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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3LMK
 | | Ligand Binding Domain of Metabotropoc glutamate receptor mGluR5 complexed with glutamate | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, GLUTAMIC ACID, MAGNESIUM ION, ... | | Authors: | Dobrovetsky, E, Khutoreskaya, G, Seitova, A, Cossar, D, Edwards, A.M, Arrowsmith, C.H, Bountra, C, Weigelt, J, Bochkarev, A, Structural Genomics Consortium (SGC) | | Deposit date: | 2010-01-30 | | Release date: | 2010-02-16 | | Last modified: | 2021-10-13 | | Method: | X-RAY DIFFRACTION (2.44 Å) | | Cite: | Metabotropic Glutamate receptor mGluR5 complexed with glutamate
To be Published
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7P2L
 | | thermostabilised 7TM domain of human mGlu5 receptor bound to photoswitchable ligand alloswitch-1 | | Descriptor: | 2-chloranyl-~{N}-[2-methoxy-4-[(~{E})-pyridin-2-yldiazenyl]phenyl]benzamide, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5 | | Authors: | Huang, C.Y, Vinothkumar, K.R, Lebon, G. | | Deposit date: | 2021-07-06 | | Release date: | 2021-09-08 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.54 Å) | | Cite: | Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations.
Cell Rep, 36, 2021
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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 | | 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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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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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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8TAO
 | | Quis and CDPPB bound active mGlu5 | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide, Metabotropic glutamate receptor 5, ... | | Authors: | Krishna Kumar, K, Wang, H, Kobilka, B.K. | | Deposit date: | 2023-06-27 | | Release date: | 2023-10-11 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Stepwise activation of a metabotropic glutamate receptor.
Nature, 629, 2024
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8T8M
 | | Quis-bound intermediate mGlu5 | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, Metabotropic glutamate receptor 5, Nb43 | | Authors: | Krishna Kumar, K, Wang, H, Kobilka, B.K. | | Deposit date: | 2023-06-22 | | Release date: | 2023-10-11 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Stepwise activation of a metabotropic glutamate receptor.
Nature, 629, 2024
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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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6N4Y
 | | Metabotropic Glutamate Receptor 5 Extracellular Domain with Nb43 | | Descriptor: | 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, Metabotropic glutamate receptor 5, ... | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Chu, M, Weis, W.I, Mathiesen, J.M, Skiniotis, G, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.262 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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8T7H
 | | Quis-bound intermediate mGlu5 | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, Metabotropic glutamate receptor 5, Nanobody 43 | | Authors: | Krishna Kumar, K, Wang, H, Kobilka, B.K. | | Deposit date: | 2023-06-20 | | Release date: | 2023-10-11 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Stepwise activation of a metabotropic glutamate receptor.
Nature, 629, 2024
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8T6J
 | | CDPPB-bound inactive mGlu5 | | Descriptor: | 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide, Metabotropic glutamate receptor 5 | | Authors: | Krishna Kumar, K, Wang, H, Kobilka, B.K. | | Deposit date: | 2023-06-16 | | Release date: | 2023-10-11 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Stepwise activation of a metabotropic glutamate receptor.
Nature, 629, 2024
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6N50
 | | Metabotropic Glutamate Receptor 5 Extracellular Domain in Complex with Nb43 and L-quisqualic acid | | 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, Chu, M, Weis, W.I, Skiniotis, G, 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 (3.751 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
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7FD8
 | | Thermostabilised full length human mGluR5-5M bound with L-quisqualic acid | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Vinothkumar, K.R, Cannone, G, Lebon, G. | | Deposit date: | 2021-07-16 | | Release date: | 2021-09-08 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.8 Å) | | Cite: | Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations.
Cell Rep, 36, 2021
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7FD9
 | | Thermostabilised full length human mGluR5-5M with orthosteric antagonist, LY341495 | | Descriptor: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5 | | Authors: | Vinothkumar, K.R, Cannone, G, Lebon, G. | | Deposit date: | 2021-07-16 | | Release date: | 2021-09-08 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations.
Cell Rep, 36, 2021
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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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