3M3K
 
 | | Ligand binding domain (S1S2) of GluA3 (flop) | | 分子名称: | GLUTAMIC ACID, Glutamate receptor 3, ZINC ION | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2010-03-09 | | 公開日 | 2010-03-23 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (1.793 Å) | | 主引用文献 | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA.
Biochemistry, 49, 2010
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3M3L
 | | PEPA bound to the ligand binding domain of GluA2 (flop form) | | 分子名称: | 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | 登録日 | 2010-03-09 | | 公開日 | 2010-03-23 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA.
Biochemistry, 49, 2010
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3M3F
 | | PEPA bound to the ligand binding domain of GluA3 (flop form) | | 分子名称: | 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide, GLUTAMIC ACID, Glutamate receptor 3, ... | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2010-03-09 | | 公開日 | 2010-03-23 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Molecular mechanism of flop selectivity and subsite recognition for an AMPA receptor allosteric modulator: structures of GluA2 and GluA3 in complexes with PEPA.
Biochemistry, 49, 2010
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3RT6
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3RT8
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3RTW
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3T9V
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3RTF
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3T9X
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3T96
 | | Iodowillardiine bound to a double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2 | | 分子名称: | 2-AMINO-3-(5-IODO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, Glutamate receptor 2, ZINC ION | | 著者 | Ahmed, A.H, Wang, S, Chuang, H.H, Oswald, R.E. | | 登録日 | 2011-08-02 | | 公開日 | 2011-08-17 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.872 Å) | | 主引用文献 | Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
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3T9H
 | | Kainate bound to a double cysteine mutant (A452C/S652C) of the ligand binding domain of GluA2 | | 分子名称: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, Glutamate receptor 2, ZINC ION | | 著者 | Ahmed, A.H, Wang, S, Chuang, H.H, Oswald, R.E. | | 登録日 | 2011-08-02 | | 公開日 | 2011-08-17 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.015 Å) | | 主引用文献 | Mechanism of AMPA Receptor Activation by Partial Agonists: DISULFIDE TRAPPING OF CLOSED LOBE CONFORMATIONS.
J.Biol.Chem., 286, 2011
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3T93
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3T9U
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3H06
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3H03
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3IL1
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, IDRA-21 | | 分子名称: | (3S)-7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2009-08-06 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.998 Å) | | 主引用文献 | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3ILT
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, trichlormethiazide | | 分子名称: | 6-CHLORO-3-(DICHLOROMETHYL)-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE-7-SULFONAMIDE 1,1-DIOXIDE, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2009-08-07 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.107 Å) | | 主引用文献 | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IK6
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, chlorothiazide | | 分子名称: | 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | 登録日 | 2009-08-05 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.101 Å) | | 主引用文献 | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IJO
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, althiazide | | 分子名称: | (3S)-6-chloro-3-[(prop-2-en-1-ylsulfanyl)methyl]-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | 登録日 | 2009-08-04 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.003 Å) | | 主引用文献 | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3IJX
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, hydrochlorothiazide | | 分子名称: | 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ptak, C.P, Ahmed, A.H, Oswald, R.E. | | 登録日 | 2009-08-05 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.881 Å) | | 主引用文献 | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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3ILU
 | | Crystal structure of the AMPA subunit GluR2 bound to the allosteric modulator, hydroflumethiazide | | 分子名称: | 6-(trifluoromethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide, GLUTAMIC ACID, Glutamate receptor 2, ... | | 著者 | Ahmed, A.H, Ptak, C.P, Oswald, R.E. | | 登録日 | 2009-08-07 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.003 Å) | | 主引用文献 | Probing the allosteric modulator binding site of GluR2 with thiazide derivatives
Biochemistry, 48, 2009
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5O9A
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J-L504Y-N775S) in complex with glutamate and BPAM121 at 1.78 A resolution | | 分子名称: | 1,2-ETHANEDIOL, 7-chloro-4-(2-fluoroethyl)-2,3-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, CHLORIDE ION, ... | | 著者 | Laulumaa, S, Rovinskaja, K, Frydenvang, K.A, Kastrup, J.S. | | 登録日 | 2017-06-16 | | 公開日 | 2018-01-03 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.78 Å) | | 主引用文献 | 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
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5OEW
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with glutamate and positive allosteric modulator BPAM538 | | 分子名称: | 4-cyclopropyl-7-(3-methoxyphenoxy)-2,3-dihydro-1$l^{6},2,4-benzothiadiazine 1,1-dioxide, ACETATE ION, GLUTAMIC ACID, ... | | 著者 | Larsen, A.P, Frydenvang, K.A, Kastrup, J.S. | | 登録日 | 2017-07-10 | | 公開日 | 2018-01-03 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | 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
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2KB0
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5BUU
 | | Crystal structure of the GluA2 ligand-binding domain (L483Y-N754S) in complex with glutamate and BPAM-321 at 2.07 A resolution | | 分子名称: | (3R)-7-chloro-2,3,4-trimethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, 1,2-ETHANEDIOL, GLUTAMIC ACID, ... | | 著者 | Larsen, A.P, Tapken, D, Frydenvang, K, Kastrup, J.S. | | 登録日 | 2015-06-04 | | 公開日 | 2016-02-17 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.07 Å) | | 主引用文献 | Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.
Acs Chem Neurosci, 7, 2016
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