6Z10
 
 | | Crystal structure of a humanized (K18E, K269N) rat succinate receptor SUCNR1 (GPR91) in complex with a nanobody and antagonist | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[2-[[3-[4-chloranyl-2-fluoranyl-5-[(3~{R})-piperidin-3-yl]oxy-phenyl]-2-fluoranyl-phenyl]carbonylamino]-5-fluoranyl-phenyl]ethanoic acid, CHLORIDE ION, ... | | 著者 | Haffke, M, Villard, F. | | 登録日 | 2020-05-11 | | 公開日 | 2020-09-16 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.269 Å) | | 主引用文献 | Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
J.Med.Chem., 63, 2020
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2R4S
 | | Crystal structure of the human beta2 adrenoceptor | | 分子名称: | Beta-2 adrenergic receptor, antibody for beta2 adrenoceptor, heavy chain, ... | | 著者 | Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M, Kobilka, T.S, Thian, F.S, Edwards, P.C, Burghammer, M, Ratnala, V.R, Sanishvili, R, Fischetti, R.F, Schertler, G.F, Weis, W.I, Kobilka, B.K. | | 登録日 | 2007-08-31 | | 公開日 | 2007-11-06 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
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2R4R
 | | Crystal structure of the human beta2 adrenoceptor | | 分子名称: | Beta-2 adrenergic receptor, antibody for beta2 adrenoceptor, heavy chain, ... | | 著者 | Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M, Kobilka, T.S, Thian, F.S, Edwards, P.C, Burghammer, M, Ratnala, V.R, Sanishvili, R, Fischetti, R.F, Schertler, G.F, Weis, W.I, Kobilka, B.K. | | 登録日 | 2007-08-31 | | 公開日 | 2007-11-06 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
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2VT4
 | | TURKEY BETA1 ADRENERGIC RECEPTOR WITH STABILISING MUTATIONS AND BOUND CYANOPINDOLOL | | 分子名称: | 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile, BETA1 ADRENERGIC RECEPTOR, DECANE, ... | | 著者 | Warne, A, Serrano-Vega, M.J, Baker, J.G, Moukhametzianov, R, Edwards, P.C, Henderson, R, Leslie, A.G.W, Tate, C.G, Schertler, G.F.X. | | 登録日 | 2008-05-09 | | 公開日 | 2008-06-24 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Structure of a Beta1-Adrenergic G-Protein-Coupled Receptor.
Nature, 454, 2008
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2LNL
 | | Structure of human CXCR1 in phospholipid bilayers | | 分子名称: | C-X-C chemokine receptor type 1 | | 著者 | Park, S, Das, B.B, Casagrande, F, Nothnagel, H, Chu, M, Kiefer, H, Maier, K, De Angelis, A, Marassi, F.M, Opella, S.J. | | 登録日 | 2011-12-31 | | 公開日 | 2012-10-17 | | 最終更新日 | 2016-04-27 | | 実験手法 | SOLID-STATE NMR | | 主引用文献 | Structure of the chemokine receptor CXCR1 in phospholipid bilayers.
Nature, 491, 2012
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5LWE
 | | Crystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with vercirnon | | 分子名称: | C-C chemokine receptor type 9, CHOLESTEROL, MALONATE ION, ... | | 著者 | Oswald, C, Rappas, M, Kean, J, Dore, A.S, Errey, J.C, Bennett, K, Deflorian, F, Christopher, J.A, Jazayeri, A, Mason, J.S, Congreve, M, Cooke, R.M, Marshall, F.H. | | 登録日 | 2016-09-16 | | 公開日 | 2016-12-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Intracellular allosteric antagonism of the CCR9 receptor.
Nature, 540, 2016
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5YHL
 | | Crystal structure of the human prostaglandin E receptor EP4 in complex with Fab and an antagonist Br-derivative | | 分子名称: | 4-[2-[[(2R)-2-(4-bromanylnaphthalen-1-yl)propanoyl]amino]-4-cyano-phenyl]butanoic acid, Heavy chain of Fab fragment, Light chain of Fab fragment, ... | | 著者 | Toyoda, Y, Morimoto, K, Suno, R, Horita, S, Iwata, S, Kobayashi, T. | | 登録日 | 2017-09-28 | | 公開日 | 2018-12-05 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (4.2 Å) | | 主引用文献 | Ligand binding to human prostaglandin E receptor EP4at the lipid-bilayer interface.
Nat. Chem. Biol., 15, 2019
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5YWY
 | | Crystal structure of the human prostaglandin E receptor EP4 in complex with Fab and ONO-AE3-208 | | 分子名称: | 4-[4-cyano-2-[[(2R)-2-(4-fluoranylnaphthalen-1-yl)propanoyl]amino]phenyl]butanoic acid, Heavy chain of Fab fragment, Light chain of Fab fragment, ... | | 著者 | Toyoda, Y, Morimoto, K, Suno, R, Horita, S, Iwata, S, Kobayashi, T. | | 登録日 | 2017-11-30 | | 公開日 | 2018-12-05 | | 最終更新日 | 2018-12-19 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Ligand binding to human prostaglandin E receptor EP4at the lipid-bilayer interface.
Nat. Chem. Biol., 15, 2019
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3KJ6
 | | Crystal structure of a Methylated beta2 Adrenergic Receptor-Fab complex | | 分子名称: | Beta-2 adrenergic receptor, Fab heavy chain, Fab light chain, ... | | 著者 | Bokoch, M.P, Zou, Y, Rasmussen, S.G.F, Liu, C.W, Nygaard, R, Rosenbaum, D.M, Fung, J.J, Choi, H.-J, Thian, F.S, Kobilka, T.S, Puglisi, J.D, Weis, W.I, Pardo, L, Prosser, S, Mueller, L, Kobilka, B.K. | | 登録日 | 2009-11-02 | | 公開日 | 2010-02-16 | | 最終更新日 | 2021-10-13 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor.
Nature, 463, 2010
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4GPO
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4WW3
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4UHR
 | | Thermostabilised HUMAN A2a Receptor with CGS21680 bound | | 分子名称: | 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE, THERMOSTABILISED HUMAN A2A RECEPTOR | | 著者 | Lebon, G, Edwards, P.C, Leslie, A.G.W, Tate, C.G. | | 登録日 | 2015-03-25 | | 公開日 | 2015-04-08 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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4UG2
 | | Thermostabilised HUMAN A2a Receptor with CGS21680 bound | | 分子名称: | (2S)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE, THERMOSTABILISED HUMAN A2A RECEPTOR | | 著者 | Lebon, G, Edwards, P.C, Leslie, A.G.W, Tate, C.G. | | 登録日 | 2015-03-21 | | 公開日 | 2015-04-08 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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6Z4Q
 | | Crystal structure of the neurotensin receptor 1 in complex with the small-molecule inverse agonist SR142948A | | 分子名称: | 2-[[5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methyl-carbamoyl]-2-propan-2-yl-phenyl]pyrazol-3-yl]carbonylamino]adamantane-2-carboxylic acid, Neurotensin receptor type 1,Neurotensin receptor type 1,DARPin | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-05-25 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.923 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6ZIN
 | | Crystal structure of the neurotensin receptor 1 in complex with the small molecule inverse agonist SR48692 | | 分子名称: | 2-[[1-(7-chloranylquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl]carbonylamino]adamantane-2-carboxylic acid, Neurotensin receptor type 1,DARPin,HRV 3C protease recognition sequence | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-06-26 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.639 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6Z8N
 | | Crystal structure of the neurotensin receptor 1 in complex with the small-molecule full agonist SRI-9829 | | 分子名称: | (2~{S})-4-methyl-2-[(1-quinolin-8-ylsulfonylindol-3-yl)carbonylamino]pentanoic acid, Neurotensin receptor type 1,Neurotensin receptor type 1,Neurotensin receptor type 1,Neurotensin receptor type 1,Neurotensin receptor 1 (NTSR1),Neurotensin receptor 1 (NTSR1) | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-06-02 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.803 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6YVR
 | | Crystal structure of the neurotensin receptor 1 in complex with the peptide full agonist NTS8-13 | | 分子名称: | Neurotensin receptor type 1,Neurotensin receptor type 1,DARPin crystallisation chaperone, neurotensin NTS8-13 (full agonist), nonyl beta-D-glucopyranoside | | 著者 | Deluigi, M, Merklinger, L, Hilge, M, Ernst, P, Klipp, A, Klenk, C, Plueckthun, A. | | 登録日 | 2020-04-28 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.458 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6Z4S
 | | Crystal structure of the neurotensin receptor 1 (NTSR1-H4bmx) in complex with the small molecule inverse agonist SR48692 | | 分子名称: | 2-[[1-(7-chloranylquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl]carbonylamino]adamantane-2-carboxylic acid, Neurotensin receptor type 1,DARPin,HRV 3C protease recognition sequence | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-05-25 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.707 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6Z66
 | | Crystal structure of apo-state neurotensin receptor 1 | | 分子名称: | Neurotensin receptor type 1,Neurotensin receptor type 1,DARPin | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-05-27 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3.192 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6ZA8
 | | Crystal structure of the neurotensin receptor 1 in complex with the small-molecule partial agonist RTI-3a | | 分子名称: | (2~{S})-2-[[1-(7-chloranylquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl]carbonylamino]-4-methyl-pentanoic acid, Neurotensin receptor type 1,Neurotensin receptor type 1,Neurotensin receptor 1 (NTSR1),Neurotensin receptor 1 (NTSR1),Neurotensin receptor type 1,Neurotensin receptor 1 (NTSR1),Neurotensin receptor 1 (NTSR1) | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-06-05 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.72 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6Z4V
 | | Crystal structure of the neurotensin receptor 1 (NTSR1-H4bmx) in complex with NTS8-13 | | 分子名称: | ARG-PRO-TYR-ILE-LEU, Neurotensin receptor type 1,Neurotensin receptor type 1,DARPin | | 著者 | Deluigi, M, Klipp, A, Hilge, M, Merklinger, L, Klenk, C, Plueckthun, A. | | 登録日 | 2020-05-25 | | 公開日 | 2021-02-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.595 Å) | | 主引用文献 | Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Sci Adv, 7, 2021
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6VI4
 | | Nanobody-Enabled Monitoring of Kappa Opioid Receptor States | | 分子名称: | (3R)-7-hydroxy-N-{(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl}-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, CHOLESTEROL, Kappa opioid receptor, ... | | 著者 | Che, T, Roth, B.L. | | 登録日 | 2020-01-11 | | 公開日 | 2020-03-18 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Nanobody-enabled monitoring of kappa opioid receptor states.
Nat Commun, 11, 2020
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5A8E
 | | thermostabilised beta1-adrenoceptor with rationally designed inverse agonist 7-methylcyanopindolol bound | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (CARBAMOYLMETHYL-CARBOXYMETHYL-AMINO)-ACETIC ACID, 4-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-7-methyl-1H-indole-2-carbonitrile, ... | | 著者 | Sato, T, Baker, J.G, Warne, T, Brown, G.A, Congreve, M, Leslie, A.G.W, Tate, C.G. | | 登録日 | 2015-07-15 | | 公開日 | 2015-09-30 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound Beta1-Adrenergic Receptor.
Mol.Pharmacol., 88, 2015
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5C1M
 | | Crystal structure of active mu-opioid receptor bound to the agonist BU72 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2R,3S,3aR,5aR,6R,11bR,11cS)-3a-methoxy-3,14-dimethyl-2-phenyl-2,3,3a,6,7,11c-hexahydro-1H-6,11b-(epiminoethano)-3,5a-methanonaphtho[2,1-g]indol-10-ol, CHOLESTEROL, ... | | 著者 | Huang, W.J, Manglik, A, Venkatakrishnan, A.J, Laeremans, T, Feinberg, E.N, Sanborn, A.L, Kato, H.E, Livingston, K.E, Thorsen, T.S, Kling, R, Granier, S, Gmeiner, P, Husbands, S.M, Traynor, J.R, Weis, W.I, Steyaert, J, Dror, R.O, Kobilka, B.K. | | 登録日 | 2015-06-15 | | 公開日 | 2015-08-05 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.07 Å) | | 主引用文献 | Structural insights into mu-opioid receptor activation.
Nature, 524, 2015
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4AMI
 | | Turkey beta1 adrenergic receptor with stabilising mutations and bound biased agonist bucindolol | | 分子名称: | 2-[(2S)-3-[[1-(1H-indol-3-yl)-2-methyl-propan-2-yl]amino]-2-oxidanyl-propoxy]benzenecarbonitrile, BETA-1 ADRENERGIC RECEPTOR, HEGA-10 | | 著者 | Warne, T, Edwards, P.C, Leslie, A.G, Tate, C.G. | | 登録日 | 2012-03-11 | | 公開日 | 2012-05-23 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Crystal Structures of a Stabilized Beta1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol
Structure, 20, 2012
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