4OO9
 
 | | Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator mavoglurant | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Mavoglurant, Metabotropic glutamate receptor 5, ... | | Authors: | 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. | | Deposit date: | 2014-01-31 | | Release date: | 2014-07-02 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.
Nature, 511, 2014
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4OR2
 | | Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator | | Descriptor: | (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, ... | | Authors: | 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) | | Deposit date: | 2014-02-10 | | Release date: | 2014-03-19 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator
Science, 344, 2014
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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) | | Descriptor: | 3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, OLEIC ACID | | Authors: | 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. | | Deposit date: | 2015-07-09 | | Release date: | 2015-08-12 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.603 Å) | | Cite: | 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 | | Descriptor: | 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, ... | | Authors: | 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. | | Deposit date: | 2015-07-09 | | Release date: | 2015-08-12 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.101 Å) | | Cite: | 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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6FFH
 | | Crystal Structure of mGluR5 in complex with Fenobam at 2.65 A | | Descriptor: | (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, ... | | Authors: | 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. | | Deposit date: | 2018-01-08 | | Release date: | 2018-03-07 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | 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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6FFI
 | | Crystal Structure of mGluR5 in complex with MMPEP at 2.2 A | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[2-(3-methoxyphenyl)ethynyl]-6-methyl-pyridine, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, ... | | Authors: | 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. | | Deposit date: | 2018-01-08 | | Release date: | 2018-03-07 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | 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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6N51
 | | Metabotropic Glutamate Receptor 5 bound to L-quisqualate and Nb43 | | Descriptor: | (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, ... | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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6N52
 | | Metabotropic Glutamate Receptor 5 Apo Form | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5 | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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6N4X
 | | Metabotropic Glutamate Receptor 5 Apo Form Ligand Binding Domain | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, MAGNESIUM ION, Metabotropic glutamate receptor 5 | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (4 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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6UO8
 | | Human metabotropic GABA(B) receptor bound to agonist SKF97541 and positive allosteric modulator GS39783 | | Descriptor: | (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, ... | | Authors: | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | Deposit date: | 2019-10-14 | | Release date: | 2020-06-10 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (3.63 Å) | | Cite: | 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 | | Descriptor: | (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, ... | | Authors: | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | Deposit date: | 2019-10-14 | | Release date: | 2020-06-10 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (4.8 Å) | | Cite: | 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 | | Descriptor: | 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, ... | | Authors: | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | Deposit date: | 2019-10-14 | | Release date: | 2020-06-10 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (6.3 Å) | | Cite: | Structural basis of the activation of a metabotropic GABA receptor.
Nature, 584, 2020
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6VJM
 | | Human metabotropic GABA(B) receptor in its apo state | | Descriptor: | 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, ... | | Authors: | Shaye, H, Han, G.W, Gati, C, Cherezov, V. | | Deposit date: | 2020-01-16 | | Release date: | 2020-06-10 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (3.97 Å) | | Cite: | Structural basis of the activation of a metabotropic GABA receptor.
Nature, 584, 2020
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6W2Y
 | | CryoEM Structure of GABAB1b Homodimer | | Descriptor: | (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, ... | | Authors: | Papasergi-Scott, M.M, Robertson, M.J, Skiniotis, G. | | Deposit date: | 2020-03-08 | | Release date: | 2020-07-01 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structures of metabotropic GABABreceptor.
Nature, 584, 2020
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6W2X
 | | CryoEM Structure of Inactive GABAB Heterodimer | | Descriptor: | (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, ... | | Authors: | Papasergi-Scott, M.M, Robertson, M.J, Skiniotis, G. | | Deposit date: | 2020-03-08 | | Release date: | 2020-07-01 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Structures of metabotropic GABABreceptor.
Nature, 584, 2020
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6WIV
 | | Structure of human GABA(B) receptor in an inactive state | | Descriptor: | (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, ... | | Authors: | 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. | | Deposit date: | 2020-04-10 | | Release date: | 2020-07-01 | | Last modified: | 2020-08-26 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Structure of human GABABreceptor in an inactive state.
Nature, 584, 2020
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7C7Q
 | | Cryo-EM structure of the baclofen/BHFF-bound human GABA(B) receptor in active state | | Descriptor: | (3S)-5,7-ditert-butyl-3-oxidanyl-3-(trifluoromethyl)-1-benzofuran-2-one, 2-acetamido-2-deoxy-beta-D-glucopyranose, Gamma-aminobutyric acid type B receptor subunit 1, ... | | Authors: | Mao, C, Shen, C, Li, C, Shen, D, Xu, C, Zhang, S, Zhou, R, Shen, Q, Chen, L, Jiang, Z, Liu, J, Zhang, Y. | | Deposit date: | 2020-05-26 | | Release date: | 2020-07-01 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Cryo-EM structures of inactive and active GABABreceptor.
Cell Res., 30, 2020
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7C7S
 | | Cryo-EM structure of the CGP54626-bound human GABA(B) receptor in inactive state. | | Descriptor: | (R)-(cyclohexylmethyl)[(2S)-3-{[(1S)-1-(3,4-dichlorophenyl)ethyl]amino}-2-hydroxypropyl]phosphinic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Gamma-aminobutyric acid type B receptor subunit 1, ... | | Authors: | Mao, C, Shen, C, Li, C, Shen, D, Xu, C, Zhang, S, Zhou, R, Shen, Q, Chen, L, Jiang, Z, Liu, J, Zhang, Y. | | Deposit date: | 2020-05-26 | | Release date: | 2020-07-01 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Cryo-EM structures of inactive and active GABABreceptor.
Cell Res., 30, 2020
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7CA3
 | | Cryo-EM structure of human GABA(B) receptor bound to the positive allosteric modulator rac-BHFF | | Descriptor: | (3S)-5,7-ditert-butyl-3-oxidanyl-3-(trifluoromethyl)-1-benzofuran-2-one, CHOLESTEROL, Gamma-aminobutyric acid type B receptor subunit 1, ... | | Authors: | Kim, Y, Jeong, E, Jeong, J, Kim, Y, Cho, Y. | | Deposit date: | 2020-06-08 | | Release date: | 2020-11-11 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Structural Basis for Activation of the Heterodimeric GABA B Receptor.
J.Mol.Biol., 432, 2020
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7CA5
 | | Cryo-EM structure of human GABA(B) receptor in apo state | | Descriptor: | Gamma-aminobutyric acid type B receptor subunit 1, Gamma-aminobutyric acid type B receptor subunit 2 | | Authors: | Kim, Y, Jeong, E, Jeong, J, Kim, Y, Cho, Y. | | Deposit date: | 2020-06-08 | | Release date: | 2020-11-11 | | Last modified: | 2024-03-27 | | Method: | ELECTRON MICROSCOPY (7.6 Å) | | Cite: | Structural Basis for Activation of the Heterodimeric GABA B Receptor.
J.Mol.Biol., 432, 2020
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7CUM
 | | Cryo-EM structure of human GABA(B) receptor bound to the antagonist CGP54626 | | Descriptor: | (R)-(cyclohexylmethyl)[(2S)-3-{[(1S)-1-(3,4-dichlorophenyl)ethyl]amino}-2-hydroxypropyl]phosphinic acid, CHOLESTEROL, Gamma-aminobutyric acid type B receptor subunit 1, ... | | Authors: | Kim, Y, Jeong, E, Jeong, J, Kim, Y, Cho, Y. | | Deposit date: | 2020-08-23 | | Release date: | 2020-11-11 | | Method: | ELECTRON MICROSCOPY (3.52 Å) | | Cite: | Structural Basis for Activation of the Heterodimeric GABA B Receptor.
J.Mol.Biol., 432, 2020
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7DGE
 | | intermediate state of class C GPCR | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, Metabotropic glutamate receptor 1, nanobody | | Authors: | Zhang, J.Y, Wu, L.J, Luo, F, Hua, T, Liu, Z.J. | | Deposit date: | 2020-11-11 | | Release date: | 2021-09-22 | | Method: | ELECTRON MICROSCOPY (3.65 Å) | | Cite: | Structural insights into the activation initiation of full-length mGlu1.
Protein Cell, 12, 2021
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7DGD
 | | apo state of class C GPCR | | Descriptor: | Metabotropic glutamate receptor 1 | | Authors: | Zhang, J.Y, Wu, L.J, Luo, F, Hua, T, Liu, Z.J. | | Deposit date: | 2020-11-11 | | Release date: | 2021-09-22 | | Method: | ELECTRON MICROSCOPY (3.96 Å) | | Cite: | Structural insights into the activation initiation of full-length mGlu1.
Protein Cell, 12, 2021
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7DTW
 | | Human Calcium-Sensing Receptor in the inactive close-close conformation | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Extracellular calcium-sensing receptor | | Authors: | Ling, S.L, Tian, C.L, Shi, P, Liu, S.L, Meng, X.Y, Liu, L, Sun, D.M, Shi, C.W. | | Deposit date: | 2021-01-06 | | Release date: | 2021-03-10 | | Last modified: | 2021-04-14 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Structural mechanism of cooperative activation of the human calcium-sensing receptor by Ca 2+ ions and L-tryptophan.
Cell Res., 31, 2021
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7DTU
 | | Human Calcium-Sensing Receptor bound with L-Trp | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Extracellular calcium-sensing receptor, ... | | Authors: | Ling, S.L, Tian, C.L, Shi, P, Liu, S.L, Meng, X.Y, Liu, L, Sun, D.M, Shi, C.W. | | Deposit date: | 2021-01-06 | | Release date: | 2021-03-10 | | Last modified: | 2021-04-14 | | Method: | ELECTRON MICROSCOPY (4.4 Å) | | Cite: | Structural mechanism of cooperative activation of the human calcium-sensing receptor by Ca 2+ ions and L-tryptophan.
Cell Res., 31, 2021
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