3UZS
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4YHJ
| Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4 (GRK4) | Descriptor: | AMP PHOSPHORAMIDATE, G protein-coupled receptor kinase 4 | Authors: | Allen, S.J, Parthasarathy, G, Soisson, S, Munshi, S. | Deposit date: | 2015-02-27 | Release date: | 2015-07-08 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4. J.Biol.Chem., 290, 2015
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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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4EKD
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4EKC
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4L9I
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2V4Z
| The crystal structure of the human G-protein subunit alpha (GNAI3) in complex with an engineered regulator of G-protein signaling type 2 domain (RGS2) | Descriptor: | GUANINE NUCLEOTIDE-BINDING PROTEIN G(K) SUBUNIT ALPHA, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... | Authors: | Roos, A.K, Soundararajan, M, Pike, A.C.W, Arrowsmith, C.H, Weigelt, J, Edwards, A, Bountra, C, Knapp, S. | Deposit date: | 2008-09-30 | Release date: | 2008-11-04 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Structural Determinants of G-Protein Alpha Subunit Selectivity by Regulator of G-Protein Signaling 2(Rgs2). J.Biol.Chem., 284, 2009
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6C2Y
| Human GRK2 in complex with Gbetagamma subunits and CCG257142 | Descriptor: | (4R,5R,6S)-4-[4-fluoro-3-({[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl]methyl}carbamoyl)phenyl]-N-(2H-indazol-5-yl)-6-methyl-2-oxohexahydropyrimidine-5-carboxamide, 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: | 2018-01-09 | Release date: | 2018-04-25 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorg. Med. Chem. Lett., 28, 2018
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4MK0
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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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7EWP
| Cryo-EM structure of human GPR158 in complex with RGS7-Gbeta5 in a 2:1:1 ratio | Descriptor: | Guanine nucleotide-binding protein subunit beta-5, Probable G-protein coupled receptor 158, Regulator of G-protein signaling 7 | Authors: | Kim, Y, Jeong, E, Jeong, J, Cho, Y. | Deposit date: | 2021-05-25 | Release date: | 2021-12-01 | Last modified: | 2022-02-16 | Method: | ELECTRON MICROSCOPY (4.3 Å) | Cite: | Structure of the class C orphan GPCR GPR158 in complex with RGS7-G beta 5. Nat Commun, 12, 2021
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7EWR
| Cryo-EM structure of human GPR158 in complex with RGS7-Gbeta5 in a 2:2:2 ratio | Descriptor: | Guanine nucleotide-binding protein subunit beta-5, Probable G-protein coupled receptor 158, Regulator of G-protein signaling 7 | Authors: | Kim, Y, Jeong, E, Jeong, J, Cho, Y. | Deposit date: | 2021-05-26 | Release date: | 2021-12-01 | Last modified: | 2022-02-16 | Method: | ELECTRON MICROSCOPY (4.7 Å) | Cite: | Structure of the class C orphan GPCR GPR158 in complex with RGS7-G beta 5. Nat Commun, 12, 2021
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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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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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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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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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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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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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