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6KPF
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Cryo-EM structure of a class A GPCR with G protein complex
分子名称: 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, ...
著者Li, X.T, Hua, T, Wu, L.J, Makriyannis, A, Shen, L, Wang, Y.X, Liu, Z.J.
登録日2019-08-15
公開日2020-02-12
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (2.9 Å)
主引用文献Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
6KPG
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Cryo-EM structure of CB1-G protein complex
分子名称: (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, ...
著者Hua, T, Li, X.T, Wu, L.J, Makriyannis, A, Wang, Y.X, Shen, L, Liu, Z.J.
登録日2019-08-15
公開日2020-02-12
最終更新日2020-03-11
実験手法ELECTRON MICROSCOPY (3 Å)
主引用文献Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
6LFM
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Cryo-EM structure of a class A GPCR
分子名称: C-X-C chemokine receptor type 2, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Liu, Z.J, Hua, T, Liu, K.W, Wu, L.J.
登録日2019-12-03
公開日2020-09-02
最終更新日2020-09-16
実験手法ELECTRON MICROSCOPY (3.5 Å)
主引用文献Structural basis of CXC chemokine receptor 2 activation and signalling.
Nature, 585, 2020
6LFO
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Cryo-EM structure of a class A GPCR monomer
分子名称: C-X-C chemokine receptor type 2, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Liu, Z.J, Hua, T, Liu, K.W, Wu, L.J.
登録日2019-12-03
公開日2020-09-02
最終更新日2020-09-16
実験手法ELECTRON MICROSCOPY (3.4 Å)
主引用文献Structural basis of CXC chemokine receptor 2 activation and signalling.
Nature, 585, 2020
6LI3
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cryo-EM structure of GPR52-miniGs-NB35
分子名称: G-protein coupled receptor 52, 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Li, M, Wang, N, Xu, F, Wu, J, Lei, M.
登録日2019-12-10
公開日2020-02-26
最終更新日2020-03-18
実験手法ELECTRON MICROSCOPY (3.32 Å)
主引用文献Structural basis of ligand recognition and self-activation of orphan GPR52.
Nature, 579, 2020
6B3J
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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
7P02
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Human Neurokinin 1 receptor (NK1R) substance P Gs complex
分子名称: Antibody fragment scFv16, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Thom, C, Ehrenmann, J, Vacca, S, Waltenspuhl, Y, Schoppe, J, Medalia, O, Pluckthun, A.
登録日2021-06-29
公開日2021-12-15
実験手法ELECTRON MICROSCOPY (2.87 Å)
主引用文献Structures of neurokinin 1 receptor in complex with G q and G s proteins reveal substance P binding mode and unique activation features.
Sci Adv, 7, 2021
7P00
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Human Neurokinin 1 receptor (NK1R) substance P Gq chimera (mGsqi) complex
分子名称: Antibody fragment scFv16, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Thom, C, Ehrenmann, J, Vacca, S, Waltenspuhl, Y, Schoppe, J, Medalia, O, Pluckthun, A.
登録日2021-06-29
公開日2021-12-15
実験手法ELECTRON MICROSCOPY (2.71 Å)
主引用文献Structures of neurokinin 1 receptor in complex with G q and G s proteins reveal substance P binding mode and unique activation features.
Sci Adv, 7, 2021
6LML
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Cryo-EM structure of the human glucagon receptor in complex with Gi1
分子名称: Glucagon, Glucagon receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Qiao, A, Han, S, Li, X, Sun, F, Zhao, Q, Wu, B.
登録日2019-12-26
公開日2020-04-01
実験手法ELECTRON MICROSCOPY (3.9 Å)
主引用文献Structural basis of Gsand Girecognition by the human glucagon receptor.
Science, 367, 2020
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
6LPB
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Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein
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Kobayashi, K, Shihoya, W, Nishizawa, T, Nureki, O.
登録日2020-01-09
公開日2020-03-11
最終更新日2020-03-25
実験手法ELECTRON MICROSCOPY (3.9 Å)
主引用文献Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein.
Nat.Struct.Mol.Biol., 27, 2020
7PWD
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Structure of an inhibited GRK2-G-beta and G-gamma complex
分子名称: 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ...
著者Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M.
登録日2021-10-06
公開日2021-10-20
最終更新日2022-05-18
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Monatsh Chem, 2022
7PIU
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Cryo-EM structure of the agonist setmelanotide bound to the active melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein at 2.6 A resolution.
分子名称: CALCIUM ION, Camelid antibody fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P.
登録日2021-08-23
公開日2021-11-17
実験手法ELECTRON MICROSCOPY (2.58 Å)
主引用文献Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
7PIV
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Active Melanocortin-4 receptor (MC4R)- Gs protein complex bound to agonist NDP-alpha-MSH at 2.86 A resolution.
分子名称: CALCIUM ION, Camelid antibody VHH fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P.
登録日2021-08-23
公開日2021-11-17
実験手法ELECTRON MICROSCOPY (2.86 Å)
主引用文献Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
6CRK
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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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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
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
5UKM
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bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as)
分子名称: 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(1H-pyrazol-5-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Cruz-Rodriguez, O, Tesmer, J.J.G.
登録日2017-01-23
公開日2017-04-12
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (3.03 Å)
主引用文献Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
5WG5
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Human GRK2 in complex with Gbetagamma subunits and CCG224061
分子名称: 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, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2017-07-13
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献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
分子名称: 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, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2017-07-13
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.31 Å)
主引用文献Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
5UKK
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Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak)
分子名称: 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(pyridin-2-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Cato, M.C, Homan, K.T, Tesmer, J.J.G.
登録日2017-01-23
公開日2017-04-05
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
5UZ7
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Volta phase plate cryo-electron microscopy structure of a calcitonin receptor-heterotrimeric Gs protein complex
分子名称: Calcitonin 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Liang, Y.L, Khoshouei, M, Radjainia, M, Zhang, Y, Glukhova, A, Tarrasch, J, Thal, D.M, Furness, S.G.B, Christopoulos, G, Coudrat, T, Danev, R, Baumeister, W, Miller, L.J, Christopoulos, A, Kobilka, B.K, Wootten, D, Skiniotis, G, Sexton, P.M.
登録日2017-02-24
公開日2017-05-03
最終更新日2018-07-18
実験手法ELECTRON MICROSCOPY (4.1 Å)
主引用文献Phase-plate cryo-EM structure of a class B GPCR-G-protein complex.
Nature, 546, 2017
5VAI
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Cryo-EM structure of the activated Glucagon-like peptide-1 receptor in complex with G protein
分子名称: Glucagon-like peptide 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Zhang, Y, Sun, B, Feng, D, Hu, H, Chu, M, Qu, Q, Tarrasch, J.T, Li, S, Kobilka, T.S, Kobilka, B.K, Skiniotis, G.
登録日2017-03-27
公開日2017-05-24
最終更新日2019-12-18
実験手法ELECTRON MICROSCOPY (4.1 Å)
主引用文献Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein.
Nature, 546, 2017
5UKL
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Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd)
分子名称: 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Cato, M.C, Homan, K.T, Tesmer, J.J.G.
登録日2017-01-23
公開日2017-04-05
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.15 Å)
主引用文献Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
5TDH
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The crystal structure of the dominant negative mutant G protein alpha(i)-1-beta-1-gamma-2 G203A/A326S
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Liu, P, Jia, M.-Z, Zhou, X.E, de Waal, P.W, Dickson, B.M, Liu, B, Hou, L, Yin, Y.-T, Kang, Y.-Y, Shi, Y, Melcher, K, Xu, H.E, Jiang, Y.
登録日2016-09-19
公開日2016-11-09
最終更新日2024-03-20
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献The structural basis of the dominant negative phenotype of the G alpha i1 beta 1 gamma 2 G203A/A326S heterotrimer
Acta Pharmacol.Sin., 37, 2016

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