7NA8
 
 | | Structures of human ghrelin receptor-Gi complexes with ghrelin and a synthetic agonist | | Descriptor: | 1-(methanesulfonyl)-1'-(2-methyl-L-alanyl-O-benzyl-D-seryl)-1,2-dihydrospiro[indole-3,4'-piperidine], Antibody fragment, CHOLESTEROL, ... | | Authors: | Liu, H, Sun, D, Sun, J, Zhang, C. | | Deposit date: | 2021-06-20 | | Release date: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
Nat Commun, 12, 2021
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7NA7
 | | Structures of human ghrelin receptor-Gi complexes with ghrelin and a synthetic agonist | | Descriptor: | Antibody fragment, CHOLESTEROL, Ghrelin-27, ... | | Authors: | Liu, H, Sun, D, Sun, J, Zhang, C. | | Deposit date: | 2021-06-20 | | Release date: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
Nat Commun, 12, 2021
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7O7F
 | | Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist | | Descriptor: | C-C chemokine receptor type 5, C-C motif chemokine 5, Fab antibody fragment heavy chain, ... | | Authors: | Isaikina, P, Tsai, C.-J, Dietz, N.B, Pamula, F, Goldie, K.N, Schertler, G.F.X, Maier, T, Stahlberg, H, Deupi, X, Grzesiek, S. | | Deposit date: | 2021-04-13 | | Release date: | 2021-06-30 | | Last modified: | 2022-03-16 | | Method: | ELECTRON MICROSCOPY (3.15 Å) | | Cite: | Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist.
Sci Adv, 7, 2021
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7PIU
 | | Cryo-EM structure of the agonist setmelanotide bound to the active melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein at 2.6 A resolution. | | Descriptor: | CALCIUM ION, Camelid antibody fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P. | | Deposit date: | 2021-08-23 | | Release date: | 2021-11-17 | | Method: | ELECTRON MICROSCOPY (2.58 Å) | | Cite: | Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
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7PIV
 | | Active Melanocortin-4 receptor (MC4R)- Gs protein complex bound to agonist NDP-alpha-MSH at 2.86 A resolution. | | Descriptor: | CALCIUM ION, Camelid antibody VHH fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P. | | Deposit date: | 2021-08-23 | | Release date: | 2021-11-17 | | Method: | ELECTRON MICROSCOPY (2.86 Å) | | Cite: | Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
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5TDH
 | | The crystal structure of the dominant negative mutant G protein alpha(i)-1-beta-1-gamma-2 G203A/A326S | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Liu, P, Jia, M.-Z, Zhou, X.E, de Waal, P.W, Dickson, B.M, Liu, B, Hou, L, Yin, Y.-T, Kang, Y.-Y, Shi, Y, Melcher, K, Xu, H.E, Jiang, Y. | | Deposit date: | 2016-09-19 | | Release date: | 2016-11-09 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | The structural basis of the dominant negative phenotype of the G alpha i1 beta 1 gamma 2 G203A/A326S heterotrimer
Acta Pharmacol.Sin., 37, 2016
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5UKM
 | | bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as) | | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(1H-pyrazol-5-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cruz-Rodriguez, O, Tesmer, J.J.G. | | Deposit date: | 2017-01-23 | | Release date: | 2017-04-12 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.03 Å) | | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
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5UKK
 | | Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak) | | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(pyridin-2-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | | Deposit date: | 2017-01-23 | | Release date: | 2017-04-05 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
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5UZ7
 | | Volta phase plate cryo-electron microscopy structure of a calcitonin receptor-heterotrimeric Gs protein complex | | Descriptor: | Calcitonin receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Liang, Y.L, Khoshouei, M, Radjainia, M, Zhang, Y, Glukhova, A, Tarrasch, J, Thal, D.M, Furness, S.G.B, Christopoulos, G, Coudrat, T, Danev, R, Baumeister, W, Miller, L.J, Christopoulos, A, Kobilka, B.K, Wootten, D, Skiniotis, G, Sexton, P.M. | | Deposit date: | 2017-02-24 | | Release date: | 2017-05-03 | | Last modified: | 2018-07-18 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Phase-plate cryo-EM structure of a class B GPCR-G-protein complex.
Nature, 546, 2017
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5VAI
 | | Cryo-EM structure of the activated Glucagon-like peptide-1 receptor in complex with G protein | | Descriptor: | Glucagon-like peptide 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Zhang, Y, Sun, B, Feng, D, Hu, H, Chu, M, Qu, Q, Tarrasch, J.T, Li, S, Kobilka, T.S, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2017-03-27 | | Release date: | 2017-05-24 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein.
Nature, 546, 2017
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5UKL
 | | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | | Descriptor: | 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | | Deposit date: | 2017-01-23 | | Release date: | 2017-04-05 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
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5WG5
 | | Human GRK2 in complex with Gbetagamma subunits and CCG224061 | | Descriptor: | 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-2H-indazole, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Bouley, R, Tesmer, J.J.G. | | Deposit date: | 2017-07-13 | | Release date: | 2017-12-27 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
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5WG4
 | | Human GRK2 in complex with Gbetagamma subunits and CCG257284 | | Descriptor: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(pyridin-2-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Bouley, R, Tesmer, J.J.G. | | Deposit date: | 2017-07-13 | | Release date: | 2017-12-27 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.31 Å) | | Cite: | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
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5WG3
 | | Human GRK2 in complex with Gbetagamma subunits and CCG258748 | | Descriptor: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(1H-pyrazol-3-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Bouley, R, Tesmer, J.J.G. | | Deposit date: | 2017-07-13 | | Release date: | 2017-12-27 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.896 Å) | | Cite: | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
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6K41
 | | cryo-EM structure of alpha2BAR-GoA complex | | Descriptor: | 4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole, Alpha-2A adrenergic receptor,Endolysin,Alpha-2B adrenergic receptor,Alpha-2B adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Yuan, D, Liu, Z, Wang, H.W, Kobilka, B.K. | | Deposit date: | 2019-05-23 | | Release date: | 2020-04-15 | | Last modified: | 2020-05-13 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Activation of the alpha2Badrenoceptor by the sedative sympatholytic dexmedetomidine.
Nat.Chem.Biol., 16, 2020
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6K42
 | | cryo-EM structure of alpha2BAR-Gi1 complex | | Descriptor: | 4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole, Alpha-2A adrenergic receptor,Endolysin,Alpha-2B adrenergic receptor,Alpha-2B adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Yuan, D, Liu, Z, Wang, H.W, Kobilka, B.K. | | Deposit date: | 2019-05-23 | | Release date: | 2020-04-15 | | Last modified: | 2020-05-13 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Activation of the alpha2Badrenoceptor by the sedative sympatholytic dexmedetomidine.
Nat.Chem.Biol., 16, 2020
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6KPF
 | | Cryo-EM structure of a class A GPCR with G protein complex | | Descriptor: | 7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]- 7-methyloctanenitrile, Cannabinoid receptor 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, X.T, Hua, T, Wu, L.J, Makriyannis, A, Shen, L, Wang, Y.X, Liu, Z.J. | | Deposit date: | 2019-08-15 | | Release date: | 2020-02-12 | | Last modified: | 2022-04-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
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6KPG
 | | Cryo-EM structure of CB1-G protein complex | | Descriptor: | (6~{a}~{R},9~{R},10~{a}~{R})-9-(hydroxymethyl)-3-(8-isothiocyanato-2-methyl-octan-2-yl)-6,6-dimethyl-6~{a},7,8,9,10,10~{a}-hexahydrobenzo[c]chromen-1-ol, Cannabinoid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hua, T, Li, X.T, Wu, L.J, Makriyannis, A, Wang, Y.X, Shen, L, Liu, Z.J. | | Deposit date: | 2019-08-15 | | Release date: | 2020-02-12 | | Last modified: | 2020-03-11 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
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6LFM
 | | Cryo-EM structure of a class A GPCR | | Descriptor: | C-X-C chemokine receptor type 2, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, Z.J, Hua, T, Liu, K.W, Wu, L.J. | | Deposit date: | 2019-12-03 | | Release date: | 2020-09-02 | | Last modified: | 2020-09-16 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structural basis of CXC chemokine receptor 2 activation and signalling.
Nature, 585, 2020
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6LFO
 | | Cryo-EM structure of a class A GPCR monomer | | Descriptor: | C-X-C chemokine receptor type 2, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, Z.J, Hua, T, Liu, K.W, Wu, L.J. | | Deposit date: | 2019-12-03 | | Release date: | 2020-09-02 | | Last modified: | 2020-09-16 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural basis of CXC chemokine receptor 2 activation and signalling.
Nature, 585, 2020
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6LI3
 | | cryo-EM structure of GPR52-miniGs-NB35 | | Descriptor: | G-protein coupled receptor 52, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Li, M, Wang, N, Xu, F, Wu, J, Lei, M. | | Deposit date: | 2019-12-10 | | Release date: | 2020-02-26 | | Last modified: | 2020-03-18 | | Method: | ELECTRON MICROSCOPY (3.32 Å) | | Cite: | Structural basis of ligand recognition and self-activation of orphan GPR52.
Nature, 579, 2020
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6LML
 | | Cryo-EM structure of the human glucagon receptor in complex with Gi1 | | Descriptor: | Glucagon, Glucagon receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Qiao, A, Han, S, Li, X, Sun, F, Zhao, Q, Wu, B. | | Deposit date: | 2019-12-26 | | Release date: | 2020-04-01 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Structural basis of Gsand Girecognition by the human glucagon receptor.
Science, 367, 2020
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6LPB
 | | Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Kobayashi, K, Shihoya, W, Nishizawa, T, Nureki, O. | | Deposit date: | 2020-01-09 | | Release date: | 2020-03-11 | | Last modified: | 2020-03-25 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein.
Nat.Struct.Mol.Biol., 27, 2020
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6LMK
 | | Cryo-EM structure of the human glucagon receptor in complex with Gs | | Descriptor: | Glucagon, Glucagon receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Qiao, A, Han, S, Tai, L, Sun, F, Zhao, Q, Wu, B. | | Deposit date: | 2019-12-26 | | Release date: | 2020-04-01 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Structural basis of Gsand Girecognition by the human glucagon receptor.
Science, 367, 2020
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6M1H
 | | CryoEM structure of human PAC1 receptor in complex with maxadilan | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Song, X, Wang, J, Zhang, D, Wang, H.W, Ma, Y. | | Deposit date: | 2020-02-26 | | Release date: | 2020-03-11 | | Last modified: | 2020-05-27 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Cryo-EM structures of PAC1 receptor reveal ligand binding mechanism.
Cell Res., 30, 2020
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