1PB9
 
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1PBQ
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8BN2
 | | Crystal structure of the ligand-binding domain (LBD) of human iGluR Delta-1 (GluD1) in complex with D-Serine | | Descriptor: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | Authors: | Heroven, C, Malinauskas, T, Aricescu, A.R. | | Deposit date: | 2022-11-11 | | Release date: | 2023-11-22 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | GluD1 binds GABA and controls inhibitory plasticity.
Science, 382, 2023
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8BN5
 | | Crystal structure of the ligand-binding domain (LBD) of human iGluR Delta-1 (GluD1) in complex with GABA | | Descriptor: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | Authors: | Heroven, C, Malinauskas, T, Aricescu, A.R. | | Deposit date: | 2022-11-12 | | Release date: | 2023-11-22 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | GluD1 binds GABA and controls inhibitory plasticity.
Science, 382, 2023
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8BLJ
 | | Crystal structure of the ligand-binding domain (LBD) of human iGluR Delta-1 (GluD1), apo state | | Descriptor: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | Authors: | Heroven, C, Malinauskas, T, Aricescu, A.R. | | Deposit date: | 2022-11-09 | | Release date: | 2023-11-22 | | Last modified: | 2024-01-03 | | Method: | X-RAY DIFFRACTION (2.18 Å) | | Cite: | GluD1 binds GABA and controls inhibitory plasticity.
Science, 382, 2023
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8BSU
 | | 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
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8BST
 | | 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: | 2024-04-10 | | 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
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1SD3
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6FAZ
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with the positive allosteric modulator TDPAM01 at 1.4 A resolution. | | Descriptor: | 1,2-ETHANEDIOL, 6,6'-(Ethane-1,2-diyl)bis(4-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide), ACETATE ION, ... | | Authors: | Nielsen, L, Laulumaa, S, Kastrup, J.S. | | Deposit date: | 2017-12-18 | | Release date: | 2018-11-21 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds.
J. Med. Chem., 61, 2018
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6F29
 | | Crystal structure of the kainate receptor GluK3 ligand binding domain in complex with (S)-1-[2-Amino-2-carboxyethyl]-5,7-dihydrothieno[3,4-d]pyrimidin-2,4(1H,3H)-dione at resolution 2.6A | | Descriptor: | (2~{S})-2-azanyl-3-[2,4-bis(oxidanylidene)-5,7-dihydrothieno[3,4-d]pyrimidin-1-yl]propanoic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2017-11-23 | | Release date: | 2018-02-28 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | ( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
J. Med. Chem., 61, 2018
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8C2H
 | | Transmembrane domain of active state homomeric GluA1 AMPA receptor in tandem with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 1 flip isoform, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-22 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.64 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1P
 | | Active state homomeric GluA1 AMPA receptor in complex with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, CYCLOTHIAZIDE, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1S
 | | Transmembrane domain of resting state homomeric GluA2 F231A mutant AMPA receptor in complex with TARP gamma 2 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 2, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C2I
 | | Transmembrane domain of resting state homomeric GluA1 AMPA receptor in complex with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 1 flip isoform, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-22 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1R
 | | Resting state homomeric GluA2 F231A mutant AMPA receptor in complex with TARP gamma-2 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 2, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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8C1Q
 | | Resting state homomeric GluA1 AMPA receptor in complex with TARP gamma 3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor 1 flip isoform, ... | | Authors: | Zhang, D, Ivica, J, Krieger, J.M, Ho, H, Yamashita, K, Cais, O, Greger, I. | | Deposit date: | 2022-12-21 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.82 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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6F28
 | | Crystal structure of the kainate receptor GluK3 ligand binding domain in complex with (S)-1-[2'-Amino-2'-carboxyethyl]-6-methyl-5,7-dihydropyrrolo[3,4-d]pyrimidin-2,4(1H,3H)-dione at resolution 2.4A | | Descriptor: | (2~{S})-2-azanyl-3-[6-methyl-2,4-bis(oxidanylidene)-5,7-dihydropyrrolo[3,4-d]pyrimidin-1-yl]propanoic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | Authors: | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2017-11-23 | | Release date: | 2018-02-28 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | ( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
J. Med. Chem., 61, 2018
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7KS0
 | | GluK2/K5 with 6-Cyano-7-nitroquinoxaline-2,3-dione (CNQX) | | Descriptor: | Glutamate receptor ionotropic, kainate 2, kainate 5,Green fluorescent protein chimera | | Authors: | Khanra, N, Brown, P.M.G.E, Perozzo, A.M, Bowie, D, Meyerson, J.R. | | Deposit date: | 2020-11-20 | | Release date: | 2021-03-24 | | Last modified: | 2021-07-07 | | Method: | ELECTRON MICROSCOPY (5.3 Å) | | Cite: | Architecture and structural dynamics of the heteromeric GluK2/K5 kainate receptor.
Elife, 10, 2021
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7KS3
 | | GluK2/K5 with L-Glu | | Descriptor: | Glutamate receptor ionotropic, kainate 2, kainate 5,Green fluorescent protein chimera | | Authors: | Khanra, N, Brown, P.M.G.E, Perozzo, A.M, Bowie, D, Meyerson, J.R. | | Deposit date: | 2020-11-20 | | Release date: | 2021-03-24 | | Last modified: | 2021-07-07 | | Method: | ELECTRON MICROSCOPY (5.8 Å) | | Cite: | Architecture and structural dynamics of the heteromeric GluK2/K5 kainate receptor.
Elife, 10, 2021
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6FQI
 | | GluA2(flop) G724C ligand binding core dimer bound to L-Glutamate (Form B) at 2.91 Angstrom resolution | | Descriptor: | GLUTAMIC ACID, Glutamate receptor 2 | | Authors: | Coombs, I.D, Soto, D, Gold, M.G, Farrant, M.F, Cull-Candy, S.G. | | Deposit date: | 2018-02-14 | | Release date: | 2019-03-13 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.91001153 Å) | | Cite: | Homomeric GluA2(R) AMPA receptors can conduct when desensitized.
Nat Commun, 10, 2019
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6FQK
 | | GluA2(flop) S729C ligand binding core dimer bound to ZK200775 at 1.98 Angstrom resolution | | Descriptor: | Glutamate receptor 2,Glutamate receptor 2, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | | Authors: | Coombs, I.D, Soto, D, Gold, M.G, Farrant, M.F, Cull-Candy, S.G. | | Deposit date: | 2018-02-14 | | Release date: | 2019-03-13 | | Last modified: | 2019-10-02 | | Method: | X-RAY DIFFRACTION (1.98010445 Å) | | Cite: | Homomeric GluA2(R) AMPA receptors can conduct when desensitized.
Nat Commun, 10, 2019
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6FQJ
 | | GluA2(flop) G724C ligand binding core dimer bound to ZK200775 at 2.50 Angstrom resolution | | Descriptor: | Glutamate receptor 2,Glutamate receptor 2, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | | Authors: | Coombs, I.D, Soto, D, Gold, M.G, Farrant, M.F, Cull-Candy, S.G. | | Deposit date: | 2018-02-14 | | Release date: | 2019-03-13 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.500017 Å) | | Cite: | Homomeric GluA2(R) AMPA receptors can conduct when desensitized.
Nat Commun, 10, 2019
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6FQG
 | | GluA2(flop) G724C ligand binding core dimer bound to L-Glutamate (Form A) at 2.34 Angstrom resolution | | Descriptor: | GLUTAMIC ACID, Glutamate receptor 2 | | Authors: | Coombs, I.D, Soto, D, Gold, M.G, Farrant, M.F, Cull-Candy, S.G. | | Deposit date: | 2018-02-14 | | Release date: | 2019-03-13 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.34139085 Å) | | Cite: | X-ray structure of GluA2 flop G724C ligand binding core dimer bound to glutamate at 2.32 Angstroms resolution
To Be Published
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1S50
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6FZ4
 | | Structure of GluK1 ligand-binding domain in complex with N-(7-fluoro-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)-2-hydroxybenzamide at 1.85 A resolution | | Descriptor: | CHLORIDE ION, GLYCEROL, Glutamate receptor ionotropic, ... | | Authors: | Kastrup, J.S, Frydenvang, K, Mollerud, S. | | Deposit date: | 2018-03-14 | | Release date: | 2019-01-23 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | N1-Substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists: X-ray Crystallography, Structure-Affinity Relationships, and in Vitro Pharmacology.
Acs Chem Neurosci, 10, 2019
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