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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
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
1TBG
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BU of 1tbg by Molmil
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
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
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
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:2024-11-20
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
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
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
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:2024-10-16
Method:X-RAY DIFFRACTION (3.061 Å)
Cite:Snapshot of Activated G Proteins at the Membrane: The Gq-GRK2-G Complex
Science, 310, 2005
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
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
6K41
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BU of 6k41 by Molmil
cryo-EM structure of alpha2BAR-GoA complex
Descriptor: 4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole, Alpha-2A adrenergic receptor,Endolysin,Alpha-2B adrenergic receptor,Alpha-2B adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
Authors:Yuan, D, Liu, Z, Wang, H.W, Kobilka, B.K.
Deposit date:2019-05-23
Release date:2020-04-15
Last modified:2024-11-20
Method:ELECTRON MICROSCOPY (2.9 Å)
Cite:Activation of the alpha2Badrenoceptor by the sedative sympatholytic dexmedetomidine.
Nat.Chem.Biol., 16, 2020
7NA8
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BU of 7na8 by Molmil
Structures of human ghrelin receptor-Gi complexes with ghrelin and a synthetic agonist
Descriptor: 1-(methanesulfonyl)-1'-(2-methyl-L-alanyl-O-benzyl-D-seryl)-1,2-dihydrospiro[indole-3,4'-piperidine], Antibody fragment, CHOLESTEROL, ...
Authors:Liu, H, Sun, D, Sun, J, Zhang, C.
Deposit date:2021-06-20
Release date:2021-12-15
Last modified:2024-10-23
Method:ELECTRON MICROSCOPY (2.7 Å)
Cite:Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
Nat Commun, 12, 2021
7NA7
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BU of 7na7 by Molmil
Structures of human ghrelin receptor-Gi complexes with ghrelin and a synthetic agonist
Descriptor: Antibody fragment, CHOLESTEROL, Ghrelin-27, ...
Authors:Liu, H, Sun, D, Sun, J, Zhang, C.
Deposit date:2021-06-20
Release date:2021-12-15
Method:ELECTRON MICROSCOPY (2.7 Å)
Cite:Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
Nat Commun, 12, 2021
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
6K42
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BU of 6k42 by Molmil
cryo-EM structure of alpha2BAR-Gi1 complex
Descriptor: 4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole, Alpha-2A adrenergic receptor,Endolysin,Alpha-2B adrenergic receptor,Alpha-2B adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
Authors:Yuan, D, Liu, Z, Wang, H.W, Kobilka, B.K.
Deposit date:2019-05-23
Release date:2020-04-15
Last modified:2024-10-30
Method:ELECTRON MICROSCOPY (4.1 Å)
Cite:Activation of the alpha2Badrenoceptor by the sedative sympatholytic dexmedetomidine.
Nat.Chem.Biol., 16, 2020
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
7AD3
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BU of 7ad3 by Molmil
Class D GPCR Ste2 dimer coupled to two G proteins
Descriptor: 2-acetamido-2-deoxy-beta-D-glucopyranose, Alpha-factor mating pheromone, CHOLESTEROL HEMISUCCINATE, ...
Authors:Velazhahan, V, Tate, C.
Deposit date:2020-09-14
Release date:2020-12-09
Last modified:2024-11-13
Method:ELECTRON MICROSCOPY (3.5 Å)
Cite:Structure of the class D GPCR Ste2 dimer coupled to two G proteins.
Nature, 589, 2021
5HE2
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BU of 5he2 by Molmil
Bovine GRK2 in complex with Gbetagamma subunits and CCG224406
Descriptor: (4~{S})-4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 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:2024-03-06
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
5HE1
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BU of 5he1 by Molmil
Human GRK2 in complex with Gbetagamma subunits and CCG224062
Descriptor: (4~{S})-4-[4-fluoranyl-3-(isoquinolin-1-ylmethylcarbamoyl)phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 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:2024-03-06
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
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
7AUE
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BU of 7aue by Molmil
Melanocortin receptor 4 (MC4R) Gs protein complex
Descriptor: AMINOSERINE, CALCIUM ION, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
Authors:Degtjarik, O, Israeli, H, Prabahar, V, Shalev-Benami, M.
Deposit date:2020-11-02
Release date:2021-04-28
Last modified:2023-03-15
Method:ELECTRON MICROSCOPY (2.97 Å)
Cite:Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling.
Science, 372, 2021
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:2024-11-06
Method:X-RAY DIFFRACTION (3.45 Å)
Cite:X-ray structure of the mammalian GIRK2-beta gamma G-protein complex.
Nature, 498, 2013
5HE0
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BU of 5he0 by Molmil
Bovine GRK2 in complex with Gbetagamma subunits and CCG215022
Descriptor: (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-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:Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G.
Deposit date:2016-01-05
Release date:2016-05-11
Last modified:2023-09-27
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

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