6LI1
 
 | | Crystal structure of GPR52 ligand free form with flavodoxin fusion | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Chimera of G-protein coupled receptor 52 and Flavodoxin, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Luo, Z.P, Lin, X, Xu, F, Han, G.W. | | Deposit date: | 2019-12-10 | | Release date: | 2020-02-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structural basis of ligand recognition and self-activation of orphan GPR52.
Nature, 579, 2020
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4Z36
 | | Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO-3080573 | | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 1-(4-{[(2S,3R)-2-(2,3-dihydro-1H-inden-2-yloxy)-3-(3,5-dimethoxy-4-methylphenyl)-3-hydroxypropyl]oxy}phenyl)cyclopropanecarboxylic 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: | 2015-07-01 | | 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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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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7VDH
 | | Cryo-EM structure of pseudoallergen receptor MRGPRX2 complex with C48/80, state2 | | Descriptor: | 2-[4-methoxy-3-[[2-methoxy-3-[[2-methoxy-5-[2-(methylamino)ethyl]phenyl]methyl]-5-[2-(methylamino)ethyl]phenyl]methyl]phenyl]-~{N}-methyl-ethanamine, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, Y, Yang, F. | | Deposit date: | 2021-09-07 | | Release date: | 2021-12-01 | | Last modified: | 2022-07-20 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structure, function and pharmacology of human itch receptor complexes.
Nature, 600, 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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4XEE
 | | Structure of active-like neurotensin receptor | | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CITRATE ANION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Krumm, B.E, White, J.F, Shah, P, Grisshammer, R. | | Deposit date: | 2014-12-23 | | Release date: | 2015-07-29 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structural prerequisites for G-protein activation by the neurotensin receptor.
Nat Commun, 6, 2015
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3OE0
 | | Crystal structure of the CXCR4 chemokine receptor in complex with a cyclic peptide antagonist CVX15 | | Descriptor: | C-X-C chemokine receptor type 4, Lysozyme Chimera, Polyphemusin analog, ... | | Authors: | Wu, B, Mol, C.D, Han, G.W, Katritch, V, Chien, E.Y.T, Liu, W, Cherezov, V, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | Deposit date: | 2010-08-12 | | Release date: | 2010-10-27 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science, 330, 2010
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7VKT
 | | cryo-EM structure of LTB4-bound BLT1 in complex with Gi protein | | Descriptor: | CHOLESTEROL HEMISUCCINATE, 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: | He, Y, Wang, N. | | Deposit date: | 2021-10-01 | | Release date: | 2022-03-09 | | Last modified: | 2022-03-23 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural basis of leukotriene B4 receptor 1 activation.
Nat Commun, 13, 2022
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7VL8
 | | Cryo-EM structure of the Apo CCR1-Gi complex | | Descriptor: | C-C chemokine receptor type 1, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 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 (2.9 Å) | | Cite: | Identification and mechanism of G protein-biased ligands for chemokine receptor CCR1.
Nat.Chem.Biol., 18, 2022
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8HN1
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8PKM
 | | Befiradol-bound serotonin 5-HT1A receptor - Gi Protein Complex | | Descriptor: | (2R)-1-(heptadecanoyloxy)-3-{[(R)-hydroxy{[(1R,2R,3R,4R,5S,6R)-2,3,5,6-tetrahydroxy-4-(phosphonooxy)cyclohexyl]oxy}phosphoryl]oxy}propan-2-yl (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate, (3-chloranyl-4-fluoranyl-phenyl)-[4-fluoranyl-4-[[(5-methylpyridin-2-yl)methylamino]methyl]piperidin-1-yl]methanone, 5-hydroxytryptamine receptor 1A, ... | | Authors: | Schneider, J, Gmeiner, P, Hove, T.T, Rasmussen, T, Boettcher, B. | | Deposit date: | 2023-06-27 | | Release date: | 2024-05-29 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Discovery of a functionally selective serotonin 1A receptor agonist
for the treatment of pain
To Be Published
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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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7JVP
 | | Cryo-EM structure of SKF-83959-bound dopamine receptor 1 in complex with Gs protein | | Descriptor: | (1R)-6-chloro-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol, CHOLESTEROL, D(1A) dopamine receptor, ... | | Authors: | Zhuang, Y, Xu, P, Mao, C, Wang, L, Krumm, B, Zhou, X.E, Huang, S, Liu, H, Cheng, X, Huang, X.-P, Sheng, D.-D, Xu, T, Liu, Y.-F, Wang, Y, Guo, J, Jiang, Y, Jiang, H, Melcher, K, Roth, B.L, Zhang, Y, Zhang, C, Xu, H.E. | | Deposit date: | 2020-08-22 | | Release date: | 2021-02-24 | | Last modified: | 2021-03-03 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural insights into the human D1 and D2 dopamine receptor signaling complexes.
Cell, 184, 2021
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7S8N
 | | CryoEM structure of Gq-coupled MRGPRX2 with small molecule agonist (R)-Zinc-3573 | | Descriptor: | (3R)-N,N-dimethyl-1-[(8S)-5-phenylpyrazolo[1,5-a]pyrimidin-7-yl]pyrrolidin-3-amine, Gs-mini-Gq chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 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 (2.9 Å) | | Cite: | Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
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8TLM
 | | Structure of a class A GPCR/Fab complex | | Descriptor: | C-C chemokine receptor type 8, Green fluorescent protein fusion, Fab heavy chain, ... | | Authors: | Sun, D, Johnson, M, Masureel, M. | | Deposit date: | 2023-07-27 | | Release date: | 2023-12-20 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural basis of antibody inhibition and chemokine activation of the human CC chemokine receptor 8.
Nat Commun, 14, 2023
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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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8GG0
 | | CryoEM structure of beta-2-adrenergic receptor in complex with GTP-bound Gs heterotrimer (transition intermediate #6 of 20) | | Descriptor: | (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol, Beta-2 adrenergic receptor, GUANOSINE-5'-TRIPHOSPHATE, ... | | Authors: | Papasergi-Scott, M.M, Skiniotis, G. | | Deposit date: | 2023-03-08 | | Release date: | 2024-03-06 | | Last modified: | 2024-06-12 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 629, 2024
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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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7RYC
 | | Oxytocin receptor (OTR) bound to oxytocin in complex with a heterotrimeric Gq protein | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(i) subunit alpha-2,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Meyerowitz, J.G, Robertson, M.J, Skiniotis, G. | | Deposit date: | 2021-08-24 | | Release date: | 2022-03-09 | | Last modified: | 2022-03-30 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | The oxytocin signaling complex reveals a molecular switch for cation dependence.
Nat.Struct.Mol.Biol., 29, 2022
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7Y64
 | | Cryo-EM structure of C5a-bound C5aR1 in complex with Gi protein | | Descriptor: | C5a anaphylatoxin, C5a anaphylatoxin chemotactic receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Feng, Y.Y, Zhao, C, Yan, W, Shao, Z.H. | | Deposit date: | 2022-06-18 | | Release date: | 2023-03-01 | | Last modified: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Mechanism of activation and biased signaling in complement receptor C5aR1.
Cell Res., 33, 2023
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7Y66
 | | Cryo-EM structure of BM213-bound C5aR1 in complex with Gi protein | | Descriptor: | BM213 peptide, C5a anaphylatoxin chemotactic receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Feng, Y.Y, Zhao, C, Yan, W, Shao, Z.H. | | Deposit date: | 2022-06-18 | | Release date: | 2023-03-01 | | Last modified: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Mechanism of activation and biased signaling in complement receptor C5aR1.
Cell Res., 33, 2023
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4BEY
 | | Night blindness causing G90D rhodopsin in complex with GaCT2 peptide | | Descriptor: | ACETATE ION, Guanine nucleotide-binding protein G(t) subunit alpha-1, PALMITIC ACID, ... | | Authors: | Singhal, A, Ostermaier, M.K, Vishnivetskiy, S.A, Panneels, V, Homan, K.T, Tesmer, J.J.G, Veprintsev, D, Deupi, X, Gurevich, V.V, Schertler, G.F.X, Standfuss, J. | | Deposit date: | 2013-03-12 | | Release date: | 2013-05-08 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Insights Into Congenital Stationary Night Blindness Based on the Structure of G90D Rhodopsin.
Embo Rep., 14, 2013
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7SBF
 | | PZM21 bound Mu Opioid Receptor-Gi 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(i) subunit alpha-1, ... | | Authors: | Huang, W, Qu, Q, Wang, H, Skiniotis, G, Kobilka, B. | | Deposit date: | 2021-09-24 | | Release date: | 2022-04-20 | | Last modified: | 2022-07-06 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structure-Based Evolution of G Protein-Biased mu-Opioid Receptor Agonists.
Angew.Chem.Int.Ed.Engl., 61, 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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