3C7K
| Molecular architecture of Galphao and the structural basis for RGS16-mediated deactivation | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(o) subunit alpha, MAGNESIUM ION, ... | Authors: | Slep, K.C, Kercher, M.A, Wieland, T, Chen, C, Simon, M.I, Sigler, P.B. | Deposit date: | 2008-02-07 | Release date: | 2008-05-06 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Molecular architecture of G{alpha}o and the structural basis for RGS16-mediated deactivation. Proc.Natl.Acad.Sci.Usa, 105, 2008
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7MT8
| Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin | Descriptor: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | Deposit date: | 2021-05-13 | Release date: | 2021-07-07 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (5.8 Å) | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1. Nature, 595, 2021
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7MTA
| Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab1 | Descriptor: | Fab1 Heavy chain, Fab1 Light chain, RETINAL, ... | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | Deposit date: | 2021-05-13 | Release date: | 2021-07-07 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (4.1 Å) | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1. Nature, 595, 2021
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7MT9
| Rhodopsin kinase (GRK1) in complex with rhodopsin | Descriptor: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | Deposit date: | 2021-05-13 | Release date: | 2021-07-07 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (7 Å) | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1. Nature, 595, 2021
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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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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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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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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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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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4TND
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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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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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4TNB
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3C4W
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3C4Z
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3C50
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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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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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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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5UVC
| Design, Synthesis, and Evaluation of the First Selective and Potent G-protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure | Descriptor: | Beta-adrenergic receptor kinase 1, N-benzyl-3-({[5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)benzamide, SULFATE ION | Authors: | Hoffman, I.D, Lawson, J.D. | Deposit date: | 2017-02-20 | Release date: | 2017-07-26 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.65 Å) | Cite: | Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. 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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3PVW
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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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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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