3NYO
| Crystal Structure of G Protein-Coupled Receptor Kinase 6 in Complex with AMP | Descriptor: | (R,R)-2,3-BUTANEDIOL, ADENOSINE MONOPHOSPHATE, G protein-coupled receptor kinase 6, ... | Authors: | Tesmer, J.J.G, Singh, P. | Deposit date: | 2010-07-15 | Release date: | 2010-09-22 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.92 Å) | Cite: | Molecular basis for activation of G protein-coupled receptor kinases. Embo J., 29, 2010
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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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4L9I
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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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7K7L
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7K7Z
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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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3NYN
| Crystal Structure of G Protein-Coupled Receptor Kinase 6 in Complex with Sangivamycin | Descriptor: | (R,R)-2,3-BUTANEDIOL, G protein-coupled receptor kinase 6, SANGIVAMYCIN, ... | Authors: | Tesmer, J.J.G, Singh, P. | Deposit date: | 2010-07-15 | Release date: | 2010-09-22 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.72 Å) | Cite: | Molecular basis for activation of G protein-coupled receptor kinases. Embo J., 29, 2010
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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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4EKD
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4MK0
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4EKC
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1FQJ
| CRYSTAL STRUCTURE OF THE HETEROTRIMERIC COMPLEX OF THE RGS DOMAIN OF RGS9, THE GAMMA SUBUNIT OF PHOSPHODIESTERASE AND THE GT/I1 CHIMERA ALPHA SUBUNIT [(RGS9)-(PDEGAMMA)-(GT/I1ALPHA)-(GDP)-(ALF4-)-(MG2+)] | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(t) subunit alpha-1,Guanine nucleotide-binding protein G(i) subunit alpha-1,Guanine nucleotide-binding protein G(t) subunit alpha-1, MAGNESIUM ION, ... | Authors: | Slep, K.C, Kercher, M.A, He, W, Cowan, C.W, Wensel, T.G, Sigler, P.B. | Deposit date: | 2000-09-05 | Release date: | 2001-02-28 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.02 Å) | Cite: | Structural determinants for regulation of phosphodiesterase by a G protein at 2.0 A. Nature, 409, 2001
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1FQK
| CRYSTAL STRUCTURE OF THE HETERODIMERIC COMPLEX OF THE RGS DOMAIN OF RGS9, AND THE GT/I1 CHIMERA ALPHA SUBUNIT [(RGS9)-(GT/I1ALPHA)-(GDP)-(ALF4-)-(MG2+)] | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(t) subunit alpha-1,Guanine nucleotide-binding protein G(i) subunit alpha-1,Guanine nucleotide-binding protein G(t) subunit alpha-1, MAGNESIUM ION, ... | Authors: | Slep, K.C, Kercher, M.A, He, W, Cowan, C.W, Wensel, T.G, Sigler, P.B. | Deposit date: | 2000-09-05 | Release date: | 2001-02-28 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Structural determinants for regulation of phosphodiesterase by a G protein at 2.0 A. Nature, 409, 2001
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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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3UZT
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3V5W
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3UZS
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3C4W
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3C4Z
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