1AGR
 
 | | COMPLEX OF ALF4-ACTIVATED GI-ALPHA-1 WITH RGS4 | | Descriptor: | CITRIC ACID, GUANINE NUCLEOTIDE-BINDING PROTEIN G(I), GUANOSINE-5'-DIPHOSPHATE, ... | | Authors: | Tesmer, J.J.G, Sprang, S.R. | | Deposit date: | 1997-03-25 | | Release date: | 1997-06-16 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structure of RGS4 bound to AlF4--activated G(i alpha1): stabilization of the transition state for GTP hydrolysis.
Cell(Cambridge,Mass.), 89, 1997
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7MTB
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab6 | | Descriptor: | Fab6 heavy chain, Fab6 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 Å) | | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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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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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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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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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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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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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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3C50
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3C4Y
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3C51
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3C4X
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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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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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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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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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3PVW
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2ACX
 | | Crystal Structure of G protein coupled receptor kinase 6 bound to AMPPNP | | Descriptor: | G protein-coupled receptor kinase 6, MAGNESIUM ION, PHOSPHATE ION, ... | | Authors: | Lodowski, D.T, Tesmer, V.M, Benovic, J.L, Tesmer, J.J. | | Deposit date: | 2005-07-19 | | Release date: | 2006-04-25 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | The Structure of G Protein-coupled Receptor Kinase (GRK)-6 Defines a Second Lineage of GRKs.
J.Biol.Chem., 281, 2006
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3QC9
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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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