PDB: 109 resultsInfo pagesStatus searchChemie searchBIRD

---

3KRX	Human GRK2 in complex with Gbetgamma subunits and balanol (co-crystal) 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 (3.1 Å) Cite: Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol. J.Med.Chem., 53, 2010
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
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
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
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
4L9I	Bovine G Protein Coupled Receptor Kinase 1 in Complex with Paroxetine Descriptor: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, Paroxetine, ... Authors: Homan, K.T, Tesmer, J.J.G. Deposit date: 2013-06-18 Release date: 2014-01-22 Last modified: 2023-09-20 Method: X-RAY DIFFRACTION (2.32 Å) Cite: Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog. Mol.Pharmacol., 85, 2014
4MK0	Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative Descriptor: 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-1H-isoindol-1-one, Beta-adrenergic receptor kinase 1, GLYCEROL, ... Authors: Homan, K.T, Tesmer, J.J.G. Deposit date: 2013-09-04 Release date: 2014-01-22 Last modified: 2024-02-28 Method: X-RAY DIFFRACTION (2.4 Å) Cite: Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog. Mol.Pharmacol., 85, 2014
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
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
7K7L	Structure of a hit for G Protein Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure Descriptor: 3-benzyl-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... Authors: Spurlino, J.C, Milligan, C. Deposit date: 2020-09-23 Release date: 2020-10-28 Last modified: 2024-04-03 Method: X-RAY DIFFRACTION (2.539 Å) Cite: Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor. Bioorg.Med.Chem.Lett., 30, 2020
7K7Z	Structure of a hit for G Protein Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure Descriptor: 3-benzyl-7-(1H-pyrazol-4-yl)quinazolin-4(3H)-one, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... Authors: Spurlino, J.C, Milligan, C. Deposit date: 2020-09-24 Release date: 2020-10-28 Last modified: 2024-04-03 Method: X-RAY DIFFRACTION (2.606087 Å) Cite: Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor. Bioorg.Med.Chem.Lett., 30, 2020
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
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
5WG5	Human GRK2 in complex with Gbetagamma subunits and CCG224061 Descriptor: 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-2H-indazole, 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 (3.1 Å) Cite: Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
5WG4	Human GRK2 in complex with Gbetagamma subunits and CCG257284 Descriptor: 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-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: 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 (2.31 Å) Cite: Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
3V5W	Human G Protein-Coupled Receptor Kinase 2 in Complex with Soluble Gbetagamma Subunits and Paroxetine Descriptor: G-protein coupled receptor kinase 2, 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.G. Deposit date: 2011-12-17 Release date: 2012-09-26 Last modified: 2023-09-13 Method: X-RAY DIFFRACTION (2.07 Å) Cite: Paroxetine is a direct inhibitor of g protein-coupled receptor kinase 2 and increases myocardial contractility. Acs Chem.Biol., 7, 2012
3UZT	Structure of the C13.18 RNA Aptamer in Complex with G Protein-Coupled Receptor Kinase 2 Descriptor: Beta-adrenergic receptor kinase 1, C13.18 RNA Aptamer, MAGNESIUM ION Authors: Tesmer, J.J.G, Tesmer, V.M. Deposit date: 2011-12-07 Release date: 2012-07-11 Last modified: 2023-09-13 Method: X-RAY DIFFRACTION (3.51 Å) Cite: Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer. Structure, 20, 2012
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
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
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
3UZS	Structure of the C13.28 RNA Aptamer Bound to the G Protein-Coupled Receptor Kinase 2-Heterotrimeric G Protein Beta 1 and Gamma 2 Subunit Complex Descriptor: Beta-adrenergic receptor kinase 1, C13.28 RNA Aptamer, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... Authors: Tesmer, J.J.G, Tesmer, V.M. Deposit date: 2011-12-07 Release date: 2012-07-11 Last modified: 2023-09-13 Method: X-RAY DIFFRACTION (4.52 Å) Cite: Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer. Structure, 20, 2012
3C4Y	Crystal Structure of Apo form of G protein coupled receptor kinase 1 at 7.51A Descriptor: Rhodopsin kinase Authors: Singh, P, Tesmer, J.J.G. Deposit date: 2008-01-30 Release date: 2008-03-11 Last modified: 2023-08-30 Method: X-RAY DIFFRACTION (7.509 Å) Cite: Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation. J.Biol.Chem., 283, 2008
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
3C51	Crystal structure of G protein coupled receptor kinase 1 bound to ADP and magnesium chloride at 3.55A Descriptor: ADENOSINE-5'-DIPHOSPHATE, BROMIDE ION, MAGNESIUM ION, ... Authors: Singh, P, Tesmer, J.J.G. Deposit date: 2008-01-30 Release date: 2008-03-11 Last modified: 2023-08-30 Method: X-RAY DIFFRACTION (3.55 Å) Cite: Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation. J.Biol.Chem., 283, 2008
3C4X	Crystal Structure of G protein coupled receptor kinase 1 bound to ATP and magnesium chloride at 2.9A Descriptor: ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, MAGNESIUM ION, ... Authors: Singh, P, Tesmer, J.J.G. Deposit date: 2008-01-30 Release date: 2008-03-11 Last modified: 2023-08-30 Method: X-RAY DIFFRACTION (2.9 Å) Cite: Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation. J.Biol.Chem., 283, 2008

<12345>