8EIT
 
 | | Structure of FFAR1-Gq complex bound to DHA | | Descriptor: | A modified Guanine nucleotide-binding protein G(q) subunit alpha, DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, Free fatty acid receptor 1, ... | | Authors: | Kumari, P, Inoue, A, Chapman, K, Lian, P, Rosenbaum, D.M. | | Deposit date: | 2022-09-15 | | Release date: | 2023-05-24 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Molecular mechanism of fatty acid activation of FFAR1.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8EJC
 | | Structure of FFAR1-Gq complex bound to TAK-875 | | Descriptor: | A modified Guanine nucleotide-binding protein G(q) subunit alpha, Free fatty acid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Kumari, P, Inoue, A, Chapman, K, Lian, P, Rosenbaum, D.M. | | Deposit date: | 2022-09-16 | | Release date: | 2023-05-24 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Molecular mechanism of fatty acid activation of FFAR1.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8EJK
 | | Structure of FFAR1-Gq complex bound to TAK-875 in a lipid nanodisc | | Descriptor: | A modified Guanine nucleotide-binding protein G(q) subunit alpha, Free fatty acid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Kumari, P, Inoue, A, Chapman, K, Lian, P, Rosenbaum, D.M. | | Deposit date: | 2022-09-17 | | Release date: | 2023-05-24 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Molecular mechanism of fatty acid activation of FFAR1.
Proc.Natl.Acad.Sci.USA, 120, 2023
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7EO4
 | | Cryo-EM of Sphingosine 1-phosphate receptor 1 / Gi complex bound to BAF312 | | Descriptor: | 1-[[4-[(~{E})-~{N}-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-~{C}-methyl-carbonimidoyl]-2-ethyl-phenyl]methyl]azetidine-3-carboxylic acid, 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: | He, Y, Xu, Z, Ikuta, T, Inoue, A. | | Deposit date: | 2021-04-21 | | Release date: | 2022-01-05 | | Last modified: | 2022-03-16 | | Method: | ELECTRON MICROSCOPY (2.86 Å) | | Cite: | Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism.
Nat.Chem.Biol., 18, 2022
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6A94
 | | Crystal structure of 5-HT2AR in complex with zotepine | | Descriptor: | 2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-(3-chloranylbenzo[b][1]benzothiepin-5-yl)oxy-N,N-dimethyl-ethanamine, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, ... | | Authors: | Kimura, T.K, Asada, H, Inoue, A, Kadji, F.M.N, Im, D, Mori, C, Arakawa, T, Hirata, K, Nomura, Y, Nomura, N, Aoki, J, Iwata, S, Shimamura, T. | | Deposit date: | 2018-07-11 | | Release date: | 2019-02-13 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structures of the 5-HT2Areceptor in complex with the antipsychotics risperidone and zotepine.
Nat.Struct.Mol.Biol., 26, 2019
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6A93
 | | Crystal structure of 5-HT2AR in complex with risperidone | | Descriptor: | 3-[2-[4-(6-fluoranyl-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, CHOLESTEROL, ... | | Authors: | Kimura, T.K, Asada, H, Inoue, A, Kadji, F.M.N, Im, D, Mori, C, Arakawa, T, Hirata, K, Nomura, Y, Nomura, N, Aoki, J, Iwata, S, Shimamura, T. | | Deposit date: | 2018-07-11 | | Release date: | 2019-02-13 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structures of the 5-HT2Areceptor in complex with the antipsychotics risperidone and zotepine.
Nat.Struct.Mol.Biol., 26, 2019
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6IGK
 | | Crystal Structure of human ETB receptor in complex with Endothelin-3 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CITRIC ACID, Endothelin receptor type B,Endolysin,Endothelin receptor type B, ... | | Authors: | Shihoya, W, Izume, T, Inoue, A, Yamashita, K, Kadji, F.M.N, Hirata, K, Aoki, J, Nishizawa, T, Nureki, O. | | Deposit date: | 2018-09-25 | | Release date: | 2018-11-21 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structures of human ETBreceptor provide mechanistic insight into receptor activation and partial activation.
Nat Commun, 9, 2018
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6IGL
 | | Crystal Structure of human ETB receptor in complex with IRL1620 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CITRIC ACID, Endothelin receptor type B,Endolysin,Endothelin receptor type B, ... | | Authors: | Shihoya, W, Izume, T, Inoue, A, Yamashita, K, kadji, F.M.N, Hirata, K, Aoki, J, Nishizawa, T, Nureki, O. | | Deposit date: | 2018-09-25 | | Release date: | 2018-11-21 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystal structures of human ETBreceptor provide mechanistic insight into receptor activation and partial activation.
Nat Commun, 9, 2018
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3WZE
 | | KDR in complex with ligand sorafenib | | Descriptor: | 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, ACETATE ION, ... | | Authors: | Okamoto, K, Ikemori_Kawada, M, Inoue, A, Matsui, J. | | Deposit date: | 2014-09-24 | | Release date: | 2015-05-27 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.
ACS MED.CHEM.LETT., 6, 2015
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3WZD
 | | KDR in complex with ligand lenvatinib | | Descriptor: | 1,2-ETHANEDIOL, 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide, ... | | Authors: | Okamoto, K, Ikemori_Kawada, M, Inoue, A, Matsui, J. | | Deposit date: | 2014-09-24 | | Release date: | 2015-05-27 | | Method: | X-RAY DIFFRACTION (1.57 Å) | | Cite: | Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.
ACS MED.CHEM.LETT., 6, 2015
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3WGW
 | | Structure of PCNA bound to a small molecule inhibitor | | Descriptor: | 4-{4-[(2S)-2-amino-3-hydroxypropyl]-2,6-diiodophenoxy}phenol, Proliferating cell nuclear antigen, SULFATE ION | | Authors: | Hashimoto, H. | | Deposit date: | 2013-08-12 | | Release date: | 2014-02-05 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | A small molecule inhibitor of monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA) inhibits repair of interstrand DNA cross-link, enhances DNA double strand break, and sensitizes cancer cells to cisplatin.
J.Biol.Chem., 289, 2014
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8WW2
 | | GPR3/Gs complex | | Descriptor: | CHOLESTEROL HEMISUCCINATE, G-protein coupled receptor 3, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | He, Y, Xiong, Y. | | Deposit date: | 2023-10-24 | | Release date: | 2024-02-14 | | Last modified: | 2024-03-20 | | Method: | ELECTRON MICROSCOPY (2.79 Å) | | Cite: | Identification of oleic acid as an endogenous ligand of GPR3.
Cell Res., 34, 2024
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6ORV
 | | Non-peptide agonist (TT-OAD2) bound to the Glucagon-Like peptide-1 (GLP-1) Receptor | | 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: | Belousoff, M.J, Liang, Y.L, Danev, R. | | Deposit date: | 2019-05-01 | | Release date: | 2020-01-08 | | Last modified: | 2020-01-29 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Activation of the GLP-1 receptor by a non-peptidic agonist.
Nature, 577, 2020
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6OSA
 | | human Neurotensin Receptor 1 (hNTSR1) - Gi1 Protein Complex in non-canonical conformation (NC state) | | 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(i) subunit alpha-1, ... | | Authors: | Kato, H.E, Zhang, Y, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2019-05-01 | | Release date: | 2019-07-10 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Conformational transitions of a neurotensin receptor 1-Gi1complex.
Nature, 572, 2019
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6OS9
 | | human Neurotensin Receptor 1 (hNTSR1) - Gi1 Protein Complex in canonical conformation (C state) | | 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(i) subunit alpha-1, ... | | Authors: | Kato, H.E, Zhang, Y, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2019-05-01 | | Release date: | 2019-07-10 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Conformational transitions of a neurotensin receptor 1-Gi1complex.
Nature, 572, 2019
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6UP7
 | | neurotensin receptor and arrestin2 complex | | Descriptor: | ARG-ARG-PRO-TYR-ILE-LEU, Beta-arrestin-1, Neurotensin receptor type 1, ... | | Authors: | Qu, Q.H, Huang, W, Masureel, M, Janetzko, J, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2019-10-16 | | Release date: | 2020-02-26 | | Last modified: | 2020-06-17 | | Method: | ELECTRON MICROSCOPY (4.2 Å) | | Cite: | Structure of the neurotensin receptor 1 in complex with beta-arrestin 1.
Nature, 579, 2020
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6WJC
 | | Muscarinic acetylcholine receptor 1 - muscarinic toxin 7 complex | | Descriptor: | (1R,5S)-8-METHYL-8-AZABICYCLO[3.2.1]OCT-3-YL (2R)-3-HYDROXY-2-PHENYLPROPANOATE, ACETAMIDE, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Maeda, S, Kobilka, B.K. | | Deposit date: | 2020-04-13 | | Release date: | 2020-07-08 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Structure and selectivity engineering of the M1muscarinic receptor toxin complex.
Science, 369, 2020
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6WPW
 | | GCGR-Gs signaling complex bound to a designed glucagon derivative | | Descriptor: | Glucagon derivative ZP3780, Glucagon receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hilger, D, Krishna Kumar, K, Hu, H, Mathiesen, J.M, Skiniotis, G, Kobilka, B.K. | | Deposit date: | 2020-04-28 | | Release date: | 2020-08-12 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural insights into differences in G protein activation by family A and family B GPCRs.
Science, 369, 2020
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5GMT
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5X93
 | | Human endothelin receptor type-B in complex with antagonist K-8794 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 3-[6-[(4-tert-butylphenyl)sulfonylamino]-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]oxy-N-(2,6-dimethylphenyl)propanamide, CHOLESTEROL, ... | | Authors: | Shihoya, W, Nishizawa, T, Yamashita, K, Hirata, K, Okuta, A, Tani, K, Fujiyoshi, Y, Doi, T, Nureki, O. | | Deposit date: | 2017-03-05 | | Release date: | 2017-08-16 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog
Nat. Struct. Mol. Biol., 24, 2017
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8IYS
 | | TUG891-bound FFAR4 in complex with Gq | | Descriptor: | 3-{4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]phenyl}propanoic acid, Free fatty acid receptor 4, GUANOSINE-5'-DIPHOSPHATE, ... | | Authors: | He, Y, Yin, H. | | Deposit date: | 2023-04-06 | | Release date: | 2023-06-21 | | Last modified: | 2023-08-16 | | Method: | ELECTRON MICROSCOPY (2.95 Å) | | Cite: | Structural basis of omega-3 fatty acid receptor FFAR4 activation and G protein coupling selectivity.
Cell Res., 33, 2023
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8GHV
 | | Cannabinoid Receptor 1-G Protein Complex | | Descriptor: | (5Z,8Z,11Z,13S,14Z)-N-[(2R)-1-hydroxypropan-2-yl]-13-methylicosa-5,8,11,14-tetraenamide, Cannabinoid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Krishna Kumar, K, Robertson, M.J, Skiniotis, G, Kobilka, B.K. | | Deposit date: | 2023-03-12 | | Release date: | 2023-05-24 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Structural basis for activation of CB1 by an endocannabinoid analog.
Nat Commun, 14, 2023
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8GW8
 | | the human PTH1 receptor bound to an intracellular biased agonist | | 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, Isoform Gnas-2 of Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Kobayashi, K, Kusakizako, T, Okamoto, H.H, Nureki, O. | | Deposit date: | 2022-09-16 | | Release date: | 2023-06-14 | | Last modified: | 2023-09-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Class B1 GPCR activation by an intracellular agonist.
Nature, 618, 2023
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8H4L
 | | DHA-bound FFAR4 in complex with Gq | | Descriptor: | DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, Free fatty acid receptor 4, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | He, Y, Yin, H. | | Deposit date: | 2022-10-10 | | Release date: | 2023-06-21 | | Last modified: | 2023-08-09 | | Method: | ELECTRON MICROSCOPY (3.07 Å) | | Cite: | Structural basis of omega-3 fatty acid receptor FFAR4 activation and G protein coupling selectivity.
Cell Res., 33, 2023
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8H4K
 | | GW9508-bound FFAR4 in complex with Gq | | Descriptor: | 3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propanoic acid, Free fatty acid receptor 4, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | He, Y, Yin, H. | | Deposit date: | 2022-10-10 | | Release date: | 2023-06-21 | | Last modified: | 2023-08-09 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural basis of omega-3 fatty acid receptor FFAR4 activation and G protein coupling selectivity.
Cell Res., 33, 2023
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