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3PVU
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Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101)
分子名称: 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.48 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
1GG2
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G PROTEIN HETEROTRIMER MUTANT GI_ALPHA_1(G203A) BETA_1 GAMMA_2 WITH GDP BOUND
分子名称: G PROTEIN GI ALPHA 1, G PROTEIN GI BETA 1, G PROTEIN GI GAMMA 2, ...
著者Wall, M.A, Sprang, S.R.
登録日1996-11-13
公開日1997-02-12
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献The structure of the G protein heterotrimer Gi alpha 1 beta 1 gamma 2.
Cell(Cambridge,Mass.), 83, 1995
1GOT
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HETEROTRIMERIC COMPLEX OF A GT-ALPHA/GI-ALPHA CHIMERA AND THE GT-BETA-GAMMA SUBUNITS
分子名称: GT-ALPHA/GI-ALPHA CHIMERA, GT-BETA, GT-GAMMA, ...
著者Lambright, D.G, Sondek, J, Bohm, A, Skiba, N.P, Hamm, H.E, Sigler, P.B.
登録日1996-08-07
公開日1997-03-12
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献The 2.0 A crystal structure of a heterotrimeric G protein.
Nature, 379, 1996
3PVW
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Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD103A)
分子名称: 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, ...
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.49 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
1GP2
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G PROTEIN HETEROTRIMER GI_ALPHA_1 BETA_1 GAMMA_2 WITH GDP BOUND
分子名称: G PROTEIN GI ALPHA 1, G PROTEIN GI BETA 1, G PROTEIN GI GAMMA 2, ...
著者Wall, M.A, Sprang, S.R.
登録日1996-11-13
公開日1997-02-12
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The structure of the G protein heterotrimer Gi alpha 1 beta 1 gamma 2.
Cell(Cambridge,Mass.), 83, 1995
4PNK
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G protein-coupled receptor kinase 2 in complex with GSK180736A
分子名称: (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, ...
著者Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G.
登録日2014-05-23
公開日2014-10-08
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.56 Å)
主引用文献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
分子名称: (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, ...
著者Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G.
登録日2016-01-05
公開日2016-05-11
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.56 Å)
主引用文献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
分子名称: (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, ...
著者Cato, M.C, Tesmer, J.J.G.
登録日2016-01-05
公開日2016-05-11
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.74 Å)
主引用文献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
分子名称: (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, ...
著者Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G.
登録日2016-01-05
公開日2016-05-11
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.79 Å)
主引用文献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
分子名称: (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, ...
著者Cato, M.C, Tesmer, J.J.G.
登録日2016-01-05
公開日2016-05-11
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (3.15 Å)
主引用文献Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J.Med.Chem., 59, 2016
6B3J
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BU of 6b3j by Molmil
3.3 angstrom phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex
分子名称: Exendin-P5, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者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.
登録日2017-09-22
公開日2018-02-21
最終更新日2020-01-15
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.
Nature, 555, 2018
6B20
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Crystal structure of a complex between G protein beta gamma dimer and an inhibitory Nanobody regulator
分子名称: CHLORIDE ION, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(T) subunit gamma-T1, ...
著者Gulati, S, Kiser, P.D, Palczewski, K.
登録日2017-09-19
公開日2018-05-30
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.34 Å)
主引用文献Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor.
Nat Commun, 9, 2018
6C2Y
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Human GRK2 in complex with Gbetagamma subunits and CCG257142
分子名称: (4R,5R,6S)-4-[4-fluoro-3-({[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl]methyl}carbamoyl)phenyl]-N-(2H-indazol-5-yl)-6-methyl-2-oxohexahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2018-01-09
公開日2018-04-25
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.74 Å)
主引用文献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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BU of 6crk by Molmil
Heterotrimeric G-protein in complex with an antibody fragment
分子名称: CITRATE ANION, GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Maeda, S, Dawson, R, Kobilka, B.
登録日2018-03-19
公開日2018-10-24
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Development of an antibody fragment that stabilizes GPCR/G-protein complexes.
Nat Commun, 9, 2018
6CMO
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BU of 6cmo by Molmil
Rhodopsin-Gi complex
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Fab Heavy chain, Fab light chain, ...
著者Kang, Y, Kuybeda, O, de Waal, P.W, Mukherjee, S, Van Eps, N, Dutka, P, Zhou, X.E, Bartesaghi, A, Erramilli, S, Morizumi, T, Gu, X, Yin, Y, Liu, P, Jiang, Y, Meng, X, Zhao, G, Melcher, K, Earnst, O.P, Kossiakoff, A.A, Subramaniam, S, Xu, H.E.
登録日2018-03-05
公開日2018-06-20
最終更新日2020-07-29
実験手法ELECTRON MICROSCOPY (4.5 Å)
主引用文献Cryo-EM structure of human rhodopsin bound to an inhibitory G protein.
Nature, 558, 2018
6D9H
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BU of 6d9h by Molmil
Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist
分子名称: 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, ...
著者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.
登録日2018-04-29
公開日2018-06-20
最終更新日2018-07-11
実験手法ELECTRON MICROSCOPY (3.6 Å)
主引用文献Structure of the adenosine-bound human adenosine A1receptor-Gicomplex.
Nature, 558, 2018
6DDE
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BU of 6dde by Molmil
Mu Opioid Receptor-Gi Protein Complex
分子名称: DAMGO, 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, ...
著者Koehl, A, Hu, H, Maeda, S, Manglik, A, Zhang, Y, Kobilka, B.K, Skiniotis, G, Weis, W.I.
登録日2018-05-10
公開日2018-06-13
最終更新日2023-11-15
実験手法ELECTRON MICROSCOPY (3.5 Å)
主引用文献Structure of the mu-opioid receptor-Giprotein complex.
Nature, 558, 2018
6DDF
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Mu Opioid Receptor-Gi Protein Complex
分子名称: DAMGO, 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, ...
著者Koehl, A, Hu, H, Maeda, S, Manglik, A, Kobilka, B.K, Skiniotis, G, Weis, W.I.
登録日2018-05-10
公開日2018-06-13
最終更新日2023-11-15
実験手法ELECTRON MICROSCOPY (3.5 Å)
主引用文献Structure of the mu-opioid receptor-Giprotein complex.
Nature, 558, 2018
6E3Y
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BU of 6e3y by Molmil
Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor
分子名称: Calcitonin gene-related peptide 1, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者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.
登録日2018-07-16
公開日2018-09-19
最終更新日2020-01-15
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.
Nature, 561, 2018
6EG8
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Structure of the GDP-bound Gs heterotrimer
分子名称: 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, ...
著者Hilger, D, Liu, X, Aschauer, P, Kobilka, B.K.
登録日2018-08-19
公開日2019-06-05
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Structural Insights into the Process of GPCR-G Protein Complex Formation.
Cell, 177, 2019
6G79
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Coupling specificity of heterotrimeric Go to the serotonin 5-HT1B receptor
分子名称: 2-[5-[2-[4-(4-cyanophenyl)piperazin-1-yl]-2-oxidanylidene-ethoxy]-1~{H}-indol-3-yl]ethylazanium, 5-hydroxytryptamine receptor 1B, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Garcia-Nafria, J, Nehme, R, Edwards, P, Tate, C.G.
登録日2018-04-05
公開日2018-06-20
最終更新日2019-12-11
実験手法ELECTRON MICROSCOPY (3.78 Å)
主引用文献Cryo-EM structure of the serotonin 5-HT1Breceptor coupled to heterotrimeric Go.
Nature, 558, 2018
6GDG
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Cryo-EM structure of the adenosine A2A receptor bound to a miniGs heterotrimer
分子名称: 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, ...
著者Garcia-Nafria, J, Lee, Y.
登録日2018-04-23
公開日2018-05-16
最終更新日2019-12-18
実験手法ELECTRON MICROSCOPY (4.11 Å)
主引用文献Cryo-EM structure of the adenosine A2Areceptor coupled to an engineered heterotrimeric G protein.
Elife, 7, 2018
7LLY
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Oxyntomodulin-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein
分子名称: 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, ...
著者Wootten, D, Sexton, P.M, Belousoff, M.J, Danev, R, Zhang, X, Khoshouei, M, Venugopal, H.
登録日2021-02-04
公開日2022-01-12
最終更新日2022-01-26
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nat Commun, 13, 2022
7LLL
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Exendin-4-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein
分子名称: Exendin-4, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Wootten, D, Sexton, P.M, Belousoff, M.J, Danev, R, Zhang, X, Khoshouei, M, Venugopal, H.
登録日2021-02-04
公開日2022-01-12
最終更新日2022-01-26
実験手法ELECTRON MICROSCOPY (3.7 Å)
主引用文献Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nat Commun, 13, 2022
7MTS
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CryoEM Structure of mGlu2 - Gi Complex
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine, GLUTAMIC ACID, ...
著者Seven, A.B, Barros-Alvarez, X, Skiniotis, G.
登録日2021-05-13
公開日2021-07-07
最終更新日2021-07-28
実験手法ELECTRON MICROSCOPY (3.2 Å)
主引用文献G-protein activation by a metabotropic glutamate receptor.
Nature, 595, 2021

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