PDB: 109 resultsInfo pagesStatus searchChemie searchBIRD

---

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
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
4EKC	Structure of human regulator of G protein signaling 2 (RGS2) in complex with murine Galpha-q(R183C) Descriptor: GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(q) subunit alpha, MAGNESIUM ION, ... Authors: Tesmer, J.J.G, Nance, M.R. Deposit date: 2012-04-09 Release date: 2013-01-30 Last modified: 2023-09-13 Method: X-RAY DIFFRACTION (7.4 Å) Cite: Structural and functional analysis of the regulator of G protein signaling 2-g alpha q complex. Structure, 21, 2013
3T8O	Rhodopsin kinase (GRK1) L166K mutant at 2.5A resolution Descriptor: ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, GLYCEROL, ... Authors: Tesmer, J.J.G, Singh, P, Nance, M.R. Deposit date: 2011-08-01 Release date: 2012-06-06 Last modified: 2024-02-28 Method: X-RAY DIFFRACTION (2.5 Å) Cite: Structure of a monomeric variant of rhodopsin kinase at 2.5 A resolution. Acta Crystallogr.,Sect.F, 68, 2012
3QC9	Crystal structure of cross-linked bovine GRK1 T8C/N480C double mutant complexed with ADP and Mg Descriptor: ADENOSINE-5'-DIPHOSPHATE, GLYCEROL, MAGNESIUM ION, ... Authors: Huang, C.-C, Tesmer, J.J.G. Deposit date: 2011-01-15 Release date: 2011-02-16 Last modified: 2023-09-13 Method: X-RAY DIFFRACTION (2.7 Å) Cite: Activation of G Protein-Coupled Receptor Kinase 1 Involves Interactions between Its N-Terminal Region and Its Kinase Domain. Biochemistry, 50, 2011
4EKD	Structure of human regulator of G protein signaling 2 (RGS2) in complex with murine Galpha-q(R183C) Descriptor: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, COBALT (II) ION, ... Authors: Tesmer, J.J.G, Nance, M.R. Deposit date: 2012-04-09 Release date: 2013-01-30 Last modified: 2023-09-13 Method: X-RAY DIFFRACTION (2.71 Å) Cite: Structural and functional analysis of the regulator of G protein signaling 2-g alpha q complex. Structure, 21, 2013
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
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
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
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
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
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
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
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
2ODE	Crystal structure of the heterodimeric complex of human RGS8 and activated Gi alpha 3 Descriptor: GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(k) subunit alpha, MAGNESIUM ION, ... Authors: Gileadi, C, Soundararajan, M, Turnbull, A.P, Elkins, J.M, Papagrigoriou, E, Pike, A.C.W, Bunkoczi, G, Gorrec, F, Umeano, C, von Delft, F, Weigelt, J, Edwards, A, Arrowsmith, C.H, Sundstrom, M, Doyle, D.A, Structural Genomics Consortium (SGC) Deposit date: 2006-12-22 Release date: 2007-02-06 Last modified: 2023-08-30 Method: X-RAY DIFFRACTION (1.9 Å) Cite: Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits. Proc.Natl.Acad.Sci.Usa, 105, 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
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
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
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
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
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
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

<12345>