6GL4
| Structure of GluA2o ligand-binding domain (S1S2J) in complex with glutamate and sodium bromide at 1.95 A resolution | Descriptor: | ACETATE ION, BROMIDE ION, GLUTAMIC ACID, ... | Authors: | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | Deposit date: | 2018-05-22 | Release date: | 2019-05-15 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (1.948 Å) | Cite: | Nanoscale Mobility of the Apo State and TARP Stoichiometry Dictate the Gating Behavior of Alternatively Spliced AMPA Receptors. Neuron, 102, 2019
|
|
6GIV
| Structure of GluA2-N775S ligand-binding domain (S1S2J) in complex with glutamate and Rubidium Bromide at 1.75 A resolution | Descriptor: | BROMIDE ION, GLUTAMIC ACID, GLYCEROL, ... | Authors: | Venskutonyte, R, Frydenvang, K, Kastrup, J.S. | Deposit date: | 2018-05-15 | Release date: | 2019-05-15 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Nanoscale Mobility of the Apo State and TARP Stoichiometry Dictate the Gating Behavior of Alternatively Spliced AMPA Receptors. Neuron, 102, 2019
|
|
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
|
|
5ZG3
| Crystal structure of the GluA2o LBD in complex with glutamate and TAK-137 | Descriptor: | 9-(4-phenoxyphenyl)-3,4-dihydro-2H-2lambda~6~-pyrido[2,1-c][1,2,4]thiadiazine-2,2-dione, ACETATE ION, GLUTAMIC ACID, ... | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | Deposit date: | 2018-03-07 | Release date: | 2019-01-16 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.65 Å) | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window. Neuropsychopharmacology, 44, 2019
|
|
6CNA
| GluN1-GluN2B NMDA receptors with exon 5 | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor ionotropic, ... | Authors: | Furukawa, H, Grant, T, Grigorieff, N. | Deposit date: | 2018-03-07 | Release date: | 2018-10-03 | Last modified: | 2020-07-29 | Method: | ELECTRON MICROSCOPY (4.6 Å) | Cite: | Structural Mechanism of Functional Modulation by Gene Splicing in NMDA Receptors. Neuron, 98, 2018
|
|
5ZG1
| Crystal structure of the GluA2o LBD in complex with glutamate and Compound-2 | Descriptor: | 9-(4-~{tert}-butylphenyl)-3,4-dihydropyrido[2,1-c][1,2,4]thiadiazine 2,2-dioxide, GLUTAMIC ACID, GLYCEROL, ... | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | Deposit date: | 2018-03-07 | Release date: | 2019-01-16 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.32 Å) | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window. Neuropsychopharmacology, 44, 2019
|
|
5ZG2
| Crystal structure of the GluA2o LBD in complex with ZK200775 and Compound-2 | Descriptor: | 9-(4-~{tert}-butylphenyl)-3,4-dihydropyrido[2,1-c][1,2,4]thiadiazine 2,2-dioxide, ACETATE ION, GLYCEROL, ... | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | Deposit date: | 2018-03-07 | Release date: | 2019-01-16 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.25 Å) | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window. Neuropsychopharmacology, 44, 2019
|
|
5ZG0
| Crystal structure of the GluA2o LBD in complex with glutamate and Compound-1 | Descriptor: | 9-{4-[(propan-2-yl)oxy]phenyl}-3,4-dihydro-2H-2lambda~6~-pyrido[2,1-c][1,2,4]thiadiazine-2,2-dione, ACETATE ION, GLUTAMIC ACID, ... | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | Deposit date: | 2018-03-07 | Release date: | 2019-01-16 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.58 Å) | Cite: | TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window. Neuropsychopharmacology, 44, 2019
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
5YBF
| Crystal structure of the GluA2o LBD in complex with glutamate and HBT1 | Descriptor: | 2-[2-[5-methyl-3-(trifluoromethyl)pyrazol-1-yl]ethanoylamino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, ACETATE ION, GLUTAMIC ACID, ... | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | Deposit date: | 2017-09-04 | Release date: | 2018-01-17 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | HBT1, a Novel AMPA Receptor Potentiator with Lower Agonistic Effect, Avoided Bell-Shaped Response in In Vitro BDNF Production. J. Pharmacol. Exp. Ther., 364, 2018
|
|
5YBG
| Crystal structure of the GluA2o LBD in complex with glutamate and LY451395 | Descriptor: | ACETATE ION, GLUTAMIC ACID, GLYCEROL, ... | Authors: | Sogabe, S, Igaki, S, Hirokawa, A, Zama, Y, Lane, W, Snell, G. | Deposit date: | 2017-09-04 | Release date: | 2018-01-17 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.52 Å) | Cite: | HBT1, a Novel AMPA Receptor Potentiator with Lower Agonistic Effect, Avoided Bell-Shaped Response in In Vitro BDNF Production. J. Pharmacol. Exp. Ther., 364, 2018
|
|
5WEN
| GluA2 bound to GSG1L in digitonin, state 2 | Descriptor: | Digitonin, Glutamate receptor 2,Germ cell-specific gene 1-like protein | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (6.8 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
|
|
5OEW
| Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with glutamate and positive allosteric modulator BPAM538 | Descriptor: | 4-cyclopropyl-7-(3-methoxyphenoxy)-2,3-dihydro-1$l^{6},2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, GLUTAMIC ACID, ... | Authors: | Larsen, A.P, Frydenvang, K.A, Kastrup, J.S. | Deposit date: | 2017-07-10 | Release date: | 2018-01-03 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency. J. Med. Chem., 61, 2018
|
|
5WEK
| GluA2 bound to antagonist ZK and GSG1L in digitonin, state 1 | Descriptor: | Chimera of Glutamate receptor 2,Germ cell-specific gene 1-like protein, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2019-11-20 | Method: | ELECTRON MICROSCOPY (4.6 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
|
|
5WEM
| GluA2 bound to GSG1L in digitonin, state 1 | Descriptor: | Chimera of Glutamate receptor 2,Germ cell-specific gene 1-like protein | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2019-11-20 | Method: | ELECTRON MICROSCOPY (6.1 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
|
|
5WEO
| Activated GluA2 complex bound to glutamate, cyclothiazide, and STZ in digitonin | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit chimera | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2019-11-20 | Method: | ELECTRON MICROSCOPY (4.2 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
|
|
5WEL
| GluA2 bound to antagonist ZK and GSG1L in digitonin, state 2 | Descriptor: | Chimera of Glutamate receptor 2, Germ cell-specific gene 1-like protein, Digitonin, ... | Authors: | Twomey, E.C, Yelshanskaya, M.V, Grassucci, R.A, Frank, J, Sobolevsky, A.I. | Deposit date: | 2017-07-10 | Release date: | 2017-08-02 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (4.4 Å) | Cite: | Channel opening and gating mechanism in AMPA-subtype glutamate receptors. Nature, 549, 2017
|
|
5O9A
| Crystal structure of the GluA2 ligand-binding domain (S1S2J-L504Y-N775S) in complex with glutamate and BPAM121 at 1.78 A resolution | Descriptor: | 1,2-ETHANEDIOL, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ... | Authors: | Laulumaa, S, Rovinskaja, K, Frydenvang, K.A, Kastrup, J.S. | Deposit date: | 2017-06-16 | Release date: | 2018-01-03 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (1.78 Å) | Cite: | 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency. J. Med. Chem., 61, 2018
|
|