6AQF
 
 | | Crystal structure of A2AAR-BRIL in complex with the antagonist ZM241385 produced from Pichia pastoris | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol, ... | | 著者 | Eddy, M.T, Lee, M.Y, Gao, Z, White, K, Didenko, T, Horst, R, Audet, M, Stanczak, P, McClary, K.M, Han, G.W, Jacobson, K.A, Stevens, R.C, Wuthrich, K. | | 登録日 | 2017-08-19 | | 公開日 | 2018-01-10 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.51 Å) | | 主引用文献 | Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor.
Cell, 172, 2018
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6RZ5
 | | XFEL crystal structure of the human cysteinyl leukotriene receptor 1 in complex with zafirlukast | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Cysteinyl leukotriene receptor 1,Soluble cytochrome b562,Cysteinyl leukotriene receptor 1, OLEIC ACID, ... | | 著者 | Luginina, A, Gusach, A, Marin, E, Mishin, A, Brouillette, R, Popov, P, Shiryaeva, A, Besserer-Offroy, E, Longpre, J.M, Lyapina, E, Ishchenko, A, Patel, N, Polovinkin, V, Safronova, N, Bogorodskiy, A, Edelweiss, E, Liu, W, Batyuk, A, Gordeliy, V, Han, G.W, Sarret, P, Katritch, V, Borshchevskiy, V, Cherezov, V. | | 登録日 | 2019-06-12 | | 公開日 | 2019-10-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.53 Å) | | 主引用文献 | Structure-based mechanism of cysteinyl leukotriene receptor inhibition by antiasthmatic drugs.
Sci Adv, 5, 2019
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8FEG
 | | CryoEM structure of Kappa Opioid Receptor bound to a semi-peptide and Gi1 | | 分子名称: | ACE-TYR-ALA-DTY-THR-THR-CYS-THR-DPN-XT9, 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 | Fay, J.F, Che, T. | | 登録日 | 2022-12-06 | | 公開日 | 2023-12-06 | | 最終更新日 | 2024-01-17 | | 実験手法 | ELECTRON MICROSCOPY (2.54 Å) | | 主引用文献 | Design and structural validation of peptide-drug conjugate ligands of the kappa-opioid receptor.
Nat Commun, 14, 2023
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7S8M
 | | CryoEM structure of Gi-coupled MRGPRX2 with peptide agonist Cortistatin-14 | | 分子名称: | Cortistatin 14, 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 | Cao, C, Fay, J.F, Gumpper, R.H, Roth, B.L. | | 登録日 | 2021-09-18 | | 公開日 | 2021-11-17 | | 最終更新日 | 2021-12-15 | | 実験手法 | ELECTRON MICROSCOPY (2.54 Å) | | 主引用文献 | Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
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6OL9
 | | Structure of the M5 muscarinic acetylcholine receptor (M5-T4L) 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, 3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL, ... | | 著者 | Vuckovic, Z, Christopoulos, A, Thal, D.M. | | 登録日 | 2019-04-16 | | 公開日 | 2019-12-11 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.541 Å) | | 主引用文献 | Crystal structure of the M5muscarinic acetylcholine receptor.
Proc.Natl.Acad.Sci.USA, 116, 2019
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6TQ6
 | | Crystal structure of the Orexin-1 receptor in complex with Compound 14 | | 分子名称: | (1R)-2-{[(S)-{[(2S)-2,3-dihydroxypropyl]oxy}(hydroxy)phosphoryl]oxy}-1-[(hexadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, 2-(5-methylsulfonylpyridin-3-yl)-1,1-bis(oxidanylidene)-4-[[2,4,6-tris(fluoranyl)phenyl]methyl]pyrido[2,3-e][1,2,4]thiadiazin-3-one, Orexin receptor type 1, ... | | 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 | 2019-12-16 | | 公開日 | 2020-01-01 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.546 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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8J6P
 | | Cryo-EM structure of the MK-6892-bound human HCAR2-Gi1 complex | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 7-methyl-N-[(2R)-1-phenoxypropan-2-yl]-3-(4-propan-2-ylphenyl)pyrazolo[1,5-a]pyrimidine-6-carboxamide, CHOLESTEROL, ... | | 著者 | Mao, C, Gao, M, Zang, S, Zhu, Y, Ma, X, Zhang, Y. | | 登録日 | 2023-04-26 | | 公開日 | 2023-12-06 | | 実験手法 | ELECTRON MICROSCOPY (2.55 Å) | | 主引用文献 | Orthosteric and allosteric modulation of human HCAR2 signaling complex.
Nat Commun, 14, 2023
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6WJC
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8X7A
 | | Treprostinil bound Prostacyclin Receptor G protein complex | | 分子名称: | 2-[[(1~{R},2~{R},3~{a}~{S},9~{a}~{S})-2-oxidanyl-1-[(3~{S})-3-oxidanyloctyl]-2,3,3~{a},4,9,9~{a}-hexahydro-1~{H}-cyclopenta[g]naphthalen-5-yl]oxy]ethanoic 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, ... | | 著者 | Wang, J.J, Jin, S, Zhang, H, Xu, Y, Hu, W, Jiang, Y, Chen, C, Wang, D.W, Xu, H.E, Wu, C. | | 登録日 | 2023-11-23 | | 公開日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (2.56 Å) | | 主引用文献 | Molecular recognition and activation of the prostacyclin receptor by anti-pulmonary arterial hypertension drugs.
Sci Adv, 10, 2024
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8EA0
 | | CryoEM structure of miniGq-coupled hM3R in complex with iperoxo (local refinement) | | 分子名称: | 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, CHOLESTEROL HEMISUCCINATE, Muscarinic acetylcholine receptor M3 | | 著者 | Zhang, S, Fay, J.F, Roth, B.L. | | 登録日 | 2022-08-27 | | 公開日 | 2022-11-30 | | 最終更新日 | 2022-12-21 | | 実験手法 | ELECTRON MICROSCOPY (2.56 Å) | | 主引用文献 | Molecular basis for selective activation of DREADD-based chemogenetics.
Nature, 612, 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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7S8O
 | | CryoEM structure of Gi-coupled MRGPRX2 with small molecule agonist (R)-Zinc-3573 | | 分子名称: | (3R)-N,N-dimethyl-1-[(8S)-5-phenylpyrazolo[1,5-a]pyrimidin-7-yl]pyrrolidin-3-amine, 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 | Cao, C, Fay, J.F, Gumpper, R.H, Roth, B.L. | | 登録日 | 2021-09-18 | | 公開日 | 2021-11-17 | | 最終更新日 | 2021-12-15 | | 実験手法 | ELECTRON MICROSCOPY (2.58 Å) | | 主引用文献 | Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
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8IOD
 | | Cryo-EM structure of the PG-901-bound human melanocortin receptor 5 (MC5R)-Gs complex | | 分子名称: | CALCIUM ION, 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,HiBiT, ... | | 著者 | Feng, W.B, Zhou, Q.T, Chen, X.Y, Dai, A.T, Cai, X.Q, Liu, X, Zhao, F.H, Chen, Y, Ye, C.Y, Xu, Y.N, Cong, Z.T, Li, H, Lin, S, Yang, D.H, Wang, M.W. | | 登録日 | 2023-03-10 | | 公開日 | 2023-09-20 | | 最終更新日 | 2023-11-15 | | 実験手法 | ELECTRON MICROSCOPY (2.59 Å) | | 主引用文献 | Structural insights into ligand recognition and subtype selectivity of the human melanocortin-3 and melanocortin-5 receptors.
Cell Discov, 9, 2023
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8FMZ
 | | Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator | | 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, MiniGq, ... | | 著者 | Krumm, B.E, Diberto, J.F, Olsen, R.H.J, Kang, H, Slocum, S.T, Zhang, S, Strachan, R.T, Fay, J.F, Roth, B.L. | | 登録日 | 2022-12-26 | | 公開日 | 2023-03-29 | | 最終更新日 | 2023-04-19 | | 実験手法 | ELECTRON MICROSCOPY (2.59 Å) | | 主引用文献 | Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator.
Biochemistry, 62, 2023
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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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7F1T
 | | Crystal structure of the human chemokine receptor CCR5 in complex with MIP-1a | | 分子名称: | C-C motif chemokine 3,C-C chemokine receptor type 5,Rubredoxin,C-C chemokine receptor type 5, ZINC ION | | 著者 | Zhang, H, Chen, K, Tan, Q, Han, S, Zhu, Y, Zhao, Q, Wu, B. | | 登録日 | 2021-06-09 | | 公開日 | 2021-07-14 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structural basis for chemokine recognition and receptor activation of chemokine receptor CCR5.
Nat Commun, 12, 2021
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8W88
 | | Cryo-EM structure of the SEP363856-bound TAAR1-Gs complex | | 分子名称: | 1-[(7~{S})-5,7-dihydro-4~{H}-thieno[2,3-c]pyran-7-yl]-~{N}-methyl-methanamine, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Liu, H, Zheng, Y, Wang, Y, Wang, Y, He, X, Xu, P, Huang, S, Yuan, Q, Zhang, X, Wang, S, Xu, H.E, Xu, F. | | 登録日 | 2023-09-01 | | 公開日 | 2023-11-22 | | 最終更新日 | 2024-01-03 | | 実験手法 | ELECTRON MICROSCOPY (2.6 Å) | | 主引用文献 | Recognition of methamphetamine and other amines by trace amine receptor TAAR1.
Nature, 624, 2023
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8XZH
 | | Cryo-EM structure of the MM07-bound human APLNR-Gi complex | | 分子名称: | Apelin 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 | Wang, W, Ji, S, Zhang, Y. | | 登録日 | 2024-01-21 | | 公開日 | 2024-03-20 | | 最終更新日 | 2024-03-27 | | 実験手法 | ELECTRON MICROSCOPY (2.6 Å) | | 主引用文献 | Structure-based design of non-hypertrophic apelin receptor modulator.
Cell, 187, 2024
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7WC7
 | | Crystal structure of serotonin 2A receptor in complex with lisuride | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2A,5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, CHOLESTEROL, ... | | 著者 | Cao, D, Yu, J, Wang, H, Luo, Z, Liu, X, He, L, Qi, J, Fan, L, Tang, L, Chen, Z, Li, J, Cheng, J, Wang, S. | | 登録日 | 2021-12-18 | | 公開日 | 2022-01-26 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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7WC6
 | | Crystal structure of serotonin 2A receptor in complex with LSD | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, ... | | 著者 | Cao, D, Yu, J, Wang, H, Luo, Z, Liu, X, He, L, Qi, J, Fan, L, Tang, L, Chen, Z, Li, J, Cheng, J, Wang, S. | | 登録日 | 2021-12-18 | | 公開日 | 2022-01-26 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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8THK
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7WQ4
 | | Galanin-bound galanin receptor 2 in complex with Gq | | 分子名称: | CHOLESTEROL, Engineered Guanine nucleotide-binding protein G(q) subunit alpha, Galanin, ... | | 著者 | Duan, J, Shen, D.D, Xu, H.E, Zhang, Y, Jiang, Y. | | 登録日 | 2022-01-24 | | 公開日 | 2022-04-20 | | 最終更新日 | 2022-10-19 | | 実験手法 | ELECTRON MICROSCOPY (2.6 Å) | | 主引用文献 | Molecular basis for allosteric agonism and G protein subtype selectivity of galanin receptors
Nat Commun, 13, 2022
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4XES
 | | Structure of active-like neurotensin receptor | | 分子名称: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CITRIC ACID, DI(HYDROXYETHYL)ETHER, ... | | 著者 | Krumm, B.E, White, J.F, Shah, P, Grisshammer, R. | | 登録日 | 2014-12-24 | | 公開日 | 2015-07-29 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structural prerequisites for G-protein activation by the neurotensin receptor.
Nat Commun, 6, 2015
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7PYR
 | | Crystal structure of the adenosine A2A receptor (A2A-PSB1-bRIL) in complex with preladenant conjugate PSB-2115 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[2-[2-[2-[2-[2-[4-[4-[2-[7-azanyl-4-(furan-2-yl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.0^{2,6}]dodeca-1(9),2,4,7,11-pentaen-10-yl]ethyl]piperazin-1-yl]phenoxy]ethanoylamino]ethoxy]ethoxy]ethoxy]ethoxy]-~{N}-[5-[2,2-bis(fluoranyl)-4,6,10,12-tetramethyl-1,3-diaza-2$l^{4}-boratricyclo[7.3.0.0^{3,7}]dodeca-4,6,9,11-tetraen-8-yl]pentyl]ethanamide, Adenosine receptor A2a,Soluble cytochrome b562,Adenosine receptor A2a, ... | | 著者 | Claff, T, Klapschinski, T.A, Tiruttani Subhramanyam, U.K, Vaassen, V.J, Schlegel, J.G, Vielmuth, C, Voss, J.H, Labahn, J, Muller, C.E. | | 登録日 | 2021-10-11 | | 公開日 | 2022-03-02 | | 最終更新日 | 2022-05-25 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A 2A Receptor with Preladenant Conjugates.
Angew.Chem.Int.Ed.Engl., 61, 2022
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7TD4
 | | Sphingosine-1-phosphate receptor 1-Gi complex bound to Siponimod | | 分子名称: | 1-[[4-[(~{E})-~{N}-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-~{C}-methyl-carbonimidoyl]-2-ethyl-phenyl]methyl]azetidine-3-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Liu, S, Paknejad, N, Zhu, L, Kihara, Y, Ray, D, Chun, J, Liu, W, Hite, R.K, Huang, X.Y. | | 登録日 | 2021-12-30 | | 公開日 | 2022-02-09 | | 最終更新日 | 2022-02-23 | | 実験手法 | ELECTRON MICROSCOPY (2.6 Å) | | 主引用文献 | Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate.
Nat Commun, 13, 2022
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