3KRW
| Human GRK2 in complex with Gbetgamma subunits and balanol (soak) | Descriptor: | BALANOL, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Tesmer, J.J.G, Tesmer, V.M. | Deposit date: | 2009-11-19 | Release date: | 2010-02-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol. J.Med.Chem., 53, 2010
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3KRX
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4EKD
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4EKC
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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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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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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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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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4MK0
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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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7SHF
| Cryo-EM structure of GPR158 coupled to the RGS7-Gbeta5 complex | Descriptor: | (2S)-1-{[(S)-hydroxy{[(1s,2R,3R,4R,5S,6S)-2,3,4,5,6-pentahydroxycyclohexyl]oxy}phosphoryl]oxy}-3-(octadecanoyloxy)propan-2-yl (5E,8E,11E,14E)-icosa-5,8,11,14-tetraenoate, 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine, CHOLESTEROL, ... | Authors: | Patil, D.N, Singh, S, Singh, A.K, Martemyanov, K.A. | Deposit date: | 2021-10-08 | Release date: | 2021-12-01 | Last modified: | 2022-01-19 | Method: | ELECTRON MICROSCOPY (3.4 Å) | Cite: | Cryo-EM structure of human GPR158 receptor coupled to the RGS7-G beta 5 signaling complex. Science, 375, 2022
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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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4PNI
| Bovine G protein-coupled receptor kinase 1 in complex with GSK2163632A | Descriptor: | 3-[(2-{[1-(N,N-dimethylglycyl)-6-methoxy-4,4-dimethyl-1,2,3,4-tetrahydroquinolin-7-yl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]thiophene-2-carboxamide, CHLORIDE ION, Rhodopsin kinase | Authors: | Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2014-05-23 | Release date: | 2014-10-08 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (1.85 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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4L9I
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3T8O
| Rhodopsin kinase (GRK1) L166K mutant at 2.5A resolution | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, GLYCEROL, ... | Authors: | Tesmer, J.J.G, Singh, P, Nance, M.R. | Deposit date: | 2011-08-01 | Release date: | 2012-06-06 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Structure of a monomeric variant of rhodopsin kinase at 2.5 A resolution. Acta Crystallogr.,Sect.F, 68, 2012
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3V5W
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3UZT
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3UZS
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5DO9
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2ODE
| Crystal structure of the heterodimeric complex of human RGS8 and activated Gi alpha 3 | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(k) subunit alpha, MAGNESIUM ION, ... | Authors: | Gileadi, C, Soundararajan, M, Turnbull, A.P, Elkins, J.M, Papagrigoriou, E, Pike, A.C.W, Bunkoczi, G, Gorrec, F, Umeano, C, von Delft, F, Weigelt, J, Edwards, A, Arrowsmith, C.H, Sundstrom, M, Doyle, D.A, Structural Genomics Consortium (SGC) | Deposit date: | 2006-12-22 | Release date: | 2007-02-06 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits. Proc.Natl.Acad.Sci.Usa, 105, 2008
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2PBI
| The multifunctional nature of Gbeta5/RGS9 revealed from its crystal structure | Descriptor: | GLYCEROL, Guanine nucleotide-binding protein subunit beta 5, Regulator of G-protein signaling 9 | Authors: | Cheever, M.L, Snyder, J.T, Gershburg, S, Siderovski, D.P, Harden, T.K, Sondek, J. | Deposit date: | 2007-03-28 | Release date: | 2008-01-29 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Crystal structure of the multifunctional Gbeta5-RGS9 complex. Nat.Struct.Mol.Biol., 15, 2008
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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
| 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
| 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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