6DRY
 
 | | Structural Determinants of Activation and Biased Agonism at the 5-HT2B Receptor | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (8beta)-N-[(2S)-1-hydroxybutan-2-yl]-6-methyl-9,10-didehydroergoline-8-carboxamide, 5HT2B receptor, ... | | 著者 | McCorvy, J.D, Wacker, D, Wang, S, Agegnehu, B, Liu, J, Lansu, K, Tribo, A.R, Olsen, R.H.J, Che, T, Jin, J, Roth, B.L. | | 登録日 | 2018-06-13 | | 公開日 | 2018-08-29 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.918 Å) | | 主引用文献 | Structural determinants of 5-HT2Breceptor activation and biased agonism.
Nat. Struct. Mol. Biol., 25, 2018
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8TB7
 | | Cryo-EM Structure of GPR61- | | 分子名称: | 6-{[(3,5-difluoropyridin-4-yl)methyl]amino}-N-(4-ethoxy-6-methylpyrimidin-2-yl)-2-methoxy-N-(2-methoxyethyl)pyridine-3-sulfonamide, Fab hinge-binding nanobody, Fab24 BAK5 heavy chain, ... | | 著者 | Lees, J.A, Dias, J.M, Han, S. | | 登録日 | 2023-06-28 | | 公開日 | 2023-10-04 | | 実験手法 | ELECTRON MICROSCOPY (2.94 Å) | | 主引用文献 | An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism.
Nat Commun, 14, 2023
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8HNM
 | | CXCR3-DNGi complex activated by VUF11222 | | 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 | Jiao, H.Z, Hu, H.L. | | 登録日 | 2022-12-08 | | 公開日 | 2023-11-29 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (2.94 Å) | | 主引用文献 | Structural insights into the activation and inhibition of CXC chemokine receptor 3.
Nat.Struct.Mol.Biol., 31, 2024
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8FYL
 | | Vilazodone-bound serotonin 1A (5-HT1A) receptor-Gi1 protein complex | | 分子名称: | 5-{4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl}-1-benzofuran-2-carboxamide, CHOLESTEROL HEMISUCCINATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Warren, A.L, Zilberg, G, Capper, M.J, Wacker, D. | | 登録日 | 2023-01-26 | | 公開日 | 2024-05-15 | | 最終更新日 | 2024-06-19 | | 実験手法 | ELECTRON MICROSCOPY (2.94 Å) | | 主引用文献 | Structural pharmacology and therapeutic potential of 5-methoxytryptamines.
Nature, 630, 2024
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7F83
 | | Crystal Structure of a receptor in Complex with inverse agonist | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone, Growth hormone secretagogue receptor type 1,Soluble cytochrome b562 | | 著者 | Xu, Z, Shao, Z. | | 登録日 | 2021-07-01 | | 公開日 | 2022-01-19 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.94 Å) | | 主引用文献 | Molecular mechanism of agonism and inverse agonism in ghrelin receptor.
Nat Commun, 13, 2022
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8DRK
 | | LRRC8A:C conformation 1 (round) top focus | | 分子名称: | 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine, Volume-regulated anion channel subunit LRRC8A,Soluble cytochrome b562, Volume-regulated anion channel subunit LRRC8C | | 著者 | Kern, D.M, Brohawn, S.G. | | 登録日 | 2022-07-21 | | 公開日 | 2023-03-08 | | 最終更新日 | 2023-07-05 | | 実験手法 | ELECTRON MICROSCOPY (2.95 Å) | | 主引用文献 | Structural basis for assembly and lipid-mediated gating of LRRC8A:C volume-regulated anion channels.
Nat.Struct.Mol.Biol., 30, 2023
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8HQM
 | | Activation mechanism of GPR132 by NPGLY | | 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(i) subunit alpha-1, ... | | 著者 | Wang, J.L, Ding, J.H, Sun, J.P, Yu, X. | | 登録日 | 2022-12-13 | | 公開日 | 2023-10-11 | | 最終更新日 | 2023-11-01 | | 実験手法 | ELECTRON MICROSCOPY (2.95 Å) | | 主引用文献 | Functional screening and rational design of compounds targeting GPR132 to treat diabetes.
Nat Metab, 5, 2023
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5ZKB
 | | Crystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with AF-DX 384 | | 分子名称: | Muscarinic acetylcholine receptor M2,Apo-cytochrome b562,Muscarinic acetylcholine receptor M2, N-[2-[(2S)-2-[(dipropylamino)methyl]piperidin-1-yl]ethyl]-6-oxidanylidene-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide | | 著者 | Suno, R, Maeda, S, Yasuda, S, Yamashita, K, Hirata, K, Horita, S, Tawaramoto, M.S, Tsujimoto, H, Murata, T, Kinoshita, M, Yamamoto, M, Kobilka, B.K, Iwata, S, Kobayashi, T. | | 登録日 | 2018-03-23 | | 公開日 | 2018-11-21 | | 最終更新日 | 2022-03-23 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | Structural insights into the subtype-selective antagonist binding to the M2muscarinic receptor
Nat. Chem. Biol., 14, 2018
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8HQE
 | | Cryo-EM structure of the apo-GPR132-Gi | | 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(i) subunit alpha-1, ... | | 著者 | Wang, J.L, Ding, J.H, Sun, J.P, Yu, X. | | 登録日 | 2022-12-13 | | 公開日 | 2023-10-11 | | 最終更新日 | 2023-11-01 | | 実験手法 | ELECTRON MICROSCOPY (2.97 Å) | | 主引用文献 | Functional screening and rational design of compounds targeting GPR132 to treat diabetes.
Nat Metab, 5, 2023
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8IHF
 | | Cryo-EM structure of HCA2-Gi complex with MK6892 | | 分子名称: | 2-[[2,2-dimethyl-3-[3-(5-oxidanylpyridin-2-yl)-1,2,4-oxadiazol-5-yl]propanoyl]amino]cyclohexene-1-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Suzuki, S, Nishikawa, K, Suzuki, H, Fujiyoshi, Y. | | 登録日 | 2023-02-22 | | 公開日 | 2023-08-30 | | 最終更新日 | 2023-12-06 | | 実験手法 | ELECTRON MICROSCOPY (2.97 Å) | | 主引用文献 | Structural basis of hydroxycarboxylic acid receptor signaling mechanisms through ligand binding.
Nat Commun, 14, 2023
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8K9K
 | | Full agonist-bound mu-type opioid receptor-G protein complex | | 分子名称: | DAMGO, G protein subunit alpha i3, Guanine nucleotide binding protein, ... | | 著者 | Hisano, T, Uchikubo-Kamo, T, Shirouzu, M, Imai, S, Kaneko, S, Shimada, I. | | 登録日 | 2023-08-01 | | 公開日 | 2024-05-29 | | 実験手法 | ELECTRON MICROSCOPY (2.98 Å) | | 主引用文献 | Structural and dynamic insights into the activation of the mu-opioid receptor by an allosteric modulator.
Nat Commun, 15, 2024
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8HNL
 | | CXCR3-DNGi complex activated by PS372424 | | 分子名称: | (3S)-N-[(2S)-5-carbamimidamido-1-(cyclohexylmethylamino)-1-oxidanylidene-pentan-2-yl]-2-(4-oxidanylidene-4-phenyl-butanoyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Jiao, H.Z, Hu, H.L. | | 登録日 | 2022-12-08 | | 公開日 | 2023-11-29 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (2.98 Å) | | 主引用文献 | Structural insights into the activation and inhibition of CXC chemokine receptor 3.
Nat.Struct.Mol.Biol., 31, 2024
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7XY6
 | | Adenosine receptor bound to an agonist in complex with G protein obtained by cryo-EM | | 分子名称: | 2-[6-azanyl-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylethanamide, 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, J.Y, Chen, Y, Hua, T, Song, G.J. | | 登録日 | 2022-05-31 | | 公開日 | 2023-05-03 | | 最終更新日 | 2023-05-31 | | 実験手法 | ELECTRON MICROSCOPY (2.99 Å) | | 主引用文献 | Cryo-EM structure of the human adenosine A 2B receptor-G s signaling complex.
Sci Adv, 8, 2022
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4Z34
 | | Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO9780307 | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, Lysophosphatidic acid receptor 1, Soluble cytochrome b562, ... | | 著者 | Chrencik, J.E, Roth, C.B, Terakado, M, Kurata, H, Omi, R, Kihara, Y, Warshaviak, D, Nakade, S, Asmar-Rovira, G, Mileni, M, Mizuno, H, Griffith, M.T, Rodgers, C, Han, G.W, Velasquez, J, Chun, J, Stevens, R.C, Hanson, M.A, GPCR Network (GPCR) | | 登録日 | 2015-03-30 | | 公開日 | 2015-06-03 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Cell, 161, 2015
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7C61
 | | Crystal structure of 5-HT1B-BRIL and SRP2070_Fab complex | | 分子名称: | 5-hydroxytryptamine receptor 1B,Soluble cytochrome b562,5-hydroxytryptamine receptor 1B, Ergotamine, IGG HEAVY CHAIN, ... | | 著者 | Suzuki, M, Miyagi, H, Asada, H, Yasunaga, M, Suno, C, Takahashi, Y, Saito, J, Iwata, S. | | 登録日 | 2020-05-21 | | 公開日 | 2020-07-29 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | The discovery of a new antibody for BRIL-fused GPCR structure determination.
Sci Rep, 10, 2020
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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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6A93
 | | Crystal structure of 5-HT2AR in complex with risperidone | | 分子名称: | 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, ... | | 著者 | 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. | | 登録日 | 2018-07-11 | | 公開日 | 2019-02-13 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Structures of the 5-HT2Areceptor in complex with the antipsychotics risperidone and zotepine.
Nat.Struct.Mol.Biol., 26, 2019
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8TH3
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8HJ5
 | | Cryo-EM structure of Gq-coupled MRGPRX1 bound with Compound-16 | | 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(q) subunit alpha, ... | | 著者 | Gan, B, Yu, L.Y, Ren, R.B. | | 登録日 | 2022-11-22 | | 公開日 | 2023-05-31 | | 最終更新日 | 2023-12-13 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Mechanism of agonist-induced activation of the human itch receptor MRGPRX1.
Plos Biol., 21, 2023
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8HQN
 | | Activation mechanism of GPR132 by 9(S)-HODE | | 分子名称: | (9S,10E,12Z)-9-hydroxyoctadeca-10,12-dienoic 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.L, Ding, J.H, Sun, J.P, Yu, X. | | 登録日 | 2022-12-13 | | 公開日 | 2023-10-11 | | 最終更新日 | 2023-11-01 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Functional screening and rational design of compounds targeting GPR132 to treat diabetes.
Nat Metab, 5, 2023
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7JNI
 | | Crystal structure of the angiotensin II type 2 receptoror (AT2R) in complex with EMA401 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, FORMIC ACID, HEXANE-1,6-DIOL, ... | | 著者 | Cherezov, V, Shaye, H, Han, G.W. | | 登録日 | 2020-08-04 | | 公開日 | 2022-02-09 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Inhibition of the angiotensin II type 2 receptor AT 2 R is a novel therapeutic strategy for glioblastoma.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7ZI0
 | | Structure of human Smoothened in complex with cholesterol and SAG | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-{[3-(pyridin-4-yl)phenyl]methyl}-1-benzothiophene-2-carboxamide, CHOLESTEROL, ... | | 著者 | Byrne, E.F.X, Woolley, R.E, Ansell, B, Sansom, M.S.P, Newstead, S, Siebold, C. | | 登録日 | 2022-04-07 | | 公開日 | 2022-06-15 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Patched 1 regulates Smoothened by controlling sterol binding to its extracellular cysteine-rich domain.
Sci Adv, 8, 2022
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8HN8
 | | Cryo-EM structure of ligand histamine-bound Histamine H4 receptor Gi complex | | 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(i) subunit alpha-1, ... | | 著者 | Tang, W.Q, Sun, X.Y, Li, F.H, Wang, J.Y. | | 登録日 | 2022-12-07 | | 公開日 | 2023-12-20 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structure insights into Histamine H4 receptor activation by an endogenous ligand histamine and agonist imetit
To Be Published
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8HOC
 | | Cryo-EM structure of ligand histamine-bound Histamine H4 receptor Gi complex | | 分子名称: | 2-(1~{H}-imidazol-5-yl)ethyl carbamimidothioate, 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 | Tang, W.Q, Sun, X.Y, Li, F.H, Wang, J.Y. | | 登録日 | 2022-12-09 | | 公開日 | 2023-12-20 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structure insights into Histamine H4 receptor activation by an endogenous ligand histamine and agonist imetit
To Be Published
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7KOO
 | | Alpha-7 nicotinic acetylcholine receptor bound to alpha-bungarotoxin in a resting state | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Alpha-bungarotoxin isoform V31, ... | | 著者 | Noviello, C.M, Hibbs, R.E, Gharpure, A, Mukhtasimova, N, Cabuco, R, Baxter, L, Borek, D, Sine, S. | | 登録日 | 2020-11-09 | | 公開日 | 2021-03-17 | | 最終更新日 | 2021-05-12 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structure and gating mechanism of the alpha 7 nicotinic acetylcholine receptor.
Cell, 184, 2021
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