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5WG3
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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
1OMW
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BU of 1omw by Molmil
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
6XOX
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BU of 6xox by Molmil
cryo-EM of human GLP-1R bound to non-peptide agonist LY3502970
Descriptor: 3-[(1S,2S)-1-(5-[(4S)-2,2-dimethyloxan-4-yl]-2-{(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carbonyl}-1H-indol-1-yl)-2-methylcyclopropyl]-1,2,4-oxadiazol-5(4H)-one, Alpha subunit of Gs with N-terminus swapped with equivalent residues in Gi,Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas, Glucagon-like peptide 1 receptor, ...
Authors:Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S.
Deposit date:2020-07-07
Release date:2020-11-18
Last modified:2020-12-09
Method:ELECTRON MICROSCOPY (3.1 Å)
Cite:Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Proc.Natl.Acad.Sci.USA, 117, 2020
1TBG
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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
2TRC
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BU of 2trc by Molmil
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
1XHM
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BU of 1xhm by Molmil
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
5KDO
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BU of 5kdo by Molmil
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
6RMV
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BU of 6rmv by Molmil
The crystal structure of a TRP channel peptide bound to a G protein beta gamma heterodimer
Descriptor: GLYCEROL, 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:Gruss, F, Oberwinkler, J, Ulens, C.
Deposit date:2019-05-07
Release date:2020-10-14
Last modified:2024-01-24
Method:X-RAY DIFFRACTION (1.94 Å)
Cite:The structural basis for an on-off switch controlling G beta gamma-mediated inhibition of TRPM3 channels.
Proc.Natl.Acad.Sci.USA, 117, 2020
2BCJ
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BU of 2bcj by Molmil
Crystal Structure of G Protein-Coupled Receptor Kinase 2 in Complex with Galpha-q and Gbetagamma Subunits
Descriptor: G-protein-coupled receptor kinase 2, GUANOSINE-5'-DIPHOSPHATE, 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:2023-08-23
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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BU of 2pbi by Molmil
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
3CIK
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BU of 3cik by Molmil
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
4PNK
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BU of 4pnk by Molmil
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
3AH8
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BU of 3ah8 by Molmil
Structure of heterotrimeric G protein Galpha-q beta gamma in complex with an inhibitor YM-254890
Descriptor: GUANOSINE-5'-DIPHOSPHATE, 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: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:2023-11-15
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
3KRW
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BU of 3krw by Molmil
Human GRK2 in complex with Gbetgamma subunits and balanol (soak)
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 (2.9 Å)
Cite:Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
3KRX
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BU of 3krx by Molmil
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
4KFM
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BU of 4kfm by Molmil
Crystal structure of the G protein-gated inward rectifier K+ channel GIRK2 (Kir3.2) in complex with the beta-gamma G protein subunits
Descriptor: DODECYL-BETA-D-MALTOSIDE, G protein-activated inward rectifier potassium channel 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
Authors:Whorton, M.R, MacKinnon, R.
Deposit date:2013-04-27
Release date:2013-06-12
Last modified:2013-09-11
Method:X-RAY DIFFRACTION (3.45 Å)
Cite:X-ray structure of the mammalian GIRK2-beta gamma G-protein complex.
Nature, 498, 2013
3V5W
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BU of 3v5w by Molmil
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
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BU of 3uzs by Molmil
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
4MK0
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BU of 4mk0 by Molmil
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
6EG8
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BU of 6eg8 by Molmil
Structure of the GDP-bound Gs heterotrimer
Descriptor: GUANOSINE-5'-DIPHOSPHATE, 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:Hilger, D, Liu, X, Aschauer, P, Kobilka, B.K.
Deposit date:2018-08-19
Release date:2019-06-05
Last modified:2024-03-13
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Structural Insights into the Process of GPCR-G Protein Complex Formation.
Cell, 177, 2019
1B9Y
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BU of 1b9y by Molmil
STRUCTURAL ANALYSIS OF PHOSDUCIN AND ITS PHOSPHORYLATION-REGULATED INTERACTION WITH TRANSDUCIN BETA-GAMMA
Descriptor: GADOLINIUM ATOM, PROTEIN (PHOSDUCIN), PROTEIN (TRANSDUCIN)
Authors:Gaudet, R, Sigler, P.B.
Deposit date:1999-02-16
Release date:1999-02-23
Last modified:2023-08-09
Method:X-RAY DIFFRACTION (3 Å)
Cite:A molecular mechanism for the phosphorylation-dependent regulation of heterotrimeric G proteins by phosducin.
Mol.Cell, 3, 1999
1A0R
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BU of 1a0r by Molmil
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
1GG2
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BU of 1gg2 by Molmil
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:2024-02-07
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
1GOT
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BU of 1got by Molmil
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
6GDG
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Cryo-EM structure of the adenosine A2A receptor bound to a miniGs heterotrimer
Descriptor: 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, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ...
Authors:Garcia-Nafria, J, Lee, Y.
Deposit date:2018-04-23
Release date:2018-05-16
Last modified:2019-12-18
Method:ELECTRON MICROSCOPY (4.11 Å)
Cite:Cryo-EM structure of the adenosine A2Areceptor coupled to an engineered heterotrimeric G protein.
Elife, 7, 2018

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