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3GBA
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X-RAY STRUCTURE OF IGLUR5 LIGAND-BINDING CORE (S1S2) IN COMPLEX WITH DYSIHERBAINE AT 1.35A RESOLUTION
Descriptor:Glutamate receptor, ionotropic kainate 1, (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, ...
Authors:Frydenvang, K., Naur, P., Gajhede, M., Kastrup, J.S.
Deposit date:2009-02-19
Release date:2009-03-17
Last modified:2017-08-16
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
3GBB
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X-RAY STRUCUTRE OF IGLUR5 LIGAND-BINDING CORE (S1S2) IN COMPLEX WITH MSVIII-19 AT 2.10A RESOLUTION
Descriptor:Glutamate receptor, ionotropic kainate 1, (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
Authors:Frydenvang, K., Naur, P., Gajhede, M., Kastrup, J.S.
Deposit date:2009-02-19
Release date:2009-03-17
Last modified:2017-11-01
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
3PD8
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X-RAY STRUCTURE OF THE LIGAND-BINDING CORE OF GLUA2 IN COMPLEX WITH (S)-7-HPCA AT 2.5 A RESOLUTION
Descriptor:Glutamate receptor 2, ZINC ION, (7S)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-7-carboxylic acid, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2010-10-22
Release date:2010-12-29
Last modified:2018-10-10
Method:X-RAY DIFFRACTION (2.476 Å)
Cite:Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid.
J. Med. Chem., 53, 2010
3PD9
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X-RAY STRUCTURE OF THE LIGAND-BINDING CORE OF GLUA2 IN COMPLEX WITH (R)-5-HPCA AT 2.1 A RESOLUTION
Descriptor:Glutamate receptor 2, (5R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid, SULFATE ION, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2010-10-22
Release date:2010-12-29
Last modified:2018-10-10
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid.
J. Med. Chem., 53, 2010
5FHN
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J) IN COMPLEX WITH (S)-2-AMINO-3-(5-(2-(3-METHYLBENZYL)-2H-TETRAZOL-5-YL)-3-HYDROXYISOXAZOL-4-YL)PROPANOIC ACID AT 1.6 A RESOLUTION
Descriptor:Glutamate receptor 2,Glutamate receptor 2, SULFATE ION, GLYCEROL, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2015-12-22
Release date:2016-03-02
Last modified:2018-01-17
Method:X-RAY DIFFRACTION (1.6 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
5FHO
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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:Glutamate receptor 2,Glutamate receptor 2, (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, SULFATE ION, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2015-12-22
Release date:2016-03-02
Last modified:2018-01-17
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
5M2V
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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:Glutamate receptor ionotropic, kainate 1,Glutamate receptor ionotropic, kainate 1, ...
Authors:Frydenvang, K., Kastrup, J.S., Kristensen, C.M.
Deposit date:2016-10-13
Release date:2017-01-11
Last modified:2017-08-09
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
2P2A
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X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) IN COMPLEX WITH 2-BN-TET-AMPA AT 2.26A RESOLUTION
Descriptor:Glutamate receptor 2, SULFATE ION, GLUTAMIC ACID, ...
Authors:Frydenvang, K., Kastrup, J.S., Gajhede, M.
Deposit date:2007-03-07
Release date:2007-06-19
Last modified:2017-08-16
Method:X-RAY DIFFRACTION (2.26 Å)
Cite:A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
J.Med.Chem., 50, 2007
3TZA
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J) IN COMPLEX WITH THE ANTAGONIST (S)-2-AMINO-3-(2-(2-CARBOXYETHYL)-5-CHLORO-4-NITROPHENYL)PROPIONIC ACID AT 1.9A RESOLUTION
Descriptor:Glutamate receptor 2,Glutamate receptor 2, (S)-2-amino-3-(2-(2-carboxyethyl)-5-chloro-4-nitrophenyl)propionic acid, SULFATE ION
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2011-09-27
Release date:2011-10-26
Last modified:2017-06-14
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:A new phenylalanine derivative acts as an antagonist at the AMPA receptor GluA2 and introduces partial domain closure: synthesis, resolution, pharmacology, and crystal structure
J.Med.Chem., 54, 2011
4E0X
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CRYSTAL STRUCTURE OF THE KAINATE RECEPTOR GLUK1 LIGAND-BINDING DOMAIN IN COMPLEX WITH KAINATE IN THE ABSENCE OF GLYCEROL
Descriptor:Glutamate receptor, ionotropic kainate 1, 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2012-03-05
Release date:2012-04-25
Last modified:2017-08-02
Method:X-RAY DIFFRACTION (2 Å)
Cite:Kainate induces various domain closures in AMPA and kainate receptors.
Neurochem Int, 61, 2012
5CBR
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J) IN COMPLEX WITH THE ANTAGONIST (S)-2-AMINO-3-(3,4-DICHLORO-5-(5-HYDROXYPYRIDIN-3-YL)PHENYL)PROPANOIC ACID AT 2.0A RESOLUTION
Descriptor:Glutamate receptor 2,Glutamate receptor 2, 3,4-dichloro-5-(5-hydroxypyridin-3-yl)-L-phenylalanine, GLYCEROL, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2015-07-01
Release date:2015-12-30
Last modified:2016-01-27
Method:X-RAY DIFFRACTION (1.996 Å)
Cite:Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors.
J.Med.Chem., 59, 2016
5CBS
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J) IN COMPLEX WITH THE ANTAGONIST (R)-2-AMINO-3-(3'-HYDROXYBIPHENYL-3-YL)PROPANOIC ACID AT 1.8A RESOLUTION
Descriptor:Glutamate receptor 2,Glutamate receptor 2, (R)-2-amino-3-(3'-hydroxybiphenyl-3-yl)propanoic acid, SULFATE ION, ...
Authors:Frydenvang, K., Kastrup, J.S.
Deposit date:2015-07-01
Release date:2015-12-30
Last modified:2018-01-17
Method:X-RAY DIFFRACTION (1.801 Å)
Cite:Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors.
J.Med.Chem., 59, 2016
5NF5
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STRUCTURE OF GLUK1 LIGAND-BINDING DOMAIN (S1S2) IN COMPLEX WITH CIP-AS AT 2.85 A RESOLUTION
Descriptor:Glutamate receptor ionotropic, kainate 1,Glutamate receptor ionotropic, kainate 1, ...
Authors:Frydenvang, K., Venskutonyte, R., Thorsen, T.S., Kastrup, J.S.
Deposit date:2017-03-13
Release date:2017-07-26
Last modified:2017-09-27
Method:X-RAY DIFFRACTION (2.85 Å)
Cite:Structure and Affinity of Two Bicyclic Glutamate Analogues at AMPA and Kainate Receptors.
ACS Chem Neurosci, 8, 2017
5NF6
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STRUCTURE OF GLUK3 LIGAND-BINDING DOMAIN (S1S2) IN COMPLEX WITH CIP-AS AT 2.55 A RESOLUTION
Descriptor:Glutamate receptor ionotropic, kainate 3,Glutamate receptor ionotropic, kainate 3, ...
Authors:Frydenvang, K., Venskutonyte, R., Thorsen, T.S., Kastrup, J.S.
Deposit date:2017-03-13
Release date:2017-07-26
Last modified:2017-09-27
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
5ELV
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L504-N775) IN COMPLEX WITH GLUTAMATE AND BPAM-521 AT 1.92 A RESOLUTION
Descriptor:Glutamate receptor 2,Glutamate receptor 2, SULFATE ION, GLYCEROL, ...
Authors:Krintel, C., Juknaite, L., Frydenvang, K., Kastrup, J.S.
Deposit date:2015-11-05
Release date:2016-05-04
Last modified:2018-03-07
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
4U4S
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L483Y-N754S) IN COMPLEX WITH GLUTAMATE AND BPAM25 AT 1.90 A RESOLUTION.
Descriptor:Glutamate receptor 2,Glutamate receptor 2, 4-ethyl-3,4-dihydro-2H-pyrido[4,3-e][1,2,4]thiadiazine 1,1-dioxide, SULFATE ION, ...
Authors:Noerholm, A.B., Deva, T., Frydenvang, K., Kastrup, J.S.
Deposit date:2014-07-24
Release date:2014-11-19
Last modified:2018-06-13
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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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L483Y-N754S) IN COMPLEX WITH GLUTAMATE AND BPAM37 AT 1.56 A RESOLUTION.
Descriptor:Glutamate receptor 2,Glutamate receptor 2, 4-ethyl-3,4-dihydro-2H-pyrido[3,2-e][1,2,4]thiadiazine 1,1-dioxide, SULFATE ION, ...
Authors:Noerholm, A.B., Frydenvang, K., Kastrup, J.S.
Deposit date:2014-07-24
Release date:2014-11-19
Last modified:2018-01-17
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
4IY5
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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L483Y-N754S) IN COMPLEX WITH GLUTAMATE AND CX516 AT 2.0 A RESOLUTION
Descriptor:Glutamate receptor 2, GLUTAMIC ACID, SULFATE ION, ...
Authors:Krintel, C., Frydenvang, K., Harpsoe, K., Gajhede, M., Kastrup, J.S.
Deposit date:2013-01-28
Release date:2013-10-09
Last modified:2017-08-23
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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CRYSTAL STRUCTURE OF THE GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L483Y-N754S) IN COMPLEX WITH GLUTAMATE AND ME-CX516 AT 1.72 A RESOLUTION
Descriptor:Glutamate receptor 2, [(3R)-3-methylpiperidin-1-yl](quinoxalin-6-yl)methanone, [(3S)-3-methylpiperidin-1-yl](quinoxalin-6-yl)methanone, ...
Authors:Krintel, C., Frydenvang, K., Harpsoe, K., Gajhede, M., Kastrup, J.S.
Deposit date:2013-01-28
Release date:2013-10-09
Last modified:2017-08-23
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
4E0W
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CRYSTAL STRUCTURE OF THE KAINATE RECEPTOR GLUK3 LIGAND BINDING DOMAIN IN COMPLEX WITH KAINATE
Descriptor:Glutamate receptor, ionotropic kainate 3, 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, ...
Authors:Venskutonyte, R., Frydenvang, K., Kastrup, J.S.
Deposit date:2012-03-05
Release date:2012-05-02
Last modified:2017-08-02
Method:X-RAY DIFFRACTION (2.3501 Å)
Cite:Kainate induces various domain closures in AMPA and kainate receptors.
Neurochem Int, 61, 2012
4G8N
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CRYSTAL STRUCTURE OF THE KAINATE RECEPTOR GLUK3 LIGAND-BINDING DOMAIN IN COMPLEX WITH THE AGONIST G8M
Descriptor:Glutamate receptor, ionotropic kainate 3, (1S,2R)-2-[(S)-amino(carboxy)methyl]cyclobutanecarboxylic acid, ...
Authors:Venskutonyte, R., Kastrup, J.S., Frydenvang, K., Gajhede, M.
Deposit date:2012-07-23
Release date:2012-08-29
Last modified:2017-08-23
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
4IGR
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CRYSTAL STRUCTURE OF THE KAINATE RECEPTOR GLUK3 LIGAND-BINDING DOMAIN IN COMPLEX WITH THE AGONIST ZA302
Descriptor:Glutamate receptor, ionotropic kainate 3, (4R)-4-{3-[hydroxy(methyl)amino]-3-oxopropyl}-L-glutamic acid, ...
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:2017-08-23
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
4NWC
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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:Glutamate receptor ionotropic, kainate 3, POTASSIUM ION, ...
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:2017-08-09
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
4NWD
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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:Glutamate receptor ionotropic, kainate 3, (4R)-4-[3-(methylamino)-3-oxopropyl]-L-glutamic acid, ...
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:2017-08-09
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
4YMA
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STRUCTURE OF THE LIGAND-BINDING DOMAIN OF GLUA2 IN COMPLEX WITH THE ANTAGONIST CNG10109
Descriptor:Glutamate receptor 2, SULFATE ION, GLYCEROL, ...
Authors:Moller, C., Tapken, D., Kastrup, J.S., Frydenvang, K.
Deposit date:2015-03-06
Release date:2015-08-05
Last modified:2018-03-07
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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