6TKO
 
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6ZG9
 | | Structure of M1-StaR-T4L in complex with GSK1034702 at 2.5A | | 分子名称: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 7-fluoranyl-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1~{H}-benzimidazol-2-one, Muscarinic acetylcholine receptor M1,Endolysin,Muscarinic acetylcholine receptor M1, ... | | 著者 | Rucktooa, P, Cooke, R.M. | | 登録日 | 2020-06-18 | | 公開日 | 2021-10-06 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell, 184, 2021
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6ZFZ
 | | Structure of M1-StaR-T4L in complex with 77-LH-28-1 at 2.17A | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-[3-(4-butylpiperidin-1-yl)propyl]-3,4-dihydroquinolin-2-one, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | 著者 | Rucktooa, P, Cooke, R.M. | | 登録日 | 2020-06-18 | | 公開日 | 2021-10-06 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.17 Å) | | 主引用文献 | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell, 184, 2021
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6ZG4
 | | Structure of M1-StaR-T4L in complex with HTL0009936 at 2.35A | | 分子名称: | Muscarinic acetylcholine receptor M1,Endolysin,Muscarinic acetylcholine receptor M1, OLEIC ACID, PHOSPHATE ION, ... | | 著者 | Rucktooa, P, Cooke, R.M. | | 登録日 | 2020-06-18 | | 公開日 | 2021-10-06 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell, 184, 2021
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5D5A
 | | In meso in situ serial X-ray crystallography structure of the Beta2-adrenergic receptor at 100 K | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, 1,4-BUTANEDIOL, ACETAMIDE, ... | | 著者 | Huang, C.-Y, Olieric, V, Warshamanage, R, Liu, X, Kobilka, B, Kay Diederichs, K, Wang, M, Caffrey, M. | | 登録日 | 2015-08-10 | | 公開日 | 2016-01-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.4826 Å) | | 主引用文献 | In meso in situ serial X-ray crystallography of soluble and membrane proteins at cryogenic temperatures.
Acta Crystallogr D Struct Biol, 72, 2016
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6TPN
 | | Crystal structure of the Orexin-2 receptor in complex with HTL6641 at 2.61 A resolution | | 分子名称: | 2-(5,6-dimethoxypyridin-3-yl)-1,1-bis(oxidanylidene)-4-[[2,4,6-tris(fluoranyl)phenyl]methyl]pyrido[2,3-e][1,2,4]thiadiazin-3-one, NITRATE ION, OLEIC ACID, ... | | 著者 | Rappas, M, Ali, A, Bennett, K.A, Brown, J.D, Bucknell, S.J, Congreve, M, Cooke, R.M, Cseke, G, de Graaf, C, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Mason, J.S, Mould, R, Patel, J.C, Tehan, B.G, Weir, M, Christopher, J.A. | | 登録日 | 2019-12-13 | | 公開日 | 2020-01-01 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.608 Å) | | 主引用文献 | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
J.Med.Chem., 63, 2020
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6TPJ
 | | Crystal structure of the Orexin-2 receptor in complex with suvorexant at 2.76 A resolution | | 分子名称: | AMMONIUM ION, OLEIC ACID, Orexin receptor type 2,GlgA glycogen synthase,Hypocretin receptor-2, ... | | 著者 | Rappas, M, Ali, A, Bennett, K.A, Brown, J.D, Bucknell, S.J, Congreve, M, Cooke, R.M, Cseke, G, de Graaf, C, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Mason, J.S, Mould, R, Patel, J.C, Tehan, B.G, Weir, M, Christopher, J.A. | | 登録日 | 2019-12-13 | | 公開日 | 2020-01-01 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.74 Å) | | 主引用文献 | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
J.Med.Chem., 63, 2020
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5DSG
 | | Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium | | 分子名称: | (1R,2R,4S,5S,7S)-7-{[hydroxy(dithiophen-2-yl)acetyl]oxy}-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0~2,4~]nonane, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE, ... | | 著者 | Thal, D.M, Kobilka, B.K, Sexton, P.M, Christopoulos, A. | | 登録日 | 2015-09-17 | | 公開日 | 2016-03-16 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Nature, 531, 2016
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5EN0
 | | Crystal Structure of T94I rhodopsin mutant | | 分子名称: | ACETATE ION, Guanine nucleotide-binding protein G(t) subunit alpha-3, PALMITIC ACID, ... | | 著者 | Singhal, A, Guo, Y, Matkovic, M, Schertler, G, Deupi, X, Yan, E, Standfuss, J. | | 登録日 | 2015-11-08 | | 公開日 | 2016-08-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | Structural role of the T94I rhodopsin mutation in congenital stationary night blindness.
Embo Rep., 17, 2016
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3VW7
 | | Crystal structure of human protease-activated receptor 1 (PAR1) bound with antagonist vorapaxar at 2.2 angstrom | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CHLORIDE ION, Proteinase-activated receptor 1, ... | | 著者 | Zhang, C, Srinivasan, Y, Arlow, D.H, Fung, J.J, Palmer, D, Zheng, Y, Green, H.F, Pandey, A, Dror, R.O, Shaw, D.E, Weis, W.I, Coughlin, S.R, Kobilka, B.K. | | 登録日 | 2012-08-07 | | 公開日 | 2012-12-12 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | High-resolution crystal structure of human protease-activated receptor 1
Nature, 492, 2012
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7ARO
 | | Crystal structure of the non-ribose partial agonist LUF5833 bound to the adenosine A2A receptor | | 分子名称: | 2-azanyl-6-(1~{H}-imidazol-2-ylmethylsulfanyl)-4-phenyl-pyridine-3,5-dicarbonitrile, Adenosine receptor A2a,Soluble cytochrome b562,Adenosine receptor A2a, CHOLESTEROL, ... | | 著者 | Verdon, G, Amelia, T, van Veldhoven, J, Falsini, M, Liu, R, Heitman, L, van Westen, G, Segala, E, Cheng, R, Cooke, R, van der Es, D, Ijzerman, A. | | 登録日 | 2020-10-25 | | 公開日 | 2021-04-07 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (3.119 Å) | | 主引用文献 | Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A 2A Receptor.
J.Med.Chem., 64, 2021
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7AUE
 | | Melanocortin receptor 4 (MC4R) Gs protein complex | | 分子名称: | AMINOSERINE, CALCIUM ION, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Degtjarik, O, Israeli, H, Prabahar, V, Shalev-Benami, M. | | 登録日 | 2020-11-02 | | 公開日 | 2021-04-28 | | 最終更新日 | 2023-03-15 | | 実験手法 | ELECTRON MICROSCOPY (2.97 Å) | | 主引用文献 | Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling.
Science, 372, 2021
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3V2Y
 | | Crystal Structure of a Lipid G protein-Coupled Receptor at 2.80A | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Sphingosine 1-phosphate receptor 1, Lysozyme chimera (E.C.3.2.1.17), ... | | 著者 | Hanson, M.A, Roth, C.B, Jo, E, Griffith, M.T, Scott, F.L, Reinhart, G, Desale, H, Clemons, B, Cahalan, S.M, Schuerer, S.C, Sanna, M.G, Han, G.W, Kuhn, P, Rosen, H, Stevens, R.C, GPCR Network (GPCR) | | 登録日 | 2011-12-12 | | 公開日 | 2012-02-15 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Crystal structure of a lipid G protein-coupled receptor.
Science, 335, 2012
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3V2W
 | | Crystal Structure of a Lipid G protein-Coupled Receptor at 3.35A | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Sphingosine 1-phosphate receptor 1, Lysozyme chimera, ... | | 著者 | Hanson, M.A, Roth, C.B, Jo, E, Griffith, M.T, Scott, F.L, Reinhart, G, Desale, H, Clemons, B, Cahalan, S.M, Schuerer, S.C, Sanna, M.G, Han, G.W, Kuhn, P, Rosen, H, Stevens, R.C, GPCR Network (GPCR) | | 登録日 | 2011-12-12 | | 公開日 | 2012-02-15 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (3.35 Å) | | 主引用文献 | Crystal structure of a lipid G protein-coupled receptor.
Science, 335, 2012
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3UON
 | | Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist | | 分子名称: | (3R)-1-azabicyclo[2.2.2]oct-3-yl hydroxy(diphenyl)acetate, CHLORIDE ION, Human M2 muscarinic acetylcholine, ... | | 著者 | Haga, K, Kruse, A.C, Asada, H, Yurugi-Kobayashi, T, Shiroishi, M, Zhang, C, Weis, W.I, Okada, T, Kobilka, B.K, Haga, T, Kobayashi, T. | | 登録日 | 2011-11-16 | | 公開日 | 2012-02-01 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist.
Nature, 482, 2012
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7BU7
 | | Structure of human beta1 adrenergic receptor bound to BI-167107 and nanobody 6B9 | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, ... | | 著者 | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | 登録日 | 2020-04-04 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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7BW0
 | | Active human TGR5 complex with a synthetic agonist 23H | | 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 | Chen, G, Wang, X.K, Chen, Q, Hu, H.L, Ren, R.B. | | 登録日 | 2020-04-12 | | 公開日 | 2020-09-02 | | 最終更新日 | 2024-03-27 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Cryo-EM structure of activated bile acids receptor TGR5 in complex with stimulatory G protein.
Signal Transduct Target Ther, 5, 2020
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7BZ2
 | | Cryo-EM structure of the formoterol-bound beta2 adrenergic receptor-Gs protein complex. | | 分子名称: | Beta2 adrenergic 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 | Zhang, Y.N, Yang, F, Ling, S.L, Lv, P, Zhou, Y.X, Fang, W, Sun, W, Shi, P, Tian, C.L. | | 登録日 | 2020-04-26 | | 公開日 | 2020-08-05 | | 実験手法 | ELECTRON MICROSCOPY (3.82 Å) | | 主引用文献 | Single-particle cryo-EM structural studies of the beta2AR-Gs complex bound with a full agonist formoterol.
Cell Discov, 6, 2020
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5D5B
 | | In meso X-ray crystallography structure of the Beta2-adrenergic receptor at 100 K | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, 1,4-BUTANEDIOL, ACETAMIDE, ... | | 著者 | Huang, C.-Y, Olieric, V, Liu, X, Kobilka, B, Wang, M, Caffrey, M. | | 登録日 | 2015-08-10 | | 公開日 | 2016-01-13 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.8 Å) | | 主引用文献 | In meso in situ serial X-ray crystallography of soluble and membrane proteins at cryogenic temperatures.
Acta Crystallogr D Struct Biol, 72, 2016
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5D6L
 | | beta2AR-T4L - CIM | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, 1,4-BUTANEDIOL, ACETAMIDE, ... | | 著者 | Ma, P, Caffrey, M. | | 登録日 | 2015-08-12 | | 公開日 | 2016-08-17 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | The cubicon method for concentrating membrane proteins in the cubic mesophase.
Nat Protoc, 12, 2017
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7BVQ
 | | Structure of human beta1 adrenergic receptor bound to carazolol | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, CHOLESTEROL, ... | | 著者 | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | 登録日 | 2020-04-11 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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5DHG
 | | The crystal structure of nociceptin/orphanin FQ peptide receptor (NOP) in complex with C-35 (PSI Community Target) | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-benzyl-N-{3-[4-(2,6-dichlorophenyl)piperidin-1-yl]propyl}-D-prolinamide, OLEIC ACID, ... | | 著者 | Miller, R.L, Thompson, A.A, Trapella, C, Guerrini, R, Malfacini, D, Patel, N, Han, G.W, Cherezov, V, Calo, G, Katritch, V, Stevens, R.C, GPCR Network (GPCR) | | 登録日 | 2015-08-30 | | 公開日 | 2015-10-21 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor.
Structure, 23, 2015
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5DGY
 | | Crystal structure of rhodopsin bound to visual arrestin | | 分子名称: | Endolysin,Rhodopsin,S-arrestin | | 著者 | Zhou, X.E, Gao, X, Kang, Y, He, Y, de Waal, P.W, Suino-Powell, K.M, Wang, M, Melcher, K, Xu, H.E. | | 登録日 | 2015-08-28 | | 公開日 | 2016-03-23 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (7.7 Å) | | 主引用文献 | X-ray laser diffraction for structure determination of the rhodopsin-arrestin complex.
Sci Data, 3, 2016
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7BU6
 | | Structure of human beta1 adrenergic receptor bound to norepinephrine and nanobody 6B9 | | 分子名称: | (2S)-2,3-dihydroxypropyl octanoate, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CHOLESTEROL, ... | | 著者 | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | 登録日 | 2020-04-04 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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7BR3
 | | Crystal structure of the protein 1 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2R)-2,3-dihydroxypropyl dodecanoate, 4-[[(1R)-2-[5-(2-fluoranyl-3-methoxy-phenyl)-3-[[2-fluoranyl-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-bis(oxidanylidene)pyrimidin-1-yl]-1-phenyl-ethyl]amino]butanoic acid, ... | | 著者 | Cheng, L, Shao, Z. | | 登録日 | 2020-03-26 | | 公開日 | 2020-10-07 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.79 Å) | | 主引用文献 | Structure of the human gonadotropin-releasing hormone receptor GnRH1R reveals an unusual ligand binding mode.
Nat Commun, 11, 2020
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