5KDO
 
 | | Heterotrimeric complex of the 4 alanine insertion variant of the Gi alpha1 subunit and the Gbeta1-Ggamma1 | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(T) subunit gamma-T1, ... | | Authors: | Kaya, A.I, Lokits, A.D, Gilbert, J, Iverson, T.M, Meiler, J, Hamm, H.E. | | Deposit date: | 2016-06-08 | | Release date: | 2016-08-03 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | A Conserved Hydrophobic Core in G alpha i1 Regulates G Protein Activation and Release from Activated Receptor.
J.Biol.Chem., 291, 2016
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1GOT
 | | HETEROTRIMERIC COMPLEX OF A GT-ALPHA/GI-ALPHA CHIMERA AND THE GT-BETA-GAMMA SUBUNITS | | Descriptor: | GT-ALPHA/GI-ALPHA CHIMERA, GT-BETA, GT-GAMMA, ... | | Authors: | Lambright, D.G, Sondek, J, Bohm, A, Skiba, N.P, Hamm, H.E, Sigler, P.B. | | Deposit date: | 1996-08-07 | | Release date: | 1997-03-12 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | The 2.0 A crystal structure of a heterotrimeric G protein.
Nature, 379, 1996
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3V5W
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1TBG
 | | BETA-GAMMA DIMER OF THE HETEROTRIMERIC G-PROTEIN TRANSDUCIN | | Descriptor: | TRANSDUCIN | | Authors: | Sondek, J.S, Bohm, A, Lambright, D.G, Hamm, H.E, Sigler, P.B. | | Deposit date: | 1996-06-15 | | Release date: | 1997-04-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Crystal structure of a G-protein beta gamma dimer at 2.1A resolution.
Nature, 379, 1996
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1GP2
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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
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6B20
 | | Crystal structure of a complex between G protein beta gamma dimer and an inhibitory Nanobody regulator | | Descriptor: | CHLORIDE ION, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(T) subunit gamma-T1, ... | | Authors: | Gulati, S, Kiser, P.D, Palczewski, K. | | Deposit date: | 2017-09-19 | | Release date: | 2018-05-30 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.34 Å) | | Cite: | Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor.
Nat Commun, 9, 2018
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2TRC
 | | PHOSDUCIN/TRANSDUCIN BETA-GAMMA COMPLEX | | Descriptor: | GADOLINIUM ATOM, PHOSDUCIN, TRANSDUCIN | | Authors: | Gaudet, R, Bohm, A, Sigler, P.B. | | Deposit date: | 1997-01-06 | | Release date: | 1997-06-05 | | Last modified: | 2019-08-14 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Crystal structure at 2.4 angstroms resolution of the complex of transducin betagamma and its regulator, phosducin.
Cell(Cambridge,Mass.), 87, 1996
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1GG2
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4MK0
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6U7C
 | | Human GRK2 in complex with Gbetagamma subunits and CCG258747 | | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-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: | 2019-09-02 | | Release date: | 2020-04-15 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.44 Å) | | Cite: | A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor.
Mol.Pharmacol., 97, 2020
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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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3PVW
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1OMW
 | | Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits | | Descriptor: | G-protein coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1 | | Authors: | Lodowski, D.T, Pitcher, J.A, Capel, W.D, Lefkowitz, R.J, Tesmer, J.J.G. | | Deposit date: | 2003-02-26 | | Release date: | 2003-06-03 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Keeping G proteins at Bay: A Complex Between G Protein-Coupled Receptor Kinase 2 and G-Beta-Gamma
Science, 300, 2003
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8DCS
 | | Cryo-EM structure of cyanopindolol-bound beta1-adrenergic receptor in complex with heterotrimeric Gs-protein | | Descriptor: | 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile, Endolysin,Endolysin,Beta-1 adrenergic receptor chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Su, M, Paknejad, N, Hite, R.K, Huang, X.Y. | | Deposit date: | 2022-06-17 | | Release date: | 2022-07-27 | | Method: | ELECTRON MICROSCOPY (2.5 Å) | | Cite: | Structures of beta 1 -adrenergic receptor in complex with Gs and ligands of different efficacies.
Nat Commun, 13, 2022
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8DCR
 | | Cryo-EM structure of dobutamine-bound beta1-adrenergic receptor in complex with heterotrimeric Gs-protein | | Descriptor: | DOBUTAMINE, Endolysin,Endolysin,Beta-1 adrenergic receptor chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Su, M, Paknejad, N, Hite, R.K, Huang, X.Y. | | Deposit date: | 2022-06-17 | | Release date: | 2022-07-27 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structures of beta 1 -adrenergic receptor in complex with Gs and ligands of different efficacies.
Nat Commun, 13, 2022
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7TD4
 | | Sphingosine-1-phosphate receptor 1-Gi complex bound to Siponimod | | Descriptor: | 1-[[4-[(~{E})-~{N}-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-~{C}-methyl-carbonimidoyl]-2-ethyl-phenyl]methyl]azetidine-3-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, S, Paknejad, N, Zhu, L, Kihara, Y, Ray, D, Chun, J, Liu, W, Hite, R.K, Huang, X.Y. | | Deposit date: | 2021-12-30 | | Release date: | 2022-02-09 | | Last modified: | 2022-02-23 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate.
Nat Commun, 13, 2022
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7JJO
 | | Structural Basis of the Activation of Heterotrimeric Gs-protein by Isoproterenol-bound Beta1-Adrenergic Receptor | | Descriptor: | Beta1-Adrenergic Receptor, 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: | Su, M, Zhu, L, Zhang, Y, Paknejad, N, Dey, R, Huang, J, Lee, M.Y, Williams, D, Jordan, K.D, Eng, E.T, Ernst, O.P, Meyerson, J.R, Hite, R.K, Walz, T, Liu, W, Huang, X.Y. | | Deposit date: | 2020-07-27 | | Release date: | 2020-09-02 | | Last modified: | 2020-10-14 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structural Basis of the Activation of Heterotrimeric Gs-Protein by Isoproterenol-Bound beta 1 -Adrenergic Receptor.
Mol.Cell, 80, 2020
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7PWD
 | | Structure of an inhibited GRK2-G-beta and G-gamma complex | | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | | Deposit date: | 2021-10-06 | | Release date: | 2021-10-20 | | Last modified: | 2024-06-19 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Monatsh Chem, 2022
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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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1XHM
 | | The Crystal Structure of a Biologically Active Peptide (SIGK) Bound to a G Protein Beta:Gamma Heterodimer | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1, SIGK Peptide | | Authors: | Davis, T.L, Bonacci, T.M, Smrcka, A.V, Sprang, S.R. | | Deposit date: | 2004-09-20 | | Release date: | 2005-08-09 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structural and Molecular Characterization of a Preferred Protein Interaction Surface on G Protein betagamma Subunits.
Biochemistry, 44, 2005
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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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3CIK
 | | Human 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: | Tesmer, J.J.G, Lodowski, D.T. | | Deposit date: | 2008-03-11 | | Release date: | 2009-02-17 | | Last modified: | 2012-03-07 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
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1A0R
 | | HETEROTRIMERIC COMPLEX OF PHOSDUCIN/TRANSDUCIN BETA-GAMMA | | Descriptor: | FARNESYL, PHOSDUCIN, TRANSDUCIN (BETA SUBUNIT), ... | | Authors: | Loew, A, Ho, Y.-K, Blundell, T.L, Bax, B. | | Deposit date: | 1997-12-05 | | Release date: | 1998-12-30 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Phosducin induces a structural change in transducin beta gamma.
Structure, 6, 1998
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7TD0
 | | Lysophosphatidic acid receptor 1-Gi complex bound to LPA | | Descriptor: | (2R)-2-hydroxy-3-(phosphonooxy)propyl (9E)-octadec-9-enoate, 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: | Liu, S, Paknejad, N, Zhu, L, Kihara, Y, Ray, D, Chun, J, Liu, W, Hite, R.K, Huang, X.Y. | | Deposit date: | 2021-12-30 | | Release date: | 2022-02-09 | | Last modified: | 2022-02-23 | | Method: | ELECTRON MICROSCOPY (2.83 Å) | | Cite: | Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate.
Nat Commun, 13, 2022
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