7P02
 
 | | 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
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6QNO
 | | Rhodopsin-Gi protein complex | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Fab antibody fragment heavy chain, Fab antibody fragment light chain, ... | | 著者 | Tsai, C.-J, Marino, J, Adaixo, R.J, Pamula, F, Muehle, J, Maeda, S, Flock, T, Taylor, N.M.I, Mohammed, I, Matile, H, Dawson, R.J.P, Deupi, X, Stahlberg, H, Schertler, G.F.X. | | 登録日 | 2019-02-11 | | 公開日 | 2019-07-10 | | 最終更新日 | 2020-07-29 | | 実験手法 | ELECTRON MICROSCOPY (4.38 Å) | | 主引用文献 | Cryo-EM structure of the rhodopsin-G alpha i-beta gamma complex reveals binding of the rhodopsin C-terminal tail to the G beta subunit.
Elife, 8, 2019
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7PWD
 | | 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 | 2024-06-19 | | 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
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7PIU
 | | 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
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7PIV
 | | 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
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6PT0
 | | Cryo-EM structure of human cannabinoid receptor 2-Gi protein in complex with agonist WIN 55,212-2 | | 分子名称: | CHOLESTEROL, Cannabinoid receptor 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Xu, T.H, Xing, C, Zhuang, Y, Feng, Z, Zhou, X.E, Chen, M, Wang, L, Meng, X, Xue, Y, Wang, J, Liu, H, McGuire, T, Zhao, G, Melcher, K, Zhang, C, Xu, H.E, Xie, X.Q. | | 登録日 | 2019-07-14 | | 公開日 | 2020-02-12 | | 最終更新日 | 2020-03-04 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Cryo-EM Structure of the Human Cannabinoid Receptor CB2-GiSignaling Complex.
Cell, 180, 2020
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6RMV
 | | The crystal structure of a TRP channel peptide bound to a G protein beta gamma heterodimer | | 分子名称: | 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, ... | | 著者 | Gruss, F, Oberwinkler, J, Ulens, C. | | 登録日 | 2019-05-07 | | 公開日 | 2020-10-14 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.94 Å) | | 主引用文献 | The structural basis for an on-off switch controlling G beta gamma-mediated inhibition of TRPM3 channels.
Proc.Natl.Acad.Sci.USA, 117, 2020
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6U7C
 | | Human GRK2 in complex with Gbetagamma subunits and CCG258747 | | 分子名称: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-3-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 | 2019-09-02 | | 公開日 | 2020-04-15 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.44 Å) | | 主引用文献 | A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor.
Mol.Pharmacol., 97, 2020
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6UUS
 | | CryoEM Structure of the active Adrenomedullin 2 receptor G protein complex with adrenomedullin peptide | | 分子名称: | ADM, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-10-31 | | 公開日 | 2020-04-01 | | 最終更新日 | 2020-04-29 | | 実験手法 | ELECTRON MICROSCOPY (2.4 Å) | | 主引用文献 | Structure and Dynamics of Adrenomedullin Receptors AM1and AM2Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins.
Acs Pharmacol Transl Sci, 3, 2020
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6UVA
 | | CryoEM Structure of the active Adrenomedullin 2 receptor G protein complex with adrenomedullin 2 peptide | | 分子名称: | Calcitonin gene-related peptide type 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 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-11-01 | | 公開日 | 2020-04-01 | | 最終更新日 | 2020-04-29 | | 実験手法 | ELECTRON MICROSCOPY (2.3 Å) | | 主引用文献 | Structure and Dynamics of Adrenomedullin Receptors AM1and AM2Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins.
Acs Pharmacol Transl Sci, 3, 2020
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6UUN
 | | CryoEM Structure of the active Adrenomedullin 1 receptor G protein complex with adrenomedullin peptide | | 分子名称: | ADM, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-10-30 | | 公開日 | 2020-03-25 | | 最終更新日 | 2020-04-29 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structure and Dynamics of Adrenomedullin Receptors AM1and AM2Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins.
Acs Pharmacol Transl Sci, 3, 2020
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6VCB
 | | Cryo-EM structure of the Glucagon-like peptide-1 receptor in complex with G protein, GLP-1 peptide and a positive allosteric modulator | | 分子名称: | 1-[(1R)-1-(2,6-dichloro-3-methoxyphenyl)ethyl]-6-{2-[(2R)-piperidin-2-yl]phenyl}-1H-benzimidazole, Glucagon-like peptide 1, Glucagon-like peptide 1 receptor, ... | | 著者 | Sun, B, Feng, D, Bueno, A, Kobilka, B, Sloop, K. | | 登録日 | 2019-12-20 | | 公開日 | 2020-07-22 | | 最終更新日 | 2020-09-30 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Structural insights into probe-dependent positive allosterism of the GLP-1 receptor.
Nat.Chem.Biol., 16, 2020
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6VN7
 | | Cryo-EM structure of an activated VIP1 receptor-G protein complex | | 分子名称: | CHOLESTEROL, 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 | Duan, J, Shen, D.-D, Zhou, X.E, Liu, Q.-F, Zhuang, Y.-W, Zhang, H.-B, Xu, P.-Y, Ma, S.-S, He, X.-H, Melcher, K, Zhang, Y, Xu, H.E, Yi, J. | | 登録日 | 2020-01-29 | | 公開日 | 2020-09-02 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy.
Nat Commun, 11, 2020
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6CRK
 | | 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
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6DDE
 | | 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
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6D9H
 | | 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
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6CMO
 | | 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
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6EG8
 | | 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
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6DDF
 | | 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
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6E3Y
 | | 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
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5UKM
 | | 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
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5UZ7
 | | 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
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5UKK
 | | 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
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5WG4
 | | 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
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5WG5
 | | 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
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