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, ...
Authors:Wall, M.A., Sprang, S.R.
Deposit date:1996-11-13
Release date:1997-02-12
Last modified:2011-07-13
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, ...
Authors:Wall, M.A., Sprang, S.R.
Deposit date:1996-11-13
Release date:1997-02-12
Last modified:2011-07-13
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:2011-07-13
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, 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: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, GLYCEROL
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:2017-10-18
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, ...
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:2017-08-02
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, 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:Beta-adrenergic receptor kinase 1, 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:2017-09-06
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, 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
Last modified:2017-11-22
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, 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
Last modified:2017-11-22
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, 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
Last modified:2017-11-22
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, 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
Last modified:2017-11-22
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) subunit alpha-1, 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:2017-09-13
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, 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:2017-09-20
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
5WG3
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HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG258748
Descriptor:Beta-adrenergic receptor kinase 1, 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:Bouley, R., Tesmer, J.J.G.
Deposit date:2017-07-13
Release date:2017-12-27
Last modified:2018-01-17
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
5WG4
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HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG257284
Descriptor:Beta-adrenergic receptor kinase 1, 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:Bouley, R., Tesmer, J.J.G.
Deposit date:2017-07-13
Release date:2017-12-27
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
5WG5
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HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG224061
Descriptor:Beta-adrenergic receptor kinase 1, 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:Bouley, R., Tesmer, J.J.G.
Deposit date:2017-07-13
Release date:2017-12-27
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
6B3J
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3.3 ANGSTROM PHASE-PLATE CRYO-EM STRUCTURE OF A BIASED AGONIST-BOUND HUMAN GLP-1 RECEPTOR-GS COMPLEX
Descriptor:Glucagon-like peptide 1 receptor, Exendin-P5, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ...
Authors:Liang, Y.L., Khoshouei, M., Glukhova, A., Furness, S.G.B., Koole, C., Zhao, P., Clydesdale, L., Thal, D.M., Radjainia, M., Danev, R., Baumeister, W., Wang, M.W., Miller, L.J., Christopoulos, A., Sexton, P.M., Wootten, D.
Deposit date:2017-09-22
Release date:2018-02-21
Last modified:2018-03-07
Method:ELECTRON MICROSCOPY (3.3 Å)
Cite:Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.
Nature, 555, 2018
6C2Y
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HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG257142
Descriptor:Beta-adrenergic receptor kinase 1, 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:Bouley, R., Tesmer, J.J.G.
Deposit date:2018-01-09
Release date:2018-04-25
Last modified:2018-05-02
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
6CRK
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HETEROTRIMERIC G-PROTEIN IN COMPLEX WITH AN ANTIBODY FRAGMENT
Descriptor:Guanine nucleotide-binding protein G(i) subunit alpha-1, 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:Maeda, S., Dawson, R., Kobilka, B.
Deposit date:2018-03-19
Release date:2018-10-24
Method:X-RAY DIFFRACTION (2 Å)
Cite:Development of an antibody fragment that stabilizes GPCR/G-protein complexes.
Nat Commun, 9, 2018
6D9H
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CRYO-EM STRUCTURE OF THE HUMAN ADENOSINE A1 RECEPTOR-GI2-PROTEIN COMPLEX BOUND TO ITS ENDOGENOUS AGONIST
Descriptor:Guanine nucleotide-binding protein G(i) subunit alpha-2, 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:Draper-Joyce, C.J., Khoshouei, M., Thal, D.M., Liang, Y.-L., Nguyen, A.T.N., Furness, S.G.B., Venugopal, H., Baltos, J., Plitzko, J.M., Danev, R., Baumeister, W., May, L.T., Wootten, D., Sexton, P., Glukhova, A., Christopoulos, A.
Deposit date:2018-04-29
Release date:2018-06-20
Last modified:2018-07-11
Method:ELECTRON MICROSCOPY (3.6 Å)
Cite:Structure of the adenosine-bound human adenosine A1receptor-Gicomplex.
Nature, 558, 2018
6DDE
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MU OPIOID RECEPTOR-GI PROTEIN COMPLEX
Descriptor:Guanine nucleotide-binding protein G(i) subunit alpha-1, 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:Koehl, A., Hu, H., Maeda, S., Manglik, A., Zhang, Y., Kobilka, B.K., Skiniotis, G., Weis, W.I.
Deposit date:2018-05-10
Release date:2018-06-13
Last modified:2018-07-04
Method:ELECTRON MICROSCOPY (3.5 Å)
Cite:Structure of the mu-opioid receptor-Giprotein complex.
Nature, 558, 2018
6DDF
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MU OPIOID RECEPTOR-GI PROTEIN COMPLEX
Descriptor:Guanine nucleotide-binding protein G(i) subunit alpha-1, 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:Koehl, A., Hu, H., Maeda, S., Manglik, A., Kobilka, B.K., Skiniotis, G., Weis, W.I.
Deposit date:2018-05-10
Release date:2018-06-13
Last modified:2018-07-04
Method:ELECTRON MICROSCOPY (3.5 Å)
Cite:Structure of the mu-opioid receptor-Giprotein complex.
Nature, 558, 2018
6E3Y
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CRYO-EM STRUCTURE OF THE ACTIVE, GS-PROTEIN COMPLEXED, HUMAN CGRP RECEPTOR
Descriptor:Calcitonin gene-related peptide 1, Nanobody 35, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ...
Authors:Liang, Y.L., Khoshouei, M., Deganutti, G., Glukhova, A., Koole, C., Peat, T.S., Radjainia, M., Plitzko, J.M., Baumeister, W., Miller, L.J., Hay, D.L., Christopoulos, A., Reynolds, C.A., Wootten, D., Sexton, P.M.
Deposit date:2018-07-16
Release date:2018-09-19
Last modified:2018-10-10
Method:ELECTRON MICROSCOPY (3.3 Å)
Cite:Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.
Nature, 561, 2018
6G79
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COUPLING SPECIFICITY OF HETEROTRIMERIC GO TO THE SEROTONIN 5-HT1B RECEPTOR
Descriptor: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, Guanine nucleotide-binding protein G(o) subunit alpha, ...
Authors:Garcia-Nafria, J., Nehme, R., Edwards, P., Tate, C.G.
Deposit date:2018-04-05
Release date:2018-06-20
Last modified:2018-09-19
Method:ELECTRON MICROSCOPY (3.78 Å)
Cite:Cryo-EM structure of the serotonin 5-HT1Breceptor coupled to heterotrimeric Go.
Nature, 558, 2018
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