6B20
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![BU of 6b20 by Molmil](/molmil-images/mine/6b20) | Crystal structure of a complex between G protein beta gamma dimer and an inhibitory Nanobody regulator | Descriptor: | CHLORIDE ION, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(T) subunit gamma-T1, ... | Authors: | Gulati, S, Kiser, P.D, Palczewski, K. | Deposit date: | 2017-09-19 | Release date: | 2018-05-30 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.34 Å) | Cite: | Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor. Nat Commun, 9, 2018
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5WG3
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![BU of 5wg3 by Molmil](/molmil-images/mine/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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5WG4
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![BU of 5wg4 by Molmil](/molmil-images/mine/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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5WG5
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![BU of 5wg5 by Molmil](/molmil-images/mine/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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5VAI
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![BU of 5vai by Molmil](/molmil-images/mine/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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5UZ7
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![BU of 5uz7 by Molmil](/molmil-images/mine/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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5UKM
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![BU of 5ukm by Molmil](/molmil-images/mine/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
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![BU of 5ukk by Molmil](/molmil-images/mine/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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5UKL
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![BU of 5ukl by Molmil](/molmil-images/mine/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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5TDH
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![BU of 5tdh by Molmil](/molmil-images/mine/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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5KDO
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![BU of 5kdo by Molmil](/molmil-images/mine/5kdo) | Heterotrimeric complex of the 4 alanine insertion variant of the Gi alpha1 subunit and the Gbeta1-Ggamma1 | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(T) subunit gamma-T1, ... | Authors: | Kaya, A.I, Lokits, A.D, Gilbert, J, Iverson, T.M, Meiler, J, Hamm, H.E. | Deposit date: | 2016-06-08 | Release date: | 2016-08-03 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | A Conserved Hydrophobic Core in G alpha i1 Regulates G Protein Activation and Release from Activated Receptor. J.Biol.Chem., 291, 2016
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5HE0
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![BU of 5he0 by Molmil](/molmil-images/mine/5he0) | Bovine GRK2 in complex with Gbetagamma subunits and CCG215022 | Descriptor: | (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE3
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![BU of 5he3 by Molmil](/molmil-images/mine/5he3) | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | Descriptor: | (4~{S})-4-[3-[2-(2,6-dimethylphenyl)ethylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE1
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![BU of 5he1 by Molmil](/molmil-images/mine/5he1) | Human GRK2 in complex with Gbetagamma subunits and CCG224062 | Descriptor: | (4~{S})-4-[4-fluoranyl-3-(isoquinolin-1-ylmethylcarbamoyl)phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (3.15 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE2
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![BU of 5he2 by Molmil](/molmil-images/mine/5he2) | Bovine GRK2 in complex with Gbetagamma subunits and CCG224406 | Descriptor: | (4~{S})-4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.79 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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4PNK
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![BU of 4pnk by Molmil](/molmil-images/mine/4pnk) | G protein-coupled receptor kinase 2 in complex with GSK180736A | Descriptor: | (4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G. | Deposit date: | 2014-05-23 | Release date: | 2014-10-08 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors. Acs Chem.Biol., 10, 2015
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4MK0
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![BU of 4mk0 by Molmil](/molmil-images/mine/4mk0) | |
4KFM
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![BU of 4kfm by Molmil](/molmil-images/mine/4kfm) | |
3V5W
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![BU of 3v5w by Molmil](/molmil-images/mine/3v5w) | |
3UZS
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![BU of 3uzs by Molmil](/molmil-images/mine/3uzs) | |
3SN6
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![BU of 3sn6 by Molmil](/molmil-images/mine/3sn6) | Crystal structure of the beta2 adrenergic receptor-Gs protein complex | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid antibody VHH fragment, Endolysin,Beta-2 adrenergic receptor, ... | Authors: | Rasmussen, S.G.F, DeVree, B.T, Zou, Y, Kruse, A.C, Chung, K.Y, Kobilka, T.S, Thian, F.S, Chae, P.S, Pardon, E, Calinski, D, Mathiesen, J.M, Shah, S.T.A, Lyons, J.A, Caffrey, M, Gellman, S.H, Steyaert, J, Skiniotis, G, Weis, W.I, Sunahara, R.K, Kobilka, B.K. | Deposit date: | 2011-06-28 | Release date: | 2011-07-20 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Crystal structure of the beta2 adrenergic receptor-Gs protein complex Nature, 477, 2011
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3PVU
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![BU of 3pvu by Molmil](/molmil-images/mine/3pvu) | Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101) | Descriptor: | 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Thal, D.M, Tesmer, J.J. | Deposit date: | 2010-12-07 | Release date: | 2011-06-01 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.48 Å) | Cite: | Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol.Pharmacol., 80, 2011
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3PVW
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3PSC
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![BU of 3psc by Molmil](/molmil-images/mine/3psc) | Bovine GRK2 in complex with Gbetagamma subunits | Descriptor: | Beta-adrenergic receptor kinase 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: | Thal, D.M, Tesmer, J.J. | Deposit date: | 2010-12-01 | Release date: | 2011-06-01 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.67 Å) | Cite: | Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol.Pharmacol., 80, 2011
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3AH8
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![BU of 3ah8 by Molmil](/molmil-images/mine/3ah8) | Structure of heterotrimeric G protein Galpha-q beta gamma in complex with an inhibitor YM-254890 | 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: | Nishimura, A, Kitano, K, Takasaki, J, Taniguchi, M, Mizuno, N, Tago, K, Hakoshima, T, Itoh, H. | Deposit date: | 2010-04-20 | Release date: | 2010-07-21 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule. Proc.Natl.Acad.Sci.USA, 107, 2010
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