Loading
PDBj
MenuPDBj@FacebookPDBj@TwitterPDBj@YouTubewwPDB FoundationwwPDB
RCSB PDBPDBeBMRBAdv. SearchSearch help
Search by PDB author
8BSU
DownloadVisualize
BU of 8bsu by Molmil
Crystal structure of the kainate receptor GluK3-H523A ligand binding domain in complex with kainate and the positive allosteric modulator BPAM344 at 2.9A resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, ...
Authors:Venskutonyte, R, Frydenvang, K, Kastrup, J.S.
Deposit date:2022-11-26
Release date:2023-12-13
Last modified:2024-07-03
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure.
Febs J., 291, 2024
4MH5
DownloadVisualize
BU of 4mh5 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:2013-08-29
Release date:2013-10-16
Last modified:2023-09-20
Method:X-RAY DIFFRACTION (1.65 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
8QEZ
DownloadVisualize
BU of 8qez by Molmil
Crystal structure of the AMPA receptor GluA2-L504Y-N775S ligand binding domain in complex with L-glutamate and positive allosteric modulator BPAM395 at 1.55A resolution
Descriptor: 6-chloranyl-4-cyclopropyl-2,3-dihydrothieno[3,2-e][1,2,4]thiadiazine 1,1-dioxide, ACETATE ION, CACODYLATE ION, ...
Authors:Dorosz, J, Laulumaa, S, Frydenvang, K, Kastrup, J.S.
Deposit date:2023-09-01
Release date:2023-12-27
Last modified:2024-10-16
Method:X-RAY DIFFRACTION (1.55 Å)
Cite:Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators.
Eur.J.Med.Chem., 264, 2023
8BST
DownloadVisualize
BU of 8bst by Molmil
Crystal structure of the kainate receptor GluK3-H523A ligand binding domain in complex with kainate at 2.7A resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, ACETATE ION, CHLORIDE ION, ...
Authors:Venskutonyte, R, Frydenvang, K, Kastrup, J.S.
Deposit date:2022-11-26
Release date:2023-12-13
Last modified:2024-10-23
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure.
Febs J., 291, 2024
4IY6
DownloadVisualize
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:2024-10-16
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
4YMA
DownloadVisualize
BU of 4yma by Molmil
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:2024-10-23
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
5BUU
DownloadVisualize
BU of 5buu by Molmil
Crystal structure of the GluA2 ligand-binding domain (L483Y-N754S) in complex with glutamate and BPAM-321 at 2.07 A resolution
Descriptor: (3R)-7-chloro-2,3,4-trimethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, 1,2-ETHANEDIOL, GLUTAMIC ACID, ...
Authors:Larsen, A.P, Tapken, D, Frydenvang, K, Kastrup, J.S.
Deposit date:2015-06-04
Release date:2016-02-17
Last modified:2024-01-10
Method:X-RAY DIFFRACTION (2.07 Å)
Cite:Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.
Acs Chem Neurosci, 7, 2016
4IY5
DownloadVisualize
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
6SBT
DownloadVisualize
BU of 6sbt by Molmil
Structure of GluK1 ligand-binding domain (S1S2) in complex with N-(7-(1H-imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl benzamide at 2.3 A resolution
Descriptor: CHLORIDE ION, GLYCEROL, Glutamate receptor ionotropic, ...
Authors:Moellerud, S, Frydenvang, K, Kastrup, J.S.
Deposit date:2019-07-22
Release date:2019-10-30
Last modified:2024-01-24
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:N-(7-(1H-Imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)benzamide, a New Kainate Receptor Selective Antagonist and Analgesic: Synthesis, X-ray Crystallography, Structure-Affinity Relationships, and in Vitro and in Vivo Pharmacology.
Acs Chem Neurosci, 10, 2019
4DLD
DownloadVisualize
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:2024-10-30
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural and pharmacological characterization of phenylalanine-based AMPA receptor antagonists at kainate receptors
Chemmedchem, 7, 2012
5FHM
DownloadVisualize
BU of 5fhm by Molmil
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
4G8N
DownloadVisualize
BU of 4g8n by Molmil
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:2024-10-30
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
4E0W
DownloadVisualize
BU of 4e0w by Molmil
Crystal structure of the kainate receptor GluK3 ligand binding domain in complex with kainate
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, CHLORIDE ION, Glutamate receptor, ...
Authors:Venskutonyte, R, Frydenvang, K, Kastrup, J.S.
Deposit date:2012-03-05
Release date:2012-05-02
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.3501 Å)
Cite:Kainate induces various domain closures in AMPA and kainate receptors.
Neurochem Int, 61, 2012
4IGR
DownloadVisualize
BU of 4igr by Molmil
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:2024-10-30
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
3FAS
DownloadVisualize
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
4NWD
DownloadVisualize
BU of 4nwd by Molmil
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:2024-10-09
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
4NWC
DownloadVisualize
BU of 4nwc by Molmil
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:2024-10-30
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
3FAT
DownloadVisualize
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:2024-10-16
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
8R36
DownloadVisualize
BU of 8r36 by Molmil
Crystal structure of the Gluk1 ligand-binding domain in complex with kainate and BPAM538 at 1.90 A resolution
Descriptor: 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, 4-cyclopropyl-7-(3-methoxyphenoxy)-2,3-dihydro-1$l^{6},2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ...
Authors:Bay, Y, Frantsen, S.M, Frydenvang, K, Kastrup, J.S.
Deposit date:2023-11-08
Release date:2024-08-14
Last modified:2024-10-23
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Crystal structure of the GluK1 ligand-binding domain with kainate and the full-spanning positive allosteric modulator BPAM538.
J.Struct.Biol., 216, 2024
8R32
DownloadVisualize
BU of 8r32 by Molmil
Crystal structure of the GluK2 ligand-binding domain in complex with L-glutamate and BPAM344 at 1.60 A resolution
Descriptor: 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, GLUTAMIC ACID, ...
Authors:Bay, Y, Jeppesen, M.E, Frydenvang, K, Kastrup, J.S.
Deposit date:2023-11-08
Release date:2024-09-18
Method:X-RAY DIFFRACTION (1.6 Å)
Cite:The positive allosteric modulator BPAM344 and L-glutamate introduce an active-like structure of the ligand-binding domain of GluK2.
Febs Lett., 598, 2024
4ISU
DownloadVisualize
BU of 4isu by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with the antagonist (2R)-IKM-159 at 2.3A resolution.
Descriptor: (4aS,5aR,6R,8aS,8bS)-5a-(carboxymethyl)-8-oxo-2,4a,5a,6,7,8,8a,8b-octahydro-1H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6-carboxylic acid, CHLORIDE ION, Glutamate receptor 2, ...
Authors:Juknaite, L, Frydenvang, K, Kastrup, J.S.
Deposit date:2013-01-17
Release date:2013-03-20
Last modified:2024-10-30
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization.
J.Med.Chem., 56, 2013
4YMB
DownloadVisualize
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
3S2V
DownloadVisualize
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
3S9E
DownloadVisualize
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
4G8M
DownloadVisualize
BU of 4g8m by Molmil
Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with the agonist CBG-IV at 2.05A resolution
Descriptor: (1S,2R)-2-[(S)-amino(carboxy)methyl]cyclobutanecarboxylic acid, CHLORIDE ION, GLYCEROL, ...
Authors:Juknaite, L, Frydenvang, K, Kastrup, J.S, Gajhede, M.
Deposit date:2012-07-23
Release date:2012-08-08
Last modified:2023-09-13
Method:X-RAY DIFFRACTION (2.05 Å)
Cite:Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors.
J.Struct.Biol., 180, 2012

226707

PDB entries from 2024-10-30

PDB statisticsPDBj update infoContact PDBjnumon