5IOV
 
 | | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the glutamate/glycine/Ro25-6981-bound conformation | | Descriptor: | 4-[(1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol, GLUTAMIC ACID, GLYCINE, ... | | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, Mchaourab, S.H, Gouaux, E. | | Deposit date: | 2016-03-09 | | Release date: | 2016-04-20 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (7.5 Å) | | Cite: | Mechanism of NMDA Receptor Inhibition and Activation.
Cell, 165, 2016
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5IPV
 | | Cryo-EM structure of GluN1/GluN2B NMDA receptor in the DCKA/D-APV-bound conformation, state 1 | | Descriptor: | Ionotropic glutamate receptor subunit NR2B, N-methyl-D-aspartate receptor subunit NR1-8a | | Authors: | Zhu, S, Stein, A.R, Yoshioka, C, Lee, C.H, Goehring, A, McHaourab, S.H, Gouaux, E. | | Deposit date: | 2016-03-10 | | Release date: | 2016-04-20 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (9.25 Å) | | Cite: | Mechanism of NMDA Receptor Inhibition and Activation.
Cell, 165, 2016
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5I2N
 | | Structure of the human GluN1/GluN2A LBD in complex with N-ethyl-7-{[2-fluoro-3-(trifluoromethyl)phenyl]methyl}-2-methyl-5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidine-3-carboxamide (compound 29) | | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CALCIUM ION, GLUTAMIC ACID, ... | | Authors: | Wallweber, H.J.A, Lupardus, P.J. | | Deposit date: | 2016-02-09 | | Release date: | 2016-03-16 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.12 Å) | | Cite: | Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
J.Med.Chem., 59, 2016
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5JEI
 | | Crystal structure of the GluA2 LBD in complex with FW | | Descriptor: | 1,2-ETHANEDIOL, 2-(2-METHOXYETHOXY)ETHANOL, 2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, ... | | Authors: | Eibl, C, Salazar, H, Chebli, M, Plested, A.J.R. | | Deposit date: | 2016-04-18 | | Release date: | 2017-02-22 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.229 Å) | | Cite: | Mechanism of partial agonism in AMPA-type glutamate receptors.
Nat Commun, 8, 2017
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5H8Q
 | | Structure of the human GluN1/GluN2A LBD in complex with GNE8324 | | Descriptor: | 6-[[ethyl-(4-fluorophenyl)amino]methyl]-2,3-dihydro-1~{H}-cyclopenta[3,4][1,3]thiazolo[1,4-~{a}]pyrimidin-8-one, ACETATE ION, GLUTAMIC ACID, ... | | Authors: | Wallweber, H.J.A, Lupardus, P.J. | | Deposit date: | 2015-12-23 | | Release date: | 2016-02-24 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function.
Neuron, 89, 2016
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5JTY
 | | Glutamate- and DCKA-bound GluN1/GluN2A agonist binding domains with MPX-007 | | Descriptor: | 4-hydroxy-5,7-dimethylquinoline-2-carboxylic acid, 5-({[(3,4-difluorophenyl)sulfonyl]amino}methyl)-6-methyl-N-[(2-methyl-1,3-thiazol-5-yl)methyl]pyrazine-2-carboxamide, GLUTAMIC ACID, ... | | Authors: | Mou, T.-C, Sprang, S.R, Hansen, K.B. | | Deposit date: | 2016-05-10 | | Release date: | 2016-09-21 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.72 Å) | | Cite: | Structural Basis for Negative Allosteric Modulation of GluN2A-Containing NMDA Receptors.
Neuron, 91, 2016
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5KBS
 | | Cryo-EM structure of GluA2-0xSTZ at 8.7 Angstrom resolution | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2,Voltage-dependent calcium channel gamma-2 subunit, {[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: | 2016-06-03 | | Release date: | 2016-07-13 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (8.7 Å) | | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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5KDT
 | | Structure of the human GluN1/GluN2A LBD in complex with GNE0723 | | Descriptor: | (1~{R},2~{R})-2-[7-[[5-chloranyl-3-(trifluoromethyl)pyrazol-1-yl]methyl]-5-oxidanylidene-2-(trifluoromethyl)-[1,3]thiazolo[3,2-a]pyrimidin-3-yl]cyclopropane-1-carbonitrile, ACETATE ION, GLUTAMIC ACID, ... | | Authors: | Wallweber, H.J.A, Lupardus, P.J. | | Deposit date: | 2016-06-08 | | Release date: | 2016-07-13 | | Method: | X-RAY DIFFRACTION (2.44 Å) | | Cite: | Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
J. Med. Chem., 59, 2016
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5KBV
 | | Cryo-EM structure of GluA2 bound to antagonist ZK200775 at 6.8 Angstrom resolution | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor 2, {[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.G, Frank, J, Sobolevsky, A.I. | | Deposit date: | 2016-06-03 | | Release date: | 2016-07-13 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (6.8 Å) | | Cite: | Elucidation of AMPA receptor-stargazin complexes by cryo-electron microscopy.
Science, 353, 2016
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8F0O
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8FWS
 | | Structure of the ligand-binding and transmembrane domains of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.23 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FWQ
 | | Structure of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 4-cyclopropyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.96 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FWW
 | | Structure of the ligand-binding and transmembrane domains of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 and noncompetitive inhibitor perampanel | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FWT
 | | Structure of the amino terminal domain of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 and competitive antagonist DNQX | | 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: | Yen, L.Y, Gangwar, S.P, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.09 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FWR
 | | Structure of the amino-terminal domain of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Glutamate receptor ionotropic, kainate 2, ... | | Authors: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FWV
 | | Structure of the amino-terminal domain of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 and noncompetitive inhibitor perampanel | | 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: | Gangwar, S.P, Yen, L.Y, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.03 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FWU
 | | Structure of the ligand-binding and transmembrane domains of kainate receptor GluK2 in complex with the positive allosteric modulator BPAM344 and competitive antagonist DNQX | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Yen, L.Y, Gangwar, S.P, Yelshanskaya, M.V, Sobolevsky, A.I. | | Deposit date: | 2023-01-23 | | Release date: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (3.18 Å) | | Cite: | Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.
Cell Rep, 42, 2023
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8FPC
 | | Conformation 1 of the ligand binding domain (LBDconf1) of GluA2 flip Q isoform of AMPA receptor in complex with gain-of-function TARP gamma-2, with 10mM CaCl2, 150mM NaCl, 1mM MgCl2, 330uM CTZ, and 100mM glutamate (Open-CaNaMg) | | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2 | | Authors: | Nakagawa, T. | | Deposit date: | 2023-01-04 | | Release date: | 2024-02-28 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (2.78 Å) | | Cite: | The open gate of the AMPA receptor forms a Ca 2+ binding site critical in regulating ion transport.
Nat.Struct.Mol.Biol., 31, 2024
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8FP4
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8FPH
 | | Conformation 2 of the ligand binding domain (LBDconf2) of GluA2 flip Q isoform of AMPA receptor in complex with gain-of-function TARP gamma-2, with 10mM CaCl2, 150mM NaCl, 1mM MgCl2, 330uM CTZ, and 100mM glutamate (Open-CaNaMg) | | Descriptor: | CYCLOTHIAZIDE, GLUTAMIC ACID, Glutamate receptor 2 | | Authors: | Nakagawa, T. | | Deposit date: | 2023-01-04 | | Release date: | 2024-02-28 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (3.14 Å) | | Cite: | The open gate of the AMPA receptor forms a Ca 2+ binding site critical in regulating ion transport.
Nat.Struct.Mol.Biol., 31, 2024
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8FQ5
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8FQ8
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8FP9
 | | GluA2 flip Q isoform of AMPA receptor in complex with gain-of-function TARP gamma-2, with 10mM CaCl2, 150mM NaCl, 1mM MgCl2, 330uM CTZ, and 100mM glutamate (Open-CaNaMg) | | Descriptor: | CALCIUM ION, CHLORIDE ION, Glutamate receptor 2, ... | | Authors: | Nakagawa, T. | | Deposit date: | 2023-01-04 | | Release date: | 2024-02-28 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (2.44 Å) | | Cite: | The open gate of the AMPA receptor forms a Ca 2+ binding site critical in regulating ion transport.
Nat.Struct.Mol.Biol., 31, 2024
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8FQE
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8FPL
 | | LBD conformation 2 (LBDconf2) of GluA2 flip Q isoform of AMPA receptor in complex with gain-of-function TARP gamma-2, with 10mM CaCl2, 150mM NaCl, 1mM MgCl2, 330uM CTZ, and 100uM CNQX (Closed-CaNaMg) | | Descriptor: | 6-(aminomethyl)-7-nitro-1,4-dihydroquinoxaline-2,3-dione, CYCLOTHIAZIDE, Glutamate receptor 2 | | Authors: | Nakagawa, T. | | Deposit date: | 2023-01-04 | | Release date: | 2024-02-28 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (2.81 Å) | | Cite: | The open gate of the AMPA receptor forms a Ca 2+ binding site critical in regulating ion transport.
Nat.Struct.Mol.Biol., 31, 2024
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