8XZH
 
 | | Cryo-EM structure of the MM07-bound human APLNR-Gi complex | | Descriptor: | 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, ... | | Authors: | Wang, W, Ji, S, Zhang, Y. | | Deposit date: | 2024-01-21 | | Release date: | 2024-03-20 | | Last modified: | 2024-03-27 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structure-based design of non-hypertrophic apelin receptor modulator.
Cell, 187, 2024
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8XOF
 | | Cryo-EM structure of Lys05 bound GPR30-Gq complex structure | | Descriptor: | G protein subunit q, G-protein coupled estrogen receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, H, Xu, P, Xu, H.E. | | Deposit date: | 2024-01-01 | | Release date: | 2024-04-10 | | Last modified: | 2024-07-10 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structural and functional evidence that GPR30 is not a direct estrogen receptor.
Cell Res., 34, 2024
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7DW9
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7S8P
 | | CryoEM structure of Gq-coupled MRGPRX4 with small molecule agonist MS47134 | | Descriptor: | Gs-mini-Gq chimera, 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: | Cao, C, Fay, J.F, Gumpper, R.H, Roth, B.L. | | Deposit date: | 2021-09-18 | | Release date: | 2021-11-17 | | Last modified: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
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7PYR
 | | Crystal structure of the adenosine A2A receptor (A2A-PSB1-bRIL) in complex with preladenant conjugate PSB-2115 | | Descriptor: | (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, ... | | Authors: | 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. | | Deposit date: | 2021-10-11 | | Release date: | 2022-03-02 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | 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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4UG2
 | | Thermostabilised HUMAN A2a Receptor with CGS21680 bound | | Descriptor: | (2S)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE, THERMOSTABILISED HUMAN A2A RECEPTOR | | Authors: | Lebon, G, Edwards, P.C, Leslie, A.G.W, Tate, C.G. | | Deposit date: | 2015-03-21 | | Release date: | 2015-04-08 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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3EML
 | | The 2.6 A Crystal Structure of a Human A2A Adenosine Receptor bound to ZM241385. | | Descriptor: | 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol, Human Adenosine A2A receptor/T4 lysozyme chimera, STEARIC ACID, ... | | Authors: | Jaakola, V.-P, Griffith, M.T, Hanson, M.A, Cherezov, V, Chien, E.Y.T, Lane, J.R, Ijzerman, A.P, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | Deposit date: | 2008-09-24 | | Release date: | 2008-10-14 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist.
Science, 322, 2008
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8DCR
 | | Cryo-EM structure of dobutamine-bound beta1-adrenergic receptor in complex with heterotrimeric Gs-protein | | Descriptor: | DOBUTAMINE, Endolysin,Endolysin,Beta-1 adrenergic receptor chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Su, M, Paknejad, N, Hite, R.K, Huang, X.Y. | | Deposit date: | 2022-06-17 | | Release date: | 2022-07-27 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structures of beta 1 -adrenergic receptor in complex with Gs and ligands of different efficacies.
Nat Commun, 13, 2022
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7WC6
 | | Crystal structure of serotonin 2A receptor in complex with LSD | | Descriptor: | (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, ... | | Authors: | 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. | | Deposit date: | 2021-12-18 | | Release date: | 2022-01-26 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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7WC7
 | | Crystal structure of serotonin 2A receptor in complex with lisuride | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2A,5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, CHOLESTEROL, ... | | Authors: | 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. | | Deposit date: | 2021-12-18 | | Release date: | 2022-01-26 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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8J24
 | | Cryo-EM structure of FFAR2 complex bound with acetic acid | | Descriptor: | ACETATE ION, Free fatty acid receptor 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Tai, L, Li, F, Tang, W, Sun, X, Wang, J. | | Deposit date: | 2023-04-14 | | Release date: | 2024-01-24 | | Last modified: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Molecular recognition and activation mechanism of short-chain fatty acid receptors FFAR2/3.
Cell Res., 34, 2024
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5U09
 | | High-resolution crystal structure of the human CB1 cannabinoid receptor | | Descriptor: | Cannabinoid receptor 1,GlgA glycogen synthase, DI(HYDROXYETHYL)ETHER, N-[(2S,3S)-4-(4-chlorophenyl)-3-(3-cyanophenyl)butan-2-yl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide, ... | | Authors: | Shao, Z.H, Yin, J, Rosenbaum, D. | | Deposit date: | 2016-11-23 | | Release date: | 2016-12-07 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | High-resolution crystal structure of the human CB1 cannabinoid receptor.
Nature, 2016
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7F1T
 | | Crystal structure of the human chemokine receptor CCR5 in complex with MIP-1a | | Descriptor: | C-C motif chemokine 3,C-C chemokine receptor type 5,Rubredoxin,C-C chemokine receptor type 5, ZINC ION | | Authors: | Zhang, H, Chen, K, Tan, Q, Han, S, Zhu, Y, Zhao, Q, Wu, B. | | Deposit date: | 2021-06-09 | | Release date: | 2021-07-14 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structural basis for chemokine recognition and receptor activation of chemokine receptor CCR5.
Nat Commun, 12, 2021
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8JZ7
 | | Cryo-EM structure of MK-6892-bound HCAR2 in complex with Gi protein | | Descriptor: | 2-[[2,2-dimethyl-3-[3-(5-oxidanylpyridin-2-yl)-1,2,4-oxadiazol-5-yl]propanoyl]amino]cyclohexene-1-carboxylic 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: | Zhao, C, Tian, X.W, Liu, Y, Cheng, L, Yan, W, Shao, Z.H. | | Deposit date: | 2023-07-04 | | Release date: | 2023-10-04 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Orthosteric ligand selectivity and allosteric probe dependence at Hydroxycarboxylic acid receptor HCAR2.
Signal Transduct Target Ther, 8, 2023
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7TD4
 | | Sphingosine-1-phosphate receptor 1-Gi complex bound to Siponimod | | Descriptor: | 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, ... | | Authors: | Liu, S, Paknejad, N, Zhu, L, Kihara, Y, Ray, D, Chun, J, Liu, W, Hite, R.K, Huang, X.Y. | | Deposit date: | 2021-12-30 | | Release date: | 2022-02-09 | | Last modified: | 2022-02-23 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate.
Nat Commun, 13, 2022
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6PS4
 | | XFEL beta2 AR structure by ligand exchange from Timolol to ICI-118551. | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]butan-2-ol, CHOLESTEROL, ... | | Authors: | Ishchenko, A, Stauch, B, Han, G.W, Batyuk, A, Shiriaeva, A, Li, C, Zatsepin, N.A, Weierstall, U, Liu, W, Nango, E, Nakane, T, Tanaka, R, Tono, K, Joti, Y, Iwata, S, Moraes, I, Gati, C, Cherezov, C. | | Deposit date: | 2019-07-12 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Toward G protein-coupled receptor structure-based drug design using X-ray lasers.
Iucrj, 6, 2019
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7BU7
 | | Structure of human beta1 adrenergic receptor bound to BI-167107 and nanobody 6B9 | | Descriptor: | (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, ... | | Authors: | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | Deposit date: | 2020-04-04 | | Release date: | 2020-12-02 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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1L9H
 | | Crystal structure of bovine rhodopsin at 2.6 angstroms RESOLUTION | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, HEPTANE-1,2,3-TRIOL, MERCURY (II) ION, ... | | Authors: | Okada, T, Fujiyoshi, Y, Silow, M, Navarro, J, Landau, E.M, Shichida, Y. | | Deposit date: | 2002-03-23 | | Release date: | 2002-05-15 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Functional role of internal water molecules in rhodopsin revealed by X-ray crystallography.
Proc.Natl.Acad.Sci.USA, 99, 2002
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7JJO
 | | Structural Basis of the Activation of Heterotrimeric Gs-protein by Isoproterenol-bound Beta1-Adrenergic Receptor | | Descriptor: | Beta1-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, ... | | Authors: | Su, M, Zhu, L, Zhang, Y, Paknejad, N, Dey, R, Huang, J, Lee, M.Y, Williams, D, Jordan, K.D, Eng, E.T, Ernst, O.P, Meyerson, J.R, Hite, R.K, Walz, T, Liu, W, Huang, X.Y. | | Deposit date: | 2020-07-27 | | Release date: | 2020-09-02 | | Last modified: | 2020-10-14 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structural Basis of the Activation of Heterotrimeric Gs-Protein by Isoproterenol-Bound beta 1 -Adrenergic Receptor.
Mol.Cell, 80, 2020
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7VL9
 | | Cryo-EM structure of the CCL15(26-92) bound CCR1-Gi complex | | Descriptor: | C-C chemokine receptor type 1, CCL15(26-92), CHOLESTEROL, ... | | Authors: | Shao, Z, Shen, Q, Mao, C, Yao, B, Chen, L, Zhang, H, Shen, D, Zhang, C, Li, W, Du, X, Li, F, Ma, H, Chen, Z, Xu, H.E, Ying, S, Zhang, Y, Shen, H. | | Deposit date: | 2021-10-02 | | Release date: | 2022-03-23 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Identification and mechanism of G protein-biased ligands for chemokine receptor CCR1.
Nat.Chem.Biol., 18, 2022
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8J6Q
 | | Cryo-EM structure of the 3-HB and compound 9n-bound human HCAR2-Gi1 complex | | Descriptor: | (3R)-3-hydroxybutanoic acid, 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, ... | | Authors: | Mao, C, Gao, M, Zang, S, Zhu, Y, Ma, X, Zhang, Y. | | Deposit date: | 2023-04-26 | | Release date: | 2023-12-06 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Orthosteric and allosteric modulation of human HCAR2 signaling complex.
Nat Commun, 14, 2023
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5VBL
 | | Structure of apelin receptor in complex with agonist peptide | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Apelin receptor,Rubredoxin,Apelin receptor Chimera, ZINC ION, ... | | Authors: | Ma, Y, Yue, Y, Ma, Y, Zhang, Q, Zhou, Q, Song, Y, Shen, Y, Li, X, Ma, X, Li, C, Hanson, M.A, Han, G.W, Sickmier, E.A, Swaminath, G, Zhao, S, Stevems, R.C, Hu, L.A, Zhong, W, Zhang, M, Xu, F. | | Deposit date: | 2017-03-29 | | Release date: | 2017-05-31 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structural Basis for Apelin Control of the Human Apelin Receptor
Structure, 25, 2017
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7WQ4
 | | Galanin-bound galanin receptor 2 in complex with Gq | | Descriptor: | CHOLESTEROL, Engineered Guanine nucleotide-binding protein G(q) subunit alpha, Galanin, ... | | Authors: | Duan, J, Shen, D.D, Xu, H.E, Zhang, Y, Jiang, Y. | | Deposit date: | 2022-01-24 | | Release date: | 2022-04-20 | | Last modified: | 2022-10-19 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Molecular basis for allosteric agonism and G protein subtype selectivity of galanin receptors
Nat Commun, 13, 2022
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5WF5
 | | Agonist bound human A2a adenosine receptor with D52N mutation at 2.60 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 (2.6 Å) | | Cite: | Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling.
Structure, 26, 2018
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2Y02
 | | TURKEY BETA1 ADRENERGIC RECEPTOR WITH STABILISING MUTATIONS AND BOUND AGONIST CARMOTEROL | | Descriptor: | BETA-1 ADRENERGIC RECEPTOR, CARMOTEROL, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Warne, A, Moukhametzianov, R, Baker, J.G, Nehme, R, Edwards, P.C, Leslie, A.G.W, Schertler, G.F.X, Tate, C.G. | | Deposit date: | 2010-11-30 | | Release date: | 2011-01-12 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | The Structural Basis for Agonist and Partial Agonist Action on a Beta1-Adrenergic Receptor
Nature, 469, 2011
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