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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6DM1
 | | Open state GluA2 in complex with STZ and blocked by NASPM, after micelle signal subtraction | | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, ... | | Authors: | Twomey, E.C, Yelshanskaya, M.V, Vassilevski, A.A, Sobolevsky, A.I. | | Deposit date: | 2018-06-04 | | Release date: | 2018-08-22 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (4.2 Å) | | Cite: | Mechanisms of Channel Block in Calcium-Permeable AMPA Receptors.
Neuron, 99, 2018
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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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6YK4
 | | Structure of the AMPA receptor GluA2o ligand-binding domain (S1S2J) in complex with the compound ( S) - 1- [2'-Amino-2'-carboxyethyl]-6-methyl-5 ,7- dihydropyrrolo[3,4-d]pyrimidin-2,4(1H,3H)-dione at resolution 1.00A | | 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, GLYCEROL, ... | | Authors: | Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2020-04-05 | | Release date: | 2020-06-03 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (0.999 Å) | | Cite: | Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.
Acs Chem Neurosci, 11, 2020
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6FQH
 | | GluA2(flop) S729C ligand binding core dimer bound to NBQX at 1.76 Angstrom resolution | | Descriptor: | 6-nitro-2,3-bis(oxidanylidene)-1,4-dihydrobenzo[f]quinoxaline-7-sulfonamide, Glutamate receptor 2,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: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.75940013 Å) | | Cite: | Homomeric GluA2(R) AMPA receptors can conduct when desensitized.
Nat Commun, 10, 2019
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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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8PIV
 | | Homomeric GluA2 flip R/G-unedited Q/R-edited F231A mutant in tandem with TARP gamma-2, desensitized conformation 1 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, Glutamate receptor, ... | | Authors: | Zhang, D, Krieger, J.M, Yamashita, K, Greger, I.H. | | Deposit date: | 2023-06-22 | | Release date: | 2023-08-30 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3.46 Å) | | Cite: | Structural mobility tunes signalling of the GluA1 AMPA glutamate receptor.
Nature, 621, 2023
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6HCC
 | | STRUCTURE OF GLUA2 LIGAND-BINDING DOMAIN (S1S2J-N775S) IN COMPLEX WITH GLUTAMATE AND TDPAM02 AT 1.6 A RESOLUTION. | | Descriptor: | 6,6'-(ETHANE-1,2-DIYL)BIS(4-CYCLOPROPYL-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE 1,1-DIOXIDE), ACETATE ION, CHLORIDE ION, ... | | Authors: | Laulumaa, S, Hansen, K.V, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2018-08-14 | | Release date: | 2019-04-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.617 Å) | | Cite: | Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor.
Acs Med.Chem.Lett., 10, 2019
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6HC9
 | | STRUCTURE OF GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L504Y-N775S) IN COMPLEX WITH GLUTAMATE AND TDPAM02 AT 2.4 A RESOLUTION. | | Descriptor: | 6,6'-(ETHANE-1,2-DIYL)BIS(4-CYCLOPROPYL-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE 1,1-DIOXIDE), CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Laulumaa, S, Hansen, K.V, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2018-08-14 | | Release date: | 2019-04-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor.
Acs Med.Chem.Lett., 10, 2019
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6HCB
 | | STRUCTURE OF GLUA2 LIGAND-BINDING DOMAIN (S1S2J-N775S) IN COMPLEX WITH GLUTAMATE AND TDPAM01 AT 1.9 A RESOLUTION. | | Descriptor: | 6,6'-(Ethane-1,2-diyl)bis(4-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide), CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Laulumaa, S, Masternak, M, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2018-08-14 | | Release date: | 2019-04-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor.
Acs Med.Chem.Lett., 10, 2019
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6HCA
 | | STRUCTURE OF GLUA2 LIGAND-BINDING DOMAIN (S1S1J) IN COMPLEX WITH POSITIVE ALLOSTERIC MODULATOR TDPAM02 AT 1.8 A RESOLUTION | | Descriptor: | 6,6'-(ETHANE-1,2-DIYL)BIS(4-CYCLOPROPYL-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE 1,1-DIOXIDE), CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Laulumaa, S, Hansen, K.V, Frydenvang, K, Kastrup, J.S. | | Deposit date: | 2018-08-14 | | Release date: | 2019-04-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.882 Å) | | Cite: | Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor.
Acs Med.Chem.Lett., 10, 2019
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1P1U
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8QEZ
 | | 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 | | 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
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6IRG
 | | Structure of the human GluN1/GluN2A NMDA receptor in the glutamate/glycine-bound state at pH 6.3, Class II | | Descriptor: | Glutamate receptor ionotropic, NMDA 1, NMDA 2A | | Authors: | Zhang, J, Chang, S, Zhang, X, Zhu, S. | | Deposit date: | 2018-11-12 | | Release date: | 2019-01-16 | | Last modified: | 2019-06-05 | | Method: | ELECTRON MICROSCOPY (5.5 Å) | | Cite: | Structural Basis of the Proton Sensitivity of Human GluN1-GluN2A NMDA Receptors
Cell Rep, 25, 2018
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6IRA
 | | Structure of the human GluN1/GluN2A NMDA receptor in the glutamate/glycine-bound state at pH 7.8 | | Descriptor: | Glutamate receptor ionotropic, NMDA 1, NMDA 2A | | Authors: | Zhang, J, Chang, S, Zhang, X, Zhu, S. | | Deposit date: | 2018-11-12 | | Release date: | 2019-01-16 | | Last modified: | 2019-06-05 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Structural Basis of the Proton Sensitivity of Human GluN1-GluN2A NMDA Receptors
Cell Rep, 25, 2018
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8SS4
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunits TARP gamma-5 and cornichon-2 (apo state) | | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-5 subunit chimera, Protein cornichon homolog 2, ... | | Authors: | Yen, L.Y, Gangwar, S.P, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-11-01 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS8
 | | Structure of AMPA receptor GluA2 complex with auxiliary subunit TARP gamma-5 bound to competitive antagonist ZK and antiepileptic drug perampanel (closed state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, CHOLESTEROL, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-10-25 | | Method: | ELECTRON MICROSCOPY (2.81 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS5
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunit TARP gamma-5 (apo state) | | Descriptor: | Glutamate receptor 2, Voltage-dependent calcium channel gamma-5 subunit chimera, SODIUM ION | | Authors: | Yen, L.Y, Gangwar, S.P, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-10-25 | | Method: | ELECTRON MICROSCOPY (3.56 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SSA
 | | Structure of AMPA receptor GluA2 complex with auxiliary subunits TARP gamma-5 and cornichon-2 bound to glutamate and channel blocker spermidine (desensitized state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-11-01 | | Method: | ELECTRON MICROSCOPY (3.88 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SSB
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunits TARP gamma-5 and cornichon-2 bound to glutamate and channel blocker spermidine (desensitized state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, GLUTAMIC ACID, Glutamate receptor 2, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-10-25 | | Method: | ELECTRON MICROSCOPY (3.66 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS7
 | | Structure of AMPA receptor GluA2 complex with auxiliary subunits TARP gamma-5 and cornichon-2 bound to competitive antagonist ZK, channel blocker spermidine and antiepileptic drug perampanel (closed state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, CHOLESTEROL, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-11-01 | | Method: | ELECTRON MICROSCOPY (2.76 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS3
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunits TARP gamma-5 and cornichon-2 bound to competitive antagonist ZK and channel blocker spermidine (closed state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, CHOLESTEROL, Digitonin, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-11-01 | | Method: | ELECTRON MICROSCOPY (3.21 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS2
 | | Structure of AMPA receptor GluA2 complex with auxiliary subunits TARP gamma-5 and cornichon-2 bound to competitive antagonist ZK and channel blocker spermidine (closed state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, CHOLESTEROL, Digitonin, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-11-01 | | Method: | ELECTRON MICROSCOPY (3.58 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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8SS9
 | | Structure of LBD-TMD of AMPA receptor GluA2 in complex with auxiliary subunit TARP gamma-5 bound to competitive antagonist ZK and antiepileptic drug perampanel (closed state) | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, CHOLESTEROL, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-05-08 | | Release date: | 2023-09-06 | | Last modified: | 2023-10-25 | | Method: | ELECTRON MICROSCOPY (2.72 Å) | | Cite: | Modulation of GluA2-gamma 5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2.
Nat.Struct.Mol.Biol., 30, 2023
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