8JPN
| Cryo-EM structure of succinate receptor bound to cis-epoxysuccinic acid coupling to Gi | Descriptor: | (2R,3S)-oxirane-2,3-dicarboxylic 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: | Wang, T.X, Tang, W.Q, Li, F.H, Wang, J.Y. | Deposit date: | 2023-06-12 | Release date: | 2024-05-22 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | Molecular activation and G protein coupling selectivity of human succinate receptor SUCR1. Cell Res., 2024
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6OS0
| Structure of synthetic nanobody-stabilized angiotensin II type 1 receptor bound to angiotensin II | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Angiotensinogen, CHLORIDE ION, ... | Authors: | Wingler, L.M, Staus, D.P, Skiba, M.A, McMahon, C, Kleinhenz, A.L.W, Lefkowitz, R.J, Kruse, A.C. | Deposit date: | 2019-05-01 | Release date: | 2020-02-19 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR. Science, 367, 2020
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4Z35
| Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO-9910539 | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 3-{1-[(2S,3S)-3-(4-acetyl-3,5-dimethoxyphenyl)-2-(2,3-dihydro-1H-inden-2-ylmethyl)-3-hydroxypropyl]-4-(methoxycarbonyl)-1H-pyrrol-3-yl}propanoic acid, Lysophosphatidic acid receptor 1,Soluble cytochrome b562 | Authors: | 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) | Deposit date: | 2015-03-30 | Release date: | 2015-06-03 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1. Cell, 161, 2015
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7E33
| Serotonin 1E (5-HT1E) receptor-Gi protein complex | Descriptor: | 3-(1-methylpiperidin-4-yl)-1H-indol-5-ol, 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: | Xu, P, Huang, S, Zhang, H, Mao, C, Zhou, X.E, Shen, D.D, Jiang, Y, Zhang, Y, Xu, H.E. | Deposit date: | 2021-02-07 | Release date: | 2021-04-14 | Last modified: | 2021-04-28 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | Structural insights into the lipid and ligand regulation of serotonin receptors. Nature, 592, 2021
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7E32
| Serotonin 1D (5-HT1D) receptor-Gi protein complex | Descriptor: | 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, ... | Authors: | Xu, P, Huang, S, Zhang, H, Mao, C, Zhou, X.E, Shen, D.D, Jiang, Y, Zhang, Y, Xu, H.E. | Deposit date: | 2021-02-07 | Release date: | 2021-04-21 | Last modified: | 2021-04-28 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | Structural insights into the lipid and ligand regulation of serotonin receptors. Nature, 592, 2021
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7VOE
| Crystal structure of 5-HT2AR in complex with aripiprazole | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, 7-[4-[4-[2,3-bis(chloranyl)phenyl]piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one, ... | Authors: | Chen, Z, Fan, L, Wang, H, Yu, J, Lu, D, Qi, J, Nie, F, Luo, Z, Liu, Z, Cheng, J, Wang, S. | Deposit date: | 2021-10-13 | Release date: | 2021-12-22 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. Nat.Neurosci., 25, 2022
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7W56
| Cryo-EM structure of the neuromedin S-bound neuromedin U receptor 1-Gq protein complex | 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(q) subunit alpha, ... | Authors: | You, C, Xu, H.E, Jiang, Y. | Deposit date: | 2021-11-29 | Release date: | 2022-04-20 | Last modified: | 2022-12-07 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | Structural insights into the peptide selectivity and activation of human neuromedin U receptors. Nat Commun, 13, 2022
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4YAY
| XFEL structure of human Angiotensin Receptor | Descriptor: | 5,7-diethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-3,4-dihydro-1,6-naphthyridin-2(1H)-one, Soluble cytochrome b562,Type-1 angiotensin II receptor | Authors: | Zhang, H, Unal, H, Gati, C, Han, G.W, Zatsepin, N.A, James, D, Wang, D, Nelson, G, Weierstall, U, Messerschmidt, M, Williams, G.J, Boutet, S, Yefanov, O.M, White, T.A, Liu, W, Ishchenko, A, Tirupula, K.C, Desnoyer, R, Sawaya, M.C, Xu, Q, Coe, J, Cornrad, C.E, Fromme, P, Stevens, R.C, Katritch, V, Karnik, S.S, Cherezov, V, GPCR Network (GPCR) | Deposit date: | 2015-02-18 | Release date: | 2015-04-22 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structure of the Angiotensin receptor revealed by serial femtosecond crystallography. Cell, 161, 2015
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7Y15
| Cryo-EM structure of apo-state MrgD-Gi complex | 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: | Suzuki, S, Iida, M, Kawamoto, A, Oshima, A. | Deposit date: | 2022-06-06 | Release date: | 2022-07-20 | Last modified: | 2022-11-23 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | Structural insight into the activation mechanism of MrgD with heterotrimeric Gi-protein revealed by cryo-EM. Commun Biol, 5, 2022
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5WF6
| Agonist bound human A2a adenosine receptor with S91A mutation at 2.90 A resolution | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 6-(2,2-diphenylethylamino)-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxy-oxolan-2-yl]-N-[2-[(1-pyridin-2-ylpiperidin-4-yl)carbamoylamino]ethyl]purine-2-carboxamide, Human A2a adenosine receptor T4L chimera | Authors: | White, K.L, Eddy, M.T, Gao, Z, Han, G.W, Hanson, M.A, Lian, T, Deary, A, Patel, N, Jacobson, K.A, Katritch, V, Stevens, R.C. | Deposit date: | 2017-07-11 | Release date: | 2018-02-21 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling. Structure, 26, 2018
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5TVN
| Crystal structure of the LSD-bound 5-HT2B receptor | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide, CHOLESTEROL, ... | Authors: | Wacker, D, Wang, S, McCorvy, J.D, Betz, R.M, Venkatakrishnan, A.J, Levit, A, Lansu, K, Schools, Z.L, Che, T, Nichols, D.E, Shoichet, B.K, Dror, R.O, Roth, B.L. | Deposit date: | 2016-11-09 | Release date: | 2017-02-01 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Crystal Structure of an LSD-Bound Human Serotonin Receptor. Cell, 168, 2017
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6AK3
| Crystal structure of the human prostaglandin E receptor EP3 bound to prostaglandin E2 | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, (Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxo-cyclopentyl]hept-5-enoic acid, Prostaglandin E2 receptor EP3 subtype,Soluble cytochrome b562 | Authors: | Morimoto, K, Suno, R, Iwata, S, Kobayashi, T. | Deposit date: | 2018-08-29 | Release date: | 2018-12-05 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Crystal structure of the endogenous agonist-bound prostanoid receptor EP3. Nat. Chem. Biol., 15, 2019
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6DO1
| Structure of nanobody-stabilized angiotensin II type 1 receptor bound to S1I8 | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, Angiotensin-like peptide S1I8, ... | Authors: | Wingler, L.M, McMahon, C, Staus, D.P, Lefkowitz, R.J, Kruse, A.C. | Deposit date: | 2018-06-08 | Release date: | 2019-01-30 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.901 Å) | Cite: | Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody. Cell, 176, 2019
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6DRY
| Structural Determinants of Activation and Biased Agonism at the 5-HT2B Receptor | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (8beta)-N-[(2S)-1-hydroxybutan-2-yl]-6-methyl-9,10-didehydroergoline-8-carboxamide, 5HT2B receptor, ... | Authors: | 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. | Deposit date: | 2018-06-13 | Release date: | 2018-08-29 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.918 Å) | Cite: | 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- | Descriptor: | 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, ... | Authors: | Lees, J.A, Dias, J.M, Han, S. | Deposit date: | 2023-06-28 | Release date: | 2023-10-04 | Method: | ELECTRON MICROSCOPY (2.94 Å) | Cite: | 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 | Descriptor: | 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, ... | Authors: | Jiao, H.Z, Hu, H.L. | Deposit date: | 2022-12-08 | Release date: | 2023-11-29 | Last modified: | 2024-05-01 | Method: | ELECTRON MICROSCOPY (2.94 Å) | Cite: | Structural insights into the activation and inhibition of CXC chemokine receptor 3. Nat.Struct.Mol.Biol., 31, 2024
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7F83
| Crystal Structure of a receptor in Complex with inverse agonist | Descriptor: | (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 | Authors: | Xu, Z, Shao, Z. | Deposit date: | 2021-07-01 | Release date: | 2022-01-19 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.94 Å) | Cite: | Molecular mechanism of agonism and inverse agonism in ghrelin receptor. Nat Commun, 13, 2022
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8FYL
| Vilazodone-bound serotonin 1A (5-HT1A) receptor-Gi1 protein complex | Descriptor: | 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, ... | Authors: | Warren, A.L, Zilberg, G, Capper, M.J, Wacker, D. | Deposit date: | 2023-01-26 | Release date: | 2024-05-15 | Last modified: | 2024-06-19 | Method: | ELECTRON MICROSCOPY (2.94 Å) | Cite: | Structural pharmacology and therapeutic potential of 5-methoxytryptamines. Nature, 630, 2024
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8HQM
| Activation mechanism of GPR132 by NPGLY | 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: | Wang, J.L, Ding, J.H, Sun, J.P, Yu, X. | Deposit date: | 2022-12-13 | Release date: | 2023-10-11 | Last modified: | 2023-11-01 | Method: | ELECTRON MICROSCOPY (2.95 Å) | Cite: | 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 | Descriptor: | 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 | Authors: | 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. | Deposit date: | 2018-03-23 | Release date: | 2018-11-21 | Last modified: | 2022-03-23 | Method: | X-RAY DIFFRACTION (2.95 Å) | Cite: | Structural insights into the subtype-selective antagonist binding to the M2muscarinic receptor Nat. Chem. Biol., 14, 2018
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8DRK
| LRRC8A:C conformation 1 (round) top focus | Descriptor: | 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine, Volume-regulated anion channel subunit LRRC8A,Soluble cytochrome b562, Volume-regulated anion channel subunit LRRC8C | Authors: | Kern, D.M, Brohawn, S.G. | Deposit date: | 2022-07-21 | Release date: | 2023-03-08 | Last modified: | 2023-07-05 | Method: | ELECTRON MICROSCOPY (2.95 Å) | Cite: | 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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8ZSV
| Cryo-EM structure of the RO5263397-bound mTAAR1-Gs complex | Descriptor: | (4~{S})-4-(3-fluoranyl-2-methyl-phenyl)-1,3-oxazolidin-2-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, ... | Authors: | Jiang, K.X, Zheng, Y, Xu, F. | Deposit date: | 2024-06-05 | Release date: | 2024-07-24 | Method: | ELECTRON MICROSCOPY (2.96 Å) | Cite: | The versatile binding landscape of the TAAR1 pocket for LSD and other antipsychotic drug molecules. Cell Rep, 43, 2024
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8ZFM
| Caenorhabditis elegans ACR-23 in betaine bound state | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Betaine receptor acr-23,Soluble cytochrome b562, ... | Authors: | Chen, Q.F, Liu, F.L, Li, T.Y, Gong, H.H, Guo, F, Liu, S. | Deposit date: | 2024-05-08 | Release date: | 2024-07-31 | Method: | ELECTRON MICROSCOPY (2.96 Å) | Cite: | Structural basis of acetylcholine receptor like-23 (ACR-23) activation by anthelmintics monepantel and betaine To Be Published
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8HQE
| Cryo-EM structure of the apo-GPR132-Gi | 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: | Wang, J.L, Ding, J.H, Sun, J.P, Yu, X. | Deposit date: | 2022-12-13 | Release date: | 2023-10-11 | Last modified: | 2023-11-01 | Method: | ELECTRON MICROSCOPY (2.97 Å) | Cite: | 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 | Descriptor: | 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, ... | Authors: | Suzuki, S, Nishikawa, K, Suzuki, H, Fujiyoshi, Y. | Deposit date: | 2023-02-22 | Release date: | 2023-08-30 | Last modified: | 2023-12-06 | Method: | ELECTRON MICROSCOPY (2.97 Å) | Cite: | Structural basis of hydroxycarboxylic acid receptor signaling mechanisms through ligand binding. Nat Commun, 14, 2023
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