2ANJ
| 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
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1YCJ
| 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
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1MQD
| X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.46 A resolution. Crystallization in the presence of lithium sulfate. | Descriptor: | (S)-2-AMINO-3-(3-HYDROXY-ISOXAZOL-4-YL)PROPIONIC ACID, GLYCEROL, Glutamate receptor subunit 2, ... | Authors: | Kasper, C, Lunn, M.-L, Liljefors, T, Gouaux, E, Egebjerg, J, Kastrup, J.S. | Deposit date: | 2002-09-16 | Release date: | 2003-07-01 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.46 Å) | Cite: | GluR2 ligand-binding core complexes: Importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists. FEBS Lett., 531, 2002
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1NNP
| X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-ATPA at 1.9 A resolution. Crystallization without zinc ions. | Descriptor: | 3-(5-TERT-BUTYL-3-OXIDOISOXAZOL-4-YL)-L-ALANINATE, Glutamate receptor 2, SULFATE ION | Authors: | Lunn, M.L, Hogner, A, Stensbol, T.B, Gouaux, E, Egebjerg, J, Kastrup, J.S. | Deposit date: | 2003-01-14 | Release date: | 2003-03-11 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Three-Dimensional Structure of the Ligand-Binding
Core of GluR2 in Complex with the Agonist (S)-ATPA:
Implications for Receptor Subunit Selectivity. J.Med.Chem., 46, 2003
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1NNK
| X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-ATPA at 1.85 A resolution. Crystallization with zinc ions. | Descriptor: | 3-(5-TERT-BUTYL-3-OXIDOISOXAZOL-4-YL)-L-ALANINATE, CHLORIDE ION, Glutamate receptor 2, ... | Authors: | Lunn, M.-L, Hogner, A, Stensbol, T.B, Gouaux, E, Egebjerg, J, Kastrup, J.S. | Deposit date: | 2003-01-14 | Release date: | 2003-03-04 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Three-Dimensional Structure of the Ligand-Binding
Core of GluR2 in Complex with the Agonist (S)-ATPA:
Implications for Receptor Subunit Selectivity. J.Med.Chem., 46, 2003
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1N0T
| X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with the antagonist (S)-ATPO at 2.1 A resolution. | Descriptor: | (S)-2-AMINO-3-(5-TERT-BUTYL-3-(PHOSPHONOMETHOXY)-4-ISOXAZOLYL)PROPIONIC ACID, ACETATE ION, Glutamate receptor 2, ... | Authors: | Hogner, A, Greenwood, J.R, Liljefors, T, Lunn, M.-L, Egebjerg, J, Larsen, I.K, Gouaux, E, Kastrup, J.S. | Deposit date: | 2002-10-15 | Release date: | 2003-03-04 | Last modified: | 2017-08-16 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Competitive antagonism of AMPA receptors by ligands of
different classes: crystal structure of ATPO bound to the
GluR2 ligand-binding core, in comparison with DNQX. J.Med.Chem., 46, 2003
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1MS7
| X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.97 A resolution, Crystallization in the presence of zinc acetate | Descriptor: | (S)-2-AMINO-3-(3-HYDROXY-ISOXAZOL-4-YL)PROPIONIC ACID, Glutamate receptor subunit 2, ZINC ION | Authors: | Kasper, C, Lunn, M.-L, Liljefors, T, Gouaux, E, Egebjerg, J, Kastrup, J.S. | Deposit date: | 2002-09-19 | Release date: | 2003-07-08 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.97 Å) | Cite: | GluR2 ligand-binding core complexes: importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists FEBS Lett., 531, 2002
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1M5C
| X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) IN COMPLEX WITH Br-HIBO AT 1.65 A RESOLUTION | Descriptor: | (S)-2-AMINO-3-(4-BROMO-3-HYDROXY-ISOXAZOL-5-YL)PROPIONIC ACID, Glutamate receptor 2 | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | Deposit date: | 2002-07-09 | Release date: | 2002-09-18 | Last modified: | 2017-08-16 | Method: | X-RAY DIFFRACTION (1.65 Å) | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core J.Mol.Biol., 322, 2002
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1M5F
| X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J-Y702F) IN COMPLEX WITH ACPA AT 1.95 A RESOLUTION | Descriptor: | (S)-2-AMINO-3-(3-CARBOXY-5-METHYLISOXAZOL-4-YL)PROPIONIC ACID, ACETATE ION, Glutamate receptor 2, ... | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | Deposit date: | 2002-07-09 | Release date: | 2002-09-18 | Last modified: | 2021-10-27 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core J.Mol.Biol., 322, 2002
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1M5E
| X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) IN COMPLEX WITH ACPA AT 1.46 A RESOLUTION | Descriptor: | (S)-2-AMINO-3-(3-CARBOXY-5-METHYLISOXAZOL-4-YL)PROPIONIC ACID, ACETATE ION, Glutamate receptor 2, ... | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | Deposit date: | 2002-07-09 | Release date: | 2002-09-18 | Last modified: | 2017-08-16 | Method: | X-RAY DIFFRACTION (1.46 Å) | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core J.Mol.Biol., 322, 2002
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1M5D
| X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J-Y702F) IN COMPLEX WITH Br-HIBO AT 1.73 A RESOLUTION | Descriptor: | (S)-2-AMINO-3-(4-BROMO-3-HYDROXY-ISOXAZOL-5-YL)PROPIONIC ACID, Glutamate receptor 2, SULFATE ION | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | Deposit date: | 2002-07-09 | Release date: | 2002-09-18 | Last modified: | 2021-10-27 | Method: | X-RAY DIFFRACTION (1.73 Å) | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core J.Mol.Biol., 322, 2002
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1M5B
| X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE (S1S2J) IN COMPLEX WITH 2-Me-Tet-AMPA AT 1.85 A RESOLUTION. | Descriptor: | (S)-2-AMINO-3-[3-HYDROXY-5-(2-METHYL-2H-TETRAZOL-5-YL)ISOXAZOL-4-YL]PROPIONIC ACID, Glutamate receptor 2, ZINC ION | Authors: | Hogner, A, Kastrup, J.S, Jin, R, Liljefors, T, Mayer, M.L, Egebjerg, J, Larsen, I.K, Gouaux, E. | Deposit date: | 2002-07-09 | Release date: | 2002-09-18 | Last modified: | 2017-08-16 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Structural Basis for AMPA Receptor Activation and Ligand Selectivity:
Crystal Structures of Five Agonist Complexes with the GluR2 Ligand-binding
Core J.Mol.Biol., 322, 2002
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2P2A
| X-ray structure of the GluR2 ligand binding core (S1S2J) in complex with 2-Bn-tet-AMPA at 2.26A resolution | Descriptor: | 2-AMINO-3-[3-HYDROXY-5-(2-BENZYL-2H-5-TETRAZOLYL)-4-ISOXAZOLYL]-PROPIONIC ACID, GLUTAMIC ACID, Glutamate receptor 2, ... | Authors: | Frydenvang, K, Kastrup, J.S, Gajhede, M. | Deposit date: | 2007-03-07 | Release date: | 2007-06-19 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.26 Å) | Cite: | A tetrazolyl-substituted subtype-selective AMPA receptor agonist. J.Med.Chem., 50, 2007
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2AIX
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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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2PBW
| 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
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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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4N7E
| Crystal structure of the Vps10p domain of human sortilin/NTS3 in complex with AF38469 | Descriptor: | 2-[(6-methylpyridin-2-yl)carbamoyl]-5-(trifluoromethyl)benzoic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Sortilin, ... | Authors: | Andersen, J.L, Strandbygaard, D, Thirup, S. | Deposit date: | 2013-10-15 | Release date: | 2014-01-22 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorg.Med.Chem.Lett., 24, 2014
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5MFW
| 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
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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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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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2V3T
| 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
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2V3U
| 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
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4MSL
| Crystal structure of the Vps10p domain of human sortilin/NTS3 in complex with AF40431 | Descriptor: | N-[(7-hydroxy-4-methyl-2-oxo-2H-chromen-8-yl)methyl]-L-leucine, Sortilin, TETRAETHYLENE GLYCOL, ... | Authors: | Andersen, J.L, Strandbygaard, D, Thirup, S. | Deposit date: | 2013-09-18 | Release date: | 2014-02-12 | Last modified: | 2020-07-29 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex. Acta Crystallogr.,Sect.D, 70, 2014
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