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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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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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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5UUU
 | | 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: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 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, ... | | Authors: | Hoffman, I.D, Lawson, J.D. | | Deposit date: | 2017-02-17 | | Release date: | 2017-07-26 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.7 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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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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7K7L
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7K7Z
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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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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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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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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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3PVW
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3QC9
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2GTP
 | | Crystal structure of the heterodimeric complex of human RGS1 and activated Gi alpha 1 | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(i), alpha-1 subunit, ... | | Authors: | Soundararajan, M, Turnbull, A.P, Ugochukwu, E, Gorrec, F, von Delft, F, Weigelt, J, Edwards, A, Arrowsmith, C, Sundstrom, M, Doyle, D.A, Structural Genomics Consortium (SGC) | | Deposit date: | 2006-04-28 | | Release date: | 2006-05-23 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.55 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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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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2IK8
 | | Crystal structure of the heterodimeric complex of human RGS16 and activated Gi alpha 1 | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(i), alpha-1 subunit, ... | | Authors: | Soundararajan, M, Turnbull, A.P, Papagrigoriou, E, Debreczeni, J, Gorrec, F, von Delft, F, Weigelt, J, Edwards, A, Arrowsmith, C, Sundstrom, M, Doyle, D.A, Structural Genomics Consortium (SGC) | | Deposit date: | 2006-10-02 | | Release date: | 2006-11-21 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.71 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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2IHB
 | | Crystal structure of the heterodimeric complex of human RGS10 and activated Gi alpha 3 | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(k) subunit alpha, MAGNESIUM ION, ... | | Authors: | Soundararajan, M, Turnbull, A.P, Papagrigoriou, E, Pike, A.C.W, Bunkoczi, G, Ugochukwu, E, Gorrec, F, von Delft, F, Weigelt, J, Edwards, A, Arrowsmith, C, Sundstrom, M, Doyle, D.A, Structural Genomics Consortium (SGC) | | Deposit date: | 2006-09-26 | | Release date: | 2006-11-21 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.71 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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3C4W
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