6N48
| Structure of beta2 adrenergic receptor bound to BI167107, Nanobody 6B9, and a positive allosteric modulator | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid Antibody Fragment, ... | Authors: | Liu, X, Masoudi, A, Kahsai, A.W, Huang, L.Y, Pani, B, Hirata, K, Ahn, S, Lefkowitz, R.J, Kobilka, B.K. | Deposit date: | 2018-11-17 | Release date: | 2019-06-26 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Mechanism of beta2AR regulation by an intracellular positive allosteric modulator. Science, 364, 2019
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6I9K
| Crystal structure of Jumping Spider Rhodopsin-1 bound to 9-cis retinal | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Kumopsin1, RETINAL | Authors: | Varma, N, Mutt, E, Muehle, J, Panneels, V, Terakita, A, Deupi, X, Nogly, P, Schertler, F.X.G, Lesca, E. | Deposit date: | 2018-11-23 | Release date: | 2019-07-03 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.145 Å) | Cite: | Crystal structure of jumping spider rhodopsin-1 as a light sensitive GPCR. Proc.Natl.Acad.Sci.USA, 116, 2019
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6IBB
| Crystal structure of the rat isoform of the succinate receptor SUCNR1 (GPR91) in complex with a nanobody | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2~{S},5~{R})-hexane-2,5-diol, CHOLESTEROL, ... | Authors: | Haffke, M, Jaakola, V.-P. | Deposit date: | 2018-11-29 | Release date: | 2019-08-14 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.12 Å) | Cite: | Structural basis of species-selective antagonist binding to the succinate receptor. Nature, 574, 2019
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6PT2
| Crystal structure of the active delta opioid receptor in complex with the peptide agonist KGCHM07 | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CHOLESTEROL, Delta opioid receptor, ... | Authors: | Claff, T, Yu, J, Blais, V, Patel, N, Martin, C, Wu, L, Han, G.W, Holleran, B.J, Van der Poorten, O, Hanson, M.A, Sarret, P, Gendron, L, Cherezov, V, Katritch, V, Ballet, S, Liu, Z, Muller, C.E, Stevens, R.C. | Deposit date: | 2019-07-14 | Release date: | 2019-12-11 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Elucidating the active delta-opioid receptor crystal structure with peptide and small-molecule agonists. Sci Adv, 5, 2019
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6PT3
| Crystal structure of the active delta opioid receptor in complex with the small molecule agonist DPI-287 | Descriptor: | 4-[(R)-[(2S,5R)-4-benzyl-2,5-dimethylpiperazin-1-yl](3-hydroxyphenyl)methyl]-N,N-diethylbenzamide, Delta opioid receptor | Authors: | Claff, T, Yu, J, Blais, V, Patel, N, Martin, C, Wu, L, Han, G.W, Holleran, B.J, Van der Poorten, O, Hanson, M.A, Sarret, P, Gendron, L, Cherezov, V, Katritch, V, Ballet, S, Liu, Z, Muller, C.E, Stevens, R.C. | Deposit date: | 2019-07-14 | Release date: | 2019-12-11 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | Elucidating the active delta-opioid receptor crystal structure with peptide and small-molecule agonists. Sci Adv, 5, 2019
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6IGL
| Crystal Structure of human ETB receptor in complex with IRL1620 | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CITRIC ACID, Endothelin receptor type B,Endolysin,Endothelin receptor type B, ... | Authors: | Shihoya, W, Izume, T, Inoue, A, Yamashita, K, kadji, F.M.N, Hirata, K, Aoki, J, Nishizawa, T, Nureki, O. | Deposit date: | 2018-09-25 | Release date: | 2018-11-21 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Crystal structures of human ETBreceptor provide mechanistic insight into receptor activation and partial activation. Nat Commun, 9, 2018
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6KR8
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8EA0
| CryoEM structure of miniGq-coupled hM3R in complex with iperoxo (local refinement) | Descriptor: | 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, CHOLESTEROL HEMISUCCINATE, Muscarinic acetylcholine receptor M3 | Authors: | Zhang, S, Fay, J.F, Roth, B.L. | Deposit date: | 2022-08-27 | Release date: | 2022-11-30 | Last modified: | 2022-12-21 | Method: | ELECTRON MICROSCOPY (2.56 Å) | Cite: | Molecular basis for selective activation of DREADD-based chemogenetics. Nature, 612, 2022
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8E0G
| Re-refined model of active mu-opioid receptor (PDB 5c1m) as an adduct with BU72 | Descriptor: | (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, ... | Authors: | Munro, T.A. | Deposit date: | 2022-08-09 | Release date: | 2023-10-18 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Reanalysis of a mu opioid receptor crystal structure reveals a covalent adduct with BU72. Bmc Biol., 21, 2023
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5YHL
| Crystal structure of the human prostaglandin E receptor EP4 in complex with Fab and an antagonist Br-derivative | Descriptor: | 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, ... | Authors: | Toyoda, Y, Morimoto, K, Suno, R, Horita, S, Iwata, S, Kobayashi, T. | Deposit date: | 2017-09-28 | Release date: | 2018-12-05 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (4.2 Å) | Cite: | 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 | Descriptor: | 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, ... | Authors: | Toyoda, Y, Morimoto, K, Suno, R, Horita, S, Iwata, S, Kobayashi, T. | Deposit date: | 2017-11-30 | Release date: | 2018-12-05 | Last modified: | 2018-12-19 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Ligand binding to human prostaglandin E receptor EP4at the lipid-bilayer interface. Nat. Chem. Biol., 15, 2019
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5WB1
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8GNG
| Crystal structure of human adenosine A2A receptor in complex with istradefylline. | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 8-[(~{E})-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6-dione, Adenosine receptor A2a, ... | Authors: | Suzuki, M, Saito, J, Miyagi, H, Yasunaga, M. | Deposit date: | 2022-08-23 | Release date: | 2023-03-22 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A 2A Receptor Antagonist/Inverse Agonist. Mol.Pharmacol., 103, 2023
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7SK9
| Cryo-EM structure of human ACKR3 in complex with a small molecule partial agonist CCX662, and an intracellular Fab | Descriptor: | (1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium, Atypical chemokine receptor 3, CHOLESTEROL, ... | Authors: | Yen, Y.C, Schafer, C.T, Gustavsson, M, Handel, T.M, Tesmer, J.J.G. | Deposit date: | 2021-10-19 | Release date: | 2022-07-27 | Method: | ELECTRON MICROSCOPY (3.7 Å) | Cite: | Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias. Sci Adv, 8, 2022
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7SRQ
| 5-HT2B receptor bound to LSD obtained by cryo-electron microscopy (cryoEM) | Descriptor: | (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide, 2-acetamido-2-deoxy-beta-D-glucopyranose, 5-hydroxytryptamine receptor 2B | Authors: | Barros-Alvarez, X, Cao, C, Panova, O, Roth, B.L, Skiniotis, G. | Deposit date: | 2021-11-08 | Release date: | 2022-09-21 | Last modified: | 2022-10-19 | Method: | ELECTRON MICROSCOPY (2.7 Å) | Cite: | Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD. Neuron, 110, 2022
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7TUY
| Cryo-EM structure of GSK682753A-bound EBI2/GPR183 | Descriptor: | 8-[(2E)-3-(4-chlorophenyl)prop-2-enoyl]-3-[(3,4-dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one, G-protein coupled receptor 183,Soluble cytochrome b562 fusion, anti-BRIL Fab Heavy chain, ... | Authors: | Chen, H, Huang, W, Li, X. | Deposit date: | 2022-02-03 | Release date: | 2022-04-13 | Last modified: | 2022-07-20 | Method: | ELECTRON MICROSCOPY (2.98 Å) | Cite: | Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response. Structure, 30, 2022
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7UL5
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7UL3
| CryoEM Structure of Inactive H2R Bound to Famotidine, Nb6M, and NabFab | Descriptor: | Histamine H2 receptor, NabFab HC, NabFab LC, ... | Authors: | Robertson, M.J, Skiniotis, G. | Deposit date: | 2022-04-03 | Release date: | 2022-06-29 | Last modified: | 2022-12-28 | Method: | ELECTRON MICROSCOPY (3 Å) | Cite: | Structure determination of inactive-state GPCRs with a universal nanobody. Nat.Struct.Mol.Biol., 29, 2022
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7UL2
| CryoEM Structure of Inactive NTSR1 Bound to SR48692 and Nb6 | Descriptor: | 2-[[1-(7-chloranylquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazol-3-yl]carbonylamino]adamantane-2-carboxylic acid, Nanobody 6, Neurotensin receptor 1, ... | Authors: | Robertson, M.J, Skiniotis, G. | Deposit date: | 2022-04-03 | Release date: | 2022-06-29 | Last modified: | 2022-12-28 | Method: | ELECTRON MICROSCOPY (2.4 Å) | Cite: | Structure determination of inactive-state GPCRs with a universal nanobody. Nat.Struct.Mol.Biol., 29, 2022
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7UL4
| CryoEM Structure of Inactive MOR Bound to Alvimopan and Mb6 | Descriptor: | Megabody 6, Mu-type opioid receptor, N-[(2S)-2-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl}-3-phenylpropanoyl]glycine | Authors: | Robertson, M.J, Skiniotis, G. | Deposit date: | 2022-04-03 | Release date: | 2022-06-29 | Last modified: | 2022-12-28 | Method: | ELECTRON MICROSCOPY (2.8 Å) | Cite: | Structure determination of inactive-state GPCRs with a universal nanobody. Nat.Struct.Mol.Biol., 29, 2022
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8WCC
| Cryo-EM structure of the CHA-bound mTAAR1 complex | Descriptor: | CYCLOHEXYLAMMONIUM ION, Trace amine-associated receptor 1 | Authors: | Rong, N.K, Guo, L.L, Zhang, M.H, Li, Q, Yang, F, Sun, J.P. | Deposit date: | 2023-09-11 | Release date: | 2023-12-27 | Method: | ELECTRON MICROSCOPY (3.04 Å) | Cite: | Structural and signaling mechanisms of TAAR1 enabled preferential agonist design. Cell, 186, 2023
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8WDT
| Crystal structure of the human adenosine A2A receptor in complex with photoresponsive ligand photoNECA(blue) | Descriptor: | (2S,3S,4R,5R)-5-(6-amino-2-((E)-phenyldiazenyl)-9H-purin-9-yl)-N-ethyl-3,4-dihydroxytetrahydrofuran-2-carboxamide, Adenosine receptor A2a, Antibody Fab fragment heavy chain, ... | Authors: | Araya, T, Asada, H, Iwata, S, Im, D.H. | Deposit date: | 2023-09-16 | Release date: | 2024-01-17 | Method: | X-RAY DIFFRACTION (3.34 Å) | Cite: | Crystal structure reveals the binding mode and selectivity of a photoswitchable ligand for the adenosine A 2A receptor. Biochem.Biophys.Res.Commun., 695, 2023
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8W8S
| Cryo-EM structure of the AA14-bound GPR101 complex | Descriptor: | 1-(4-methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea, Probable G-protein coupled receptor 101 | Authors: | Sun, J.P, Yu, X, Gao, N, Yang, F, Wang, J.Y, Yang, Z, Guan, Y, Wang, G.P. | Deposit date: | 2023-09-04 | Release date: | 2024-01-03 | Last modified: | 2024-04-10 | Method: | ELECTRON MICROSCOPY (3.3 Å) | Cite: | Structure of GPR101-Gs enables identification of ligands with rejuvenating potential. Nat.Chem.Biol., 20, 2024
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8XBG
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8WKY
| Crystal structure of the Melanocortin-4 Receptor (MC4R) in complex with S25 | Descriptor: | CALCIUM ION, Melanocortin receptor 4, N-(2-aminoethyl)-5-(2-{[4-(morpholin-4-yl)pyridin-2-yl]amino}-1,3-thiazol-5-yl)pyridine-3-carboxamide, ... | Authors: | Gimenez, L.E, Martin, C, Yu, J, Hollanders, C, Hernandez, C, Dahir, N.S, Wu, Y, Yao, D, Han, G.W, Wu, L, Poorten, O.V, Lamouroux, A, Mannes, M, Tourwe, D, Zhao, S, Stevens, R.C, Cone, R.D, Ballet, S. | Deposit date: | 2023-09-28 | Release date: | 2024-08-07 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design. J.Med.Chem., 67, 2024
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