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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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
3C4W	Crystal Structure of G protein coupled receptor kinase 1 bound to ATP and magnesium chloride at 2.7A 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 (2.7 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
3C4Z	Crystal structure of G protein coupled receptor kinase 1 bound to ADP and magnesium chloride at 1.84A Descriptor: ADENOSINE-5'-DIPHOSPHATE, 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 (1.84 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

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