.S.
Deposit date:2004-12-22
Release date:2005-02-01
Last modified:2023-10-25
Method:X-RAY DIFFRACTION (1.95 Å)
Cite:Crystal structure of the kainate receptor GluR5 ligand-binding core in complex with (S)-glutamate
Febs Lett., 579, 2005
2V3T
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BU of 2v3t by Molmil
Structure of the ligand-binding core of the ionotropic glutamate receptor-like GluRdelta2 in the apo form
Descriptor: CALCIUM ION, GLUTAMATE RECEPTOR DELTA-2 SUBUNIT SYNONYM GLURDELTA2, GLUR DELTA-2
Authors:Naur, P, Vestergaard, B, Gajhede, M, Kastrup, J.S.
Deposit date:2007-06-22
Release date:2007-08-07
Last modified:2019-07-24
Method:X-RAY DIFFRACTION (2.75 Å)
Cite:Ionotropic Glutamate-Like Receptor {Delta}2 Binds D-Serine and Glycine.
Proc.Natl.Acad.Sci.USA, 104, 2007
2V3U
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BU of 2v3u by Molmil
Structure of the ligand-binding core of the ionotropic glutamate receptor-like GluRdelta2 in complex with D-serine
Descriptor: CHLORIDE ION, D-SERINE, GLUTAMATE RECEPTOR DELTA-2 SUBUNIT, ...
Authors:Naur, P, Vestergaard, B, Gajhede, M, Kastrup, J.S.
Deposit date:2007-06-22
Release date:2007-08-07
Last modified:2023-12-13
Method:X-RAY DIFFRACTION (1.74 Å)
Cite:Ionotropic Glutamate-Like Receptor {Delta}2 Binds D-Serine and Glycine.
Proc.Natl.Acad.Sci.USA, 104, 2007
5CC2
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BU of 5cc2 by Molmil
STRUCTURE OF THE LIGAND-BINDING DOMAIN OF THE IONOTROPIC GLUTAMATE RECEPTOR-LIKE GLUD2 IN COMPLEX WITH 7-CKA
Descriptor: 7-Chlorokynurenic acid, CHLORIDE ION, GLYCEROL, ...
Authors:Naur, P, Gajhede, M, Kastrup, J.S.
Deposit date:2015-07-01
Release date:2015-12-30
Last modified:2024-01-10
Method:X-RAY DIFFRACTION (2.501 Å)
Cite:Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 Receptors.
Mol.Pharmacol., 89, 2016
2WKY
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BU of 2wky by Molmil
Crystal structure of the ligand-binding core of GluR5 in complex with the agonist 4-AHCP
Descriptor: 3-(3-HYDROXY-7,8-DIHYDRO-6H-CYCLOHEPTA[D]ISOXAZOL-4-YL)-L-ALANINE, CHLORIDE ION, GLUTAMATE RECEPTOR, ...
Authors:Naur, P, Gajhede, M, Kastrup, J.S.
Deposit date:2009-06-18
Release date:2009-07-21
Last modified:2023-12-13
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:The Glutamate Receptor Glur5 Agonist (S)-2-Amino-3-(3-Hydroxy-7,8-Dihydro-6H-Cyclohepta[D]Isoxazol-4-Yl)Propionic Acid and the 8-Methyl Analogue: Synthesis, Molecular Pharmacology, and Biostructural Characterization
J.Med.Chem., 52, 2009
1VSO
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BU of 1vso by Molmil
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
3GBB
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BU of 3gbb by Molmil
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
2PBW
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BU of 2pbw by Molmil
Crystal Structure of the Ligand-Binding Core of iGluR5 in Complex with the Partial agonist Domoic Acid at 2.5 A Resolution
Descriptor: (2S,3S,4S)-2-CARBOXY-4-[(1Z,3E,5R)-5-CARBOXY-1-METHYL-1,3-HEXADIENYL]-3-PYRROLIDINEACETIC ACID, Glutamate receptor, ionotropic kainate 1
Authors:Hald, H, Naur, P, Gajhede, M, Kastrup, J.S.
Deposit date:2007-03-29
Release date:2007-07-03
Last modified:2023-08-30
Method:X-RAY DIFFRACTION (2.5 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
3GBA
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BU of 3gba by Molmil
X-ray structure of iGluR5 ligand-binding core (S1S2) in complex with dysiherbaine at 1.35A resolution
Descriptor: (2R,3aR,6S,7R,7aR)-2-[(2S)-2-amino-2-carboxyethyl]-6-hydroxy-7-(methylamino)hexahydro-2H-furo[3,2-b]pyran-2-carboxylic acid, CHLORIDE ION, GLYCEROL, ...
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 (1.35 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
2ANJ
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BU of 2anj by Molmil
Crystal Structure of the Glur2 Ligand Binding Core (S1S2J-Y450W) Mutant in Complex With the Partial Agonist Kainic Acid at 2.1 A Resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, Glutamate receptor 2
Authors:Holm, M.M, Naur, P, Vestergaard, B, Geballe, M.T, Gajhede, M, Kastrup, J.S, Traynelis, S.F, Egebjerg, J.
Deposit date:2005-08-11
Release date:2005-08-30
Last modified:2023-08-23
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:A Binding Site Tyrosine Shapes Desensitization Kinetics and Agonist Potency at GluR2: a mutagenic, kinetic, and crystallographic study
J.Biol.Chem., 280, 2005
3FAS
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BU of 3fas by Molmil
X-ray structure of iGluR4 flip ligand-binding core (S1S2) in complex with (S)-glutamate at 1.40A resolution
Descriptor: GLUTAMIC ACID, GLYCEROL, Glutamate receptor 4, ...
Authors:Kasper, C, Frydenvang, K, Naur, P, Gajhede, M, Kastrup, J.S.
Deposit date:2008-11-18
Release date:2008-12-09
Last modified:2023-11-01
Method:X-RAY DIFFRACTION (1.4 Å)
Cite:Molecular mechanism of agonist recognition by the ligand-binding core of the ionotropic glutamate receptor 4
Febs Lett., 582, 2008
3FAT
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BU of 3fat by Molmil
X-ray structure of iGluR4 flip ligand-binding core (S1S2) in complex with (S)-AMPA at 1.90A resolution
Descriptor: (S)-ALPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID, ACETIC ACID, GLYCEROL, ...
Authors:Kasper, C, Frydenvang, K, Naur, P, Gajhede, M, Kastrup, J.S.
Deposit date:2008-11-18
Release date:2008-12-09
Last modified:2023-11-01
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Molecular mechanism of agonist recognition by the ligand-binding core of the ionotropic glutamate receptor 4
Febs Lett., 582, 2008
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
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
4U4S
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BU of 4u4s by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and BPAM25 at 1.90 A resolution.
Descriptor: 4-ethyl-3,4-dihydro-2H-pyrido[4,3-e][1,2,4]thiadiazine 1,1-dioxide, ACETATE ION, CHLORIDE ION, ...
Authors:Noerholm, A.B, Deva, T, Frydenvang, K, Kastrup, J.S.
Deposit date:2014-07-24
Release date:2014-11-19
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Positive Allosteric Modulators of 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors Belonging to 4-Cyclopropyl-3,4-dihydro-2H-1,2,4-pyridothiadiazine Dioxides and Diversely Chloro-Substituted 4-Cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides.
J.Med.Chem., 57, 2014
4U4X
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BU of 4u4x by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and BPAM37 at 1.56 A resolution.
Descriptor: 4-ethyl-3,4-dihydro-2H-pyrido[3,2-e][1,2,4]thiadiazine 1,1-dioxide, ACETATE ION, DI(HYDROXYETHYL)ETHER, ...
Authors:Noerholm, A.B, Frydenvang, K, Kastrup, J.S.
Deposit date:2014-07-24
Release date:2014-11-19
Last modified:2023-12-20
Method:X-RAY DIFFRACTION (1.56 Å)
Cite:Positive Allosteric Modulators of 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors Belonging to 4-Cyclopropyl-3,4-dihydro-2H-1,2,4-pyridothiadiazine Dioxides and Diversely Chloro-Substituted 4-Cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides.
J.Med.Chem., 57, 2014
5ELV
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BU of 5elv by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J-L504-N775) in complex with glutamate and BPAM-521 at 1.92 A resolution
Descriptor: 4-Cyclopropyl-3,4-dihydro-7-hydroxy-2H-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, CHLORIDE ION, ...
Authors:Krintel, C, Juknaite, L, Frydenvang, K, Kastrup, J.S.
Deposit date:2015-11-05
Release date:2016-05-04
Last modified:2024-01-10
Method:X-RAY DIFFRACTION (1.92 Å)
Cite:Enthalpy-Entropy Compensation in the Binding of Modulators at Ionotropic Glutamate Receptor GluA2.
Biophys.J., 110, 2016
4YMB
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BU of 4ymb by Molmil
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
4IY5
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BU of 4iy5 by Molmil
Crystal structure of the glua2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and CX516 at 2.0 A resolution
Descriptor: CHLORIDE ION, GLUTAMIC ACID, GLYCEROL, ...
Authors:Krintel, C, Frydenvang, K, Harpsoe, K, Gajhede, M, Kastrup, J.S.
Deposit date:2013-01-28
Release date:2013-10-09
Last modified:2023-11-08
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain
Acta Crystallogr.,Sect.D, 69, 2013
4IY6
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BU of 4iy6 by Molmil
Crystal structure of the GLUA2 ligand-binding domain (S1S2J-L483Y-N754S) in complex with glutamate and ME-CX516 at 1.72 A resolution
Descriptor: GLUTAMIC ACID, GLYCEROL, Glutamate receptor 2, ...
Authors:Krintel, C, Frydenvang, K, Harpsoe, K, Gajhede, M, Kastrup, J.S.
Deposit date:2013-01-28
Release date:2013-10-09
Last modified:2023-11-08
Method:X-RAY DIFFRACTION (1.72 Å)
Cite:Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain
Acta Crystallogr.,Sect.D, 69, 2013
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
5MFW
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BU of 5mfw by Molmil
Crystal structure of the GluK1 ligand-binding domain in complex with kainate and BPAM-121 at 2.10 A resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, ...
Authors:Larsen, A.P, Frydenvang, K, Kastrup, J.S.
Deposit date:2016-11-18
Release date:2017-04-12
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
5MFQ
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BU of 5mfq by Molmil
Crystal structure of the GluK1 ligand-binding domain in complex with kainate and BPAM-344 at 1.90 A resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ...
Authors:Larsen, A.P, Frydenvang, K, Kastrup, J.S.
Deposit date:2016-11-18
Release date:2017-04-12
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
5MFV
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BU of 5mfv by Molmil
Crystal structure of the GluK1 ligand-binding domain in complex with kainate and BPAM-521 at 2.18 A resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-Cyclopropyl-3,4-dihydro-7-hydroxy-2H-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, ...
Authors:Larsen, A.P, Frydenvang, K, Kastrup, J.S.
Deposit date:2016-11-18
Release date:2017-04-12
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (2.181 Å)
Cite:Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors.
Mol. Pharmacol., 91, 2017
4DLD
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BU of 4dld by Molmil
Crystal structure of the GluK1 ligand-binding domain (S1S2) in complex with the antagonist (S)-2-amino-3-(2-(2-carboxyethyl)-5-chloro-4-nitrophenyl)propionic acid at 2.0 A resolution
Descriptor: (S)-2-amino-3-(2-(2-carboxyethyl)-5-chloro-4-nitrophenyl)propionic acid, CHLORIDE ION, GLYCEROL, ...
Authors:Venskutonyte, R, Frydenvang, K, Kastrup, J.S.
Deposit date:2012-02-06
Release date:2012-10-10
Last modified:2023-11-08
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural and pharmacological characterization of phenylalanine-based AMPA receptor antagonists at kainate receptors
Chemmedchem, 7, 2012

 

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