8IEI
 
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8IEQ
 | | Cryo-EM structure of G-protein free GPR156 | | 分子名称: | Probable G-protein coupled receptor 156, [(2R)-3-[(E)-hexadec-9-enoyl]oxy-2-octadecanoyloxy-propyl] 2-(trimethylazaniumyl)ethyl phosphate | | 著者 | Shin, J, Park, J, Cho, Y. | | 登録日 | 2023-02-15 | | 公開日 | 2024-02-14 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (2.73 Å) | | 主引用文献 | Constitutive activation mechanism of a class C GPCR.
Nat.Struct.Mol.Biol., 31, 2024
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8IEB
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8IEP
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7P2L
 | | thermostabilised 7TM domain of human mGlu5 receptor bound to photoswitchable ligand alloswitch-1 | | 分子名称: | 2-chloranyl-~{N}-[2-methoxy-4-[(~{E})-pyridin-2-yldiazenyl]phenyl]benzamide, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5 | | 著者 | Huang, C.Y, Vinothkumar, K.R, Lebon, G. | | 登録日 | 2021-07-06 | | 公開日 | 2021-09-08 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.54 Å) | | 主引用文献 | Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations.
Cell Rep, 36, 2021
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8D1B
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6N4X
 | | Metabotropic Glutamate Receptor 5 Apo Form Ligand Binding Domain | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, MAGNESIUM ION, Metabotropic glutamate receptor 5 | | 著者 | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | 登録日 | 2018-11-20 | | 公開日 | 2019-01-23 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (4 Å) | | 主引用文献 | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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6W2X
 | | CryoEM Structure of Inactive GABAB Heterodimer | | 分子名称: | (1S)-2-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-1-[(octadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Papasergi-Scott, M.M, Robertson, M.J, Skiniotis, G. | | 登録日 | 2020-03-08 | | 公開日 | 2020-07-01 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (3.6 Å) | | 主引用文献 | Structures of metabotropic GABABreceptor.
Nature, 584, 2020
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6FFH
 | | Crystal Structure of mGluR5 in complex with Fenobam at 2.65 A | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-(3-chlorophenyl)-3-(3-methyl-5-oxidanylidene-4~{H}-imidazol-2-yl)urea, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | | 著者 | Christopher, J.A, Orgovan, Z, Congreve, M, Dore, A.S, Errey, J.C, Marshall, F.H, Mason, J.S, Okrasa, K, Rucktooa, P, Serrano-Vega, M.J, Ferenczy, G.G, Keseru, G.M. | | 登録日 | 2018-01-08 | | 公開日 | 2018-03-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.65 Å) | | 主引用文献 | Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.
J.Med.Chem., 62, 2019
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6W2Y
 | | CryoEM Structure of GABAB1b Homodimer | | 分子名称: | (1S)-2-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-1-[(octadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Papasergi-Scott, M.M, Robertson, M.J, Skiniotis, G. | | 登録日 | 2020-03-08 | | 公開日 | 2020-07-01 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Structures of metabotropic GABABreceptor.
Nature, 584, 2020
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6VJM
 | | Human metabotropic GABA(B) receptor in its apo state | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-[alpha-L-fucopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | 登録日 | 2020-01-16 | | 公開日 | 2020-06-10 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (3.97 Å) | | 主引用文献 | Structural basis of the activation of a metabotropic GABA receptor.
Nature, 584, 2020
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6FFI
 | | Crystal Structure of mGluR5 in complex with MMPEP at 2.2 A | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[2-(3-methoxyphenyl)ethynyl]-6-methyl-pyridine, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, ... | | 著者 | Christopher, J.A, Orgovan, Z, Congreve, M, Dore, A.S, Errey, J.C, Marshall, F.H, Mason, J.S, Okrasa, K, Rucktooa, P, Serrano-Vega, M.J, Ferenczy, G.G, Keseru, G.M. | | 登録日 | 2018-01-08 | | 公開日 | 2018-03-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.
J.Med.Chem., 62, 2019
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4OO9
 | | Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator mavoglurant | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Mavoglurant, Metabotropic glutamate receptor 5, ... | | 著者 | Dore, A.S, Okrasa, K, Patel, J.C, Serrano-Vega, M, Bennett, K, Cooke, R.M, Errey, J.C, Jazayeri, A, Khan, S, Tehan, B, Weir, M, Wiggin, G.R, Marshall, F.H. | | 登録日 | 2014-01-31 | | 公開日 | 2014-07-02 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.
Nature, 511, 2014
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6N51
 | | Metabotropic Glutamate Receptor 5 bound to L-quisqualate and Nb43 | | 分子名称: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5, ... | | 著者 | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | 登録日 | 2018-11-20 | | 公開日 | 2019-01-23 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (4 Å) | | 主引用文献 | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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6N52
 | | Metabotropic Glutamate Receptor 5 Apo Form | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5 | | 著者 | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | 登録日 | 2018-11-20 | | 公開日 | 2019-01-23 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (4 Å) | | 主引用文献 | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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5CGD
 | | Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator 3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile - (HTL14242) | | 分子名称: | 3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, OLEIC ACID | | 著者 | Christopher, J.A, Aves, S.J, Bennett, K.A, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Okrasa, K, Serrano-Vega, M.J, Tehan, B.G, Wiggin, G.R, Congreve, M. | | 登録日 | 2015-07-09 | | 公開日 | 2015-08-12 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.603 Å) | | 主引用文献 | Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
J.Med.Chem., 58, 2015
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5CGC
 | | Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator 3-chloro-4-fluoro-5-[6-(1H-pyrazol-1-yl)pyrimidin-4-yl]benzonitrile | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-chloro-4-fluoro-5-[6-(1H-pyrazol-1-yl)pyrimidin-4-yl]benzonitrile, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, ... | | 著者 | Christopher, J.A, Aves, S.J, Bennett, K.A, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Okrasa, K, Serrano-Vega, M.J, Tehan, B.G, Wiggin, G.R, Congreve, M. | | 登録日 | 2015-07-09 | | 公開日 | 2015-08-12 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.101 Å) | | 主引用文献 | Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
J.Med.Chem., 58, 2015
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4OR2
 | | Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 4-fluoro-N-methyl-N-{4-[6-(propan-2-ylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl}benzamide, CHOLESTEROL, ... | | 著者 | Wu, H, Wang, C, Gregory, K.J, Han, G.W, Cho, H.P, Xia, Y, Niswender, C.M, Katritch, V, Cherezov, V, Conn, P.J, Stevens, R.C, GPCR Network (GPCR) | | 登録日 | 2014-02-10 | | 公開日 | 2014-03-19 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator
Science, 344, 2014
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6WIV
 | | Structure of human GABA(B) receptor in an inactive state | | 分子名称: | (2R)-3-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-{[(9Z)-octadec-9-enoyl]oxy}propyl (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | 著者 | Park, J, Fu, Z, Frangaj, A, Liu, J, Mosyak, L, Shen, T, Slavkovich, V.N, Ray, K.M, Taura, J, Cao, B, Geng, Y, Zuo, H, Kou, Y, Grassucci, R, Chen, S, Liu, Z, Lin, X, Williams, J.P, Rice, W.J, Eng, E.T, Huang, R.K, Soni, R.K, Kloss, B, Yu, Z, Javitch, J.A, Hendrickson, W.A, Slesinger, P.A, Quick, M, Graziano, J, Yu, H, Fiehn, O, Clarke, O.B, Frank, J, Fan, Q.R. | | 登録日 | 2020-04-10 | | 公開日 | 2020-07-01 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Structure of human GABABreceptor in an inactive state.
Nature, 584, 2020
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7WI6
 | | Cryo-EM structure of LY341495/NAM-bound mGlu3 | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 3 | | 著者 | Fang, W, Yang, F, Xu, C.J, Ling, S.L, Lin, L, Zhou, Y.X, Sun, W.J, Wang, X.M, Liu, P, Rondard, P, Pan, S, Pin, J.P, Tian, C.L, Liu, J.F. | | 登録日 | 2022-01-03 | | 公開日 | 2022-03-16 | | 最終更新日 | 2022-07-20 | | 実験手法 | ELECTRON MICROSCOPY (3.71 Å) | | 主引用文献 | Structural basis of the activation of metabotropic glutamate receptor 3.
Cell Res., 32, 2022
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7WIH
 | | Cryo-EM structure of LY2794193-bound mGlu3 | | 分子名称: | (1S,2S,4S,5R,6S)-2-amino-4-[(3-methoxybenzene-1-carbonyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 3 | | 著者 | Fang, W, Yang, F, Xu, C.J, Ling, S.L, Lin, L, Zhou, Y.X, Sun, W.J, Wang, X.M, Liu, P, Rondard, P, Pan, S, Pin, J.P, Tian, C.L, Liu, J.F. | | 登録日 | 2022-01-03 | | 公開日 | 2022-03-16 | | 最終更新日 | 2022-07-20 | | 実験手法 | ELECTRON MICROSCOPY (3.68 Å) | | 主引用文献 | Structural basis of the activation of metabotropic glutamate receptor 3.
Cell Res., 32, 2022
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7WI8
 | | Cryo-EM structure of inactive mGlu3 bound to LY341495 | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 3 | | 著者 | Fang, W, Yang, F, Xu, C.J, Ling, S.L, Lin, L, Zhou, Y.X, Sun, W.J, Wang, X.M, Liu, P, Rondard, P, Pan, S, Pin, J.P, Tian, C.L, Liu, J.F. | | 登録日 | 2022-01-03 | | 公開日 | 2022-03-16 | | 最終更新日 | 2022-07-20 | | 実験手法 | ELECTRON MICROSCOPY (4.17 Å) | | 主引用文献 | Structural basis of the activation of metabotropic glutamate receptor 3.
Cell Res., 32, 2022
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6UO8
 | | Human metabotropic GABA(B) receptor bound to agonist SKF97541 and positive allosteric modulator GS39783 | | 分子名称: | (R)-(3-aminopropyl)methylphosphinic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | 登録日 | 2019-10-14 | | 公開日 | 2020-06-10 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (3.63 Å) | | 主引用文献 | Structural basis of the activation of a metabotropic GABA receptor.
Nature, 584, 2020
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6UO9
 | | Human metabotropic GABA(B) receptor bound to agonist SKF97541 in its intermediate state 2 | | 分子名称: | (R)-(3-aminopropyl)methylphosphinic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | 登録日 | 2019-10-14 | | 公開日 | 2020-06-10 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (4.8 Å) | | 主引用文献 | Structural basis of the activation of a metabotropic GABA receptor.
Nature, 584, 2020
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6UOA
 | | Human metabotropic GABA(B) receptor in its intermediate state 1 | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Gamma-aminobutyric acid type B receptor subunit 1, ... | | 著者 | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | 登録日 | 2019-10-14 | | 公開日 | 2020-06-10 | | 最終更新日 | 2020-08-26 | | 実験手法 | ELECTRON MICROSCOPY (6.3 Å) | | 主引用文献 | Structural basis of the activation of a metabotropic GABA receptor.
Nature, 584, 2020
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