2CRP
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2D9J
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2DLR
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2DLV
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2EBZ
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2ES0
| Structure of the regulator of G-protein signaling domain of RGS6 | Descriptor: | regulator of G-protein signalling 6 | Authors: | Schoch, G.A, Phillips, C, Turnbull, A, Niesen, F, Johansson, C, Elkins, J.M, Longman, E, Gilealdi, C, Sobott, F, Ball, L, Sundstrom, M, Edwards, A, Arrowsmith, C, von Delft, F, Doyle, D.A, Structural Genomics Consortium (SGC) | Deposit date: | 2005-10-25 | Release date: | 2005-11-29 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (2.1 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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1EMU
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4GOU
| Crystal structure of an RGS-RhoGEF from Entamoeba histolytica | Descriptor: | EhRGS-RhoGEF | Authors: | Bosch, D.E, Kimple, A.J, Muller, R.E, Willard, F.S, Machius, M, Siderovski, D.P. | Deposit date: | 2012-08-20 | Release date: | 2013-01-09 | Last modified: | 2013-01-30 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Structural Determinants of RGS-RhoGEF Signaling Critical to Entamoeba histolytica Pathogenesis. Structure, 21, 2013
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3CIK
| Human 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: | Tesmer, J.J.G, Lodowski, D.T. | Deposit date: | 2008-03-11 | Release date: | 2009-02-17 | Last modified: | 2012-03-07 | Method: | X-RAY DIFFRACTION (2.75 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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6PJX
| Crystal Structure of G Protein-Coupled Receptor Kinase 5 (GRK5) in Complex with Calmodulin (CaM) | Descriptor: | CALCIUM ION, Calmodulin, G protein-coupled receptor kinase 5, ... | Authors: | Bhardwaj, A, Komolov, K.E, Sulon, S, Benovic, J.L. | Deposit date: | 2019-06-28 | Release date: | 2020-12-09 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.96 Å) | Cite: | Structure of a GRK5-Calmodulin Complex Reveals Molecular Mechanism of GRK Activation and Substrate Targeting. Mol.Cell, 81, 2021
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7PWD
| Structure of an inhibited GRK2-G-beta and G-gamma complex | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | Deposit date: | 2021-10-06 | Release date: | 2021-10-20 | Last modified: | 2022-05-18 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors Monatsh Chem, 2022
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6U7C
| Human GRK2 in complex with Gbetagamma subunits and CCG258747 | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-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: | 2019-09-02 | Release date: | 2020-04-15 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.44 Å) | Cite: | A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor. Mol.Pharmacol., 97, 2020
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6N9G
| Crystal Structure of RGS7-Gbeta5 dimer | Descriptor: | Guanine nucleotide-binding protein subunit beta-5, Regulator of G-protein signaling 7 | Authors: | Patil, D.N, Rangarajan, E, Izard, T, Martemyanov, K.A. | Deposit date: | 2018-12-03 | Release date: | 2019-01-09 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.129 Å) | Cite: | Structural organization of a major neuronal G protein regulator, the RGS7-G beta 5-R7BP complex. Elife, 7, 2018
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5DO9
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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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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: | 2023-08-02 | 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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8UAQ
| Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21 | Descriptor: | (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-[(4-{[(2S)-2-(furan-2-yl)-2-hydroxyacetyl]amino}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide, G protein-coupled receptor kinase 5 | Authors: | Chen, Y, Tesmer, J.J.G. | Deposit date: | 2023-09-21 | Release date: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes. Eur.J.Med.Chem., 264, 2023
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8UAP
| Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 D311N in Complex with CCG273441 | Descriptor: | (3Z)-3-{[4-(2-chloroacetamido)-3,5-dimethyl-1H-pyrrol-2-yl]methylidene}-N-[(1R)-1-(4-fluorophenyl)ethyl]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide, G protein-coupled receptor kinase 5 | Authors: | Chen, Y, Tesmer, J.J.G. | Deposit date: | 2023-09-21 | Release date: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes. Eur.J.Med.Chem., 264, 2023
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4WBO
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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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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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4WNK
| Crystal Structure of Bovine G Protein Coupled-Receptor Kinase 5 in Complex with 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, G protein-coupled receptor kinase 5, SULFATE ION | Authors: | Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2014-10-13 | Release date: | 2015-06-10 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.42 Å) | Cite: | Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor. J.Biol.Chem., 290, 2015
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3V5W
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3UZT
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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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