1GG2
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G PROTEIN HETEROTRIMER MUTANT GI_ALPHA_1(G203A) BETA_1 GAMMA_2 WITH GDP BOUND
Descriptor:G PROTEIN GI ALPHA 1, G PROTEIN GI BETA 1, G PROTEIN GI GAMMA 2, GUANOSINE-5'-DIPHOSPHATE
Authors:Wall, M.A., Sprang, S.R.
Deposit date:1996-11-13
Release date:1997-02-12
Last modified:2009-02-24
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:The structure of the G protein heterotrimer Gi alpha 1 beta 1 gamma 2.
Cell(Cambridge,Mass.), 83, 1995
1GP2
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G PROTEIN HETEROTRIMER GI_ALPHA_1 BETA_1 GAMMA_2 WITH GDP BOUND
Descriptor:G PROTEIN GI ALPHA 1, G PROTEIN GI BETA 1, G PROTEIN GI GAMMA 2, GUANOSINE-5'-DIPHOSPHATE
Authors:Wall, M.A., Sprang, S.R.
Deposit date:1996-11-13
Release date:1997-02-12
Last modified:2009-02-24
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:The structure of the G protein heterotrimer Gi alpha 1 beta 1 gamma 2.
Cell(Cambridge,Mass.), 83, 1995
1XHM
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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(T) beta subunit 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, 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:2009-02-24
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
2BCJ
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CRYSTAL STRUCTURE OF G PROTEIN-COUPLED RECEPTOR KINASE 2 IN COMPLEX WITH GALPHA-Q AND GBETAGAMMA SUBUNITS
Descriptor:G-protein coupled receptor kinase 2 (E.C.2.7.1.126), Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1 (E.C.3.6.5.1), Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit (E.C.3.6.5.1), Guanine nucleotide-binding protein G(q), alpha subunit (E.C.3.6.5.1)
Authors:Tesmer, J.J.G.
Deposit date:2005-10-19
Release date:2005-12-20
Last modified:2017-06-28
Method:X-RAY DIFFRACTION (3.061 Å)
Cite:Snapshot of Activated G Proteins at the Membrane: The Gq-GRK2-G Complex
Science, 310, 2005
2PBI
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THE MULTIFUNCTIONAL NATURE OF GBETA5/RGS9 REVEALED FROM ITS CRYSTAL STRUCTURE
Descriptor:Regulator of G-protein signaling 9, Guanine nucleotide-binding protein subunit beta 5
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:2011-07-13
Method:X-RAY DIFFRACTION (1.95 Å)
Cite:Crystal structure of the multifunctional Gbeta5-RGS9 complex.
Nat.Struct.Mol.Biol., 15, 2008
3AH8
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STRUCTURE OF HETEROTRIMERIC G PROTEIN GALPHA-Q BETA GAMMA IN COMPLEX WITH AN INHIBITOR YM-254890
Descriptor:Guanine nucleotide-binding protein G(i) subunit alpha-1/Guanine nucleotide-binding protein G(q) subunit alpha chimeric protein, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, YM-254890
Authors:Nishimura, A., Kitano, K., Takasaki, J., Taniguchi, M., Mizuno, N., Tago, K., Hakoshima, T., Itoh, H.
Deposit date:2010-04-20
Release date:2010-07-21
Last modified:2010-08-18
Method:X-RAY DIFFRACTION (2.9 Å)
Cite:Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule.
Proc.Natl.Acad.Sci.USA, 107, 2010
3V5W
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HUMAN G PROTEIN-COUPLED RECEPTOR KINASE 2 IN COMPLEX WITH SOLUBLE GBETAGAMMA SUBUNITS AND PAROXETINE
Descriptor:G-protein coupled receptor kinase 2 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Authors:Thal, D.M., Tesmer, J.J.G.
Deposit date:2011-12-17
Release date:2012-09-26
Last modified:2012-12-12
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
4PNK
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G PROTEIN-COUPLED RECEPTOR KINASE 2 IN COMPLEX WITH GSK180736A
Descriptor:Human G protein-coupled receptor kinase 2 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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:2015-01-28
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
5HE0
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BOVINE GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG215022
Descriptor:Beta-adrenergic receptor kinase 1 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Authors:Cato, M.C., Waninger-Saroni, J., Tesmer, J.J.G.
Deposit date:2016-01-05
Release date:2016-05-11
Method:X-RAY DIFFRACTION (2.56 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
5HE1
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HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG224062
Descriptor:Beta-adrenergic receptor kinase 1 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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
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
5HE2
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BOVINE GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG224406
Descriptor:Beta-adrenergic receptor kinase 1 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Authors:Cato, M.C., Waninger-Saroni, J., Tesmer, J.J.G.
Deposit date:2016-01-05
Release date:2016-05-11
Method:X-RAY DIFFRACTION (2.79 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
5HE3
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BOVINE GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG224411
Descriptor:Beta-adrenergic receptor kinase 1 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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
Method:X-RAY DIFFRACTION (2.74 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
5KDO
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HETEROTRIMERIC COMPLEX OF THE 4 ALANINE INSERTION VARIANT OF THE GI ALPHA1 SUBUNIT AND THE GBETA1-GGAMMA1
Descriptor:Guanine nucleotide-binding protein G(i), alpha-1 subunit
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:2016-09-21
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
5UKM
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BOVINE GRK2 IN COMPLEX WITH HUMAN GBETAGAMMA SUBUNITS AND CCG258208 (14AS)
Descriptor:Beta-adrenergic receptor kinase 1 (E.C.2.7.11.15), Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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:2017-04-26
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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