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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1OMW
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![BU of 1omw by Molmil](/molmil-images/mine/1omw) | Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits | Descriptor: | G-protein coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1 | Authors: | Lodowski, D.T, Pitcher, J.A, Capel, W.D, Lefkowitz, R.J, Tesmer, J.J.G. | Deposit date: | 2003-02-26 | Release date: | 2003-06-03 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Keeping G proteins at Bay: A Complex Between G Protein-Coupled Receptor Kinase 2 and G-Beta-Gamma Science, 300, 2003
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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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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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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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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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8JPD
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![BU of 8jpd by Molmil](/molmil-images/mine/8jpd) | Focused refinement structure of GRK2 in NTSR1-GRK2-Galpha(q) complexes | Descriptor: | Beta-adrenergic receptor kinase 1, STAUROSPORINE | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | Deposit date: | 2023-06-11 | Release date: | 2023-08-09 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (2.81 Å) | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist. Nature, 620, 2023
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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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2BCJ
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8JPC
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![BU of 8jpc by Molmil](/molmil-images/mine/8jpc) | cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 2 | Descriptor: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, Beta-adrenergic receptor kinase 1, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | Deposit date: | 2023-06-11 | Release date: | 2023-08-09 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (3.07 Å) | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist. Nature, 620, 2023
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8JPB
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![BU of 8jpb by Molmil](/molmil-images/mine/8jpb) | cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 1 | Descriptor: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, Beta-adrenergic receptor kinase 1, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | Deposit date: | 2023-06-11 | Release date: | 2023-08-09 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (3.07 Å) | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist. Nature, 620, 2023
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3UZT
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![BU of 3uzt by Molmil](/molmil-images/mine/3uzt) | |
1YM7
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![BU of 1ym7 by Molmil](/molmil-images/mine/1ym7) | G Protein-Coupled Receptor Kinase 2 (GRK2) | Descriptor: | Beta-adrenergic receptor kinase 1 | Authors: | Lodowski, D.T, Barnhill, J.F, Pyskadlo, R.M, Ghirlando, R, Sterne-Marr, R, Tesmer, J.J.G. | Deposit date: | 2005-01-20 | Release date: | 2005-07-05 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (4.5 Å) | Cite: | The role of Gbetagamma and domain interfaces in the activation of G protein-coupled receptor kinase 2 Biochemistry, 44, 2005
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3UZS
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![BU of 3uzs by Molmil](/molmil-images/mine/3uzs) | |