3SN6
 
 | | Crystal structure of the beta2 adrenergic receptor-Gs protein complex | | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid antibody VHH fragment, Endolysin,Beta-2 adrenergic receptor, ... | | Authors: | Rasmussen, S.G.F, DeVree, B.T, Zou, Y, Kruse, A.C, Chung, K.Y, Kobilka, T.S, Thian, F.S, Chae, P.S, Pardon, E, Calinski, D, Mathiesen, J.M, Shah, S.T.A, Lyons, J.A, Caffrey, M, Gellman, S.H, Steyaert, J, Skiniotis, G, Weis, W.I, Sunahara, R.K, Kobilka, B.K. | | Deposit date: | 2011-06-28 | | Release date: | 2011-07-20 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Crystal structure of the beta2 adrenergic receptor-Gs protein complex
Nature, 477, 2011
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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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5WG5
 | | Human GRK2 in complex with Gbetagamma subunits and CCG224061 | | Descriptor: | 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-2H-indazole, 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 (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
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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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1GG2
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3PVW
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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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1GP2
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1B9Y
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5HE0
 | | 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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5HE3
 | | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | | Descriptor: | (4~{S})-4-[3-[2-(2,6-dimethylphenyl)ethylcarbamoyl]-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, Tesmer, J.J.G. | | Deposit date: | 2016-01-05 | | Release date: | 2016-05-11 | | Last modified: | 2024-03-06 | | 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
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7LD3
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist and an allosteric ligand | | Descriptor: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A. | | Deposit date: | 2021-01-12 | | Release date: | 2021-09-08 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
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7LD4
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist | | Descriptor: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A. | | Deposit date: | 2021-01-12 | | Release date: | 2021-09-08 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
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7LLL
 | | Exendin-4-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein | | Descriptor: | Exendin-4, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Wootten, D, Sexton, P.M, Belousoff, M.J, Danev, R, Zhang, X, Khoshouei, M, Venugopal, H. | | Deposit date: | 2021-02-04 | | Release date: | 2022-01-12 | | Last modified: | 2022-01-26 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nat Commun, 13, 2022
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7LLY
 | | Oxyntomodulin-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein | | Descriptor: | Glucagon-like peptide 1 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: | Wootten, D, Sexton, P.M, Belousoff, M.J, Danev, R, Zhang, X, Khoshouei, M, Venugopal, H. | | Deposit date: | 2021-02-04 | | Release date: | 2022-01-12 | | Last modified: | 2022-01-26 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nat Commun, 13, 2022
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7RTB
 | | Peptide-19 bound to the Glucagon-Like Peptide-1 Receptor (GLP-1R) | | Descriptor: | Glucagon-like peptide 1 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: | Johnson, R.M, Danev, R, Sexton, P.M, Wootten, D. | | Deposit date: | 2021-08-12 | | Release date: | 2021-10-06 | | Method: | ELECTRON MICROSCOPY (2.14 Å) | | Cite: | Cryo-EM structure of the dual incretin receptor agonist, peptide-19, in complex with the glucagon-like peptide-1 receptor.
Biochem.Biophys.Res.Commun., 578, 2021
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6KPF
 | | Cryo-EM structure of a class A GPCR with G protein complex | | Descriptor: | 7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]- 7-methyloctanenitrile, Cannabinoid receptor 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, X.T, Hua, T, Wu, L.J, Makriyannis, A, Shen, L, Wang, Y.X, Liu, Z.J. | | Deposit date: | 2019-08-15 | | Release date: | 2020-02-12 | | Last modified: | 2022-04-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
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7RMI
 | | SP6-11 biased agonist bound to active human neurokinin 1 receptor in complex with miniGs/q70 | | 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, ... | | Authors: | Harris, J.A, Faust, B, Gondin, A.B, Daemgen, M.A, Suomivuori, C.M, Veldhuis, N.A, Cheng, Y, Dror, R.O, Thal, D, Manglik, A. | | Deposit date: | 2021-07-27 | | Release date: | 2021-11-03 | | Last modified: | 2022-01-05 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Selective G protein signaling driven by substance P-neurokinin receptor dynamics.
Nat.Chem.Biol., 18, 2022
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7RMG
 | | Substance P bound to active human neurokinin 1 receptor in complex with miniGs/q70 | | 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, ... | | Authors: | Harris, J.A, Faust, B, Gondin, A.B, Daemgen, M.A, Suomivuori, C.M, Veldhuis, N.A, Cheng, Y, Dror, R.O, Thal, D, Manglik, A. | | Deposit date: | 2021-07-27 | | Release date: | 2021-11-03 | | Last modified: | 2022-01-05 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Selective G protein signaling driven by substance P-neurokinin receptor dynamics.
Nat.Chem.Biol., 18, 2022
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7RMH
 | | Substance P bound to active human neurokinin 1 receptor in complex with miniGs399 | | 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, ... | | Authors: | Harris, J.A, Faust, B, Gondin, A.B, Daemgen, M.A, Suomivuori, C.M, Veldhuis, N.A, Cheng, Y, Dror, R.O, Thal, D, Manglik, A. | | Deposit date: | 2021-07-27 | | Release date: | 2021-11-03 | | Last modified: | 2022-01-05 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Selective G protein signaling driven by substance P-neurokinin receptor dynamics.
Nat.Chem.Biol., 18, 2022
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6KPG
 | | Cryo-EM structure of CB1-G protein complex | | Descriptor: | (6~{a}~{R},9~{R},10~{a}~{R})-9-(hydroxymethyl)-3-(8-isothiocyanato-2-methyl-octan-2-yl)-6,6-dimethyl-6~{a},7,8,9,10,10~{a}-hexahydrobenzo[c]chromen-1-ol, Cannabinoid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hua, T, Li, X.T, Wu, L.J, Makriyannis, A, Wang, Y.X, Shen, L, Liu, Z.J. | | Deposit date: | 2019-08-15 | | Release date: | 2020-02-12 | | Last modified: | 2020-03-11 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
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6LFM
 | | Cryo-EM structure of a class A GPCR | | Descriptor: | C-X-C chemokine receptor type 2, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, Z.J, Hua, T, Liu, K.W, Wu, L.J. | | Deposit date: | 2019-12-03 | | Release date: | 2020-09-02 | | Last modified: | 2020-09-16 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structural basis of CXC chemokine receptor 2 activation and signalling.
Nature, 585, 2020
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6LFO
 | | Cryo-EM structure of a class A GPCR monomer | | Descriptor: | C-X-C chemokine receptor type 2, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, Z.J, Hua, T, Liu, K.W, Wu, L.J. | | Deposit date: | 2019-12-03 | | Release date: | 2020-09-02 | | Last modified: | 2020-09-16 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural basis of CXC chemokine receptor 2 activation and signalling.
Nature, 585, 2020
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7AUE
 | | 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
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5HE1
 | | 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
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