5XPR
 
 | | Human endothelin receptor type-B in complex with antagonist bosentan | | Descriptor: | 4-tert-butyl-N-[6-(2-hydroxyethyloxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]benzenesulfonamide, Endothelin B receptor,Endolysin,Endothelin B receptor, SULFATE ION | | Authors: | Shihoya, W, Nishizawa, T, Yamashita, K, Hirata, K, Okuta, A, Tani, K, Fujiyoshi, Y, Doi, T, Nureki, O. | | Deposit date: | 2017-06-04 | | Release date: | 2017-08-16 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (3.6 Å) | | Cite: | X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog
Nat. Struct. Mol. Biol., 24, 2017
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6OIK
 | | Muscarinic acetylcholine receptor 2-Go complex | | Descriptor: | 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Antibody fragment, ... | | Authors: | Maeda, S, Qianhui, Q, Skiniotis, G, Kobilka, B. | | Deposit date: | 2019-04-09 | | Release date: | 2019-05-08 | | Last modified: | 2020-01-08 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes.
Science, 364, 2019
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8HNN
 | | Structure of CXCR3 complexed with antagonist SCH546738 | | Descriptor: | 3-azanyl-6-chloranyl-5-[(3S)-4-[1-[(4-chlorophenyl)methyl]piperidin-4-yl]-3-ethyl-piperazin-1-yl]pyrazine-2-carboxamide, CHOLESTEROL, Nb6, ... | | 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 (3.6 Å) | | Cite: | Structural insights into the activation and inhibition of CXC chemokine receptor 3.
Nat.Struct.Mol.Biol., 31, 2024
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6D9H
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist | | Descriptor: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Draper-Joyce, C.J, Khoshouei, M, Thal, D.M, Liang, Y.-L, Nguyen, A.T.N, Furness, S.G.B, Venugopal, H, Baltos, J, Plitzko, J.M, Danev, R, Baumeister, W, May, L.T, Wootten, D, Sexton, P, Glukhova, A, Christopoulos, A. | | Deposit date: | 2018-04-29 | | Release date: | 2018-06-20 | | Last modified: | 2018-07-11 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Structure of the adenosine-bound human adenosine A1receptor-Gicomplex.
Nature, 558, 2018
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7V6A
 | | Cry-EM structure of M4-c110-G 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: | Wang, J.J, Wu, M, Wu, L.J, Hua, T, Liu, Z.J, Wang, T. | | Deposit date: | 2021-08-20 | | Release date: | 2022-05-11 | | Last modified: | 2022-11-23 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands.
Nat Commun, 13, 2022
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7EJA
 | | Structure of the alpha2A-adrenergic receptor GoA signaling complex bound to dexmedetomidine | | Descriptor: | 4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole, Alpha-2A adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Xu, J, Cao, S, Liu, Z, Du, Y. | | Deposit date: | 2021-04-01 | | Release date: | 2022-04-13 | | Last modified: | 2023-11-29 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Structural insights into ligand recognition, activation, and signaling of the alpha 2A adrenergic receptor.
Sci Adv, 8, 2022
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8UNX
 | | CryoEM structure of beta-2-adrenergic receptor in complex with GTP-bound Gs heterotrimer (Class M) | | 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: | 2023-10-19 | | Release date: | 2024-03-06 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 629, 2024
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8UO2
 | | CryoEM structure of beta-2-adrenergic receptor in complex with GTP-bound Gs heterotrimer (Class R) | | 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: | 2023-10-19 | | Release date: | 2024-03-06 | | Last modified: | 2024-06-12 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 629, 2024
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8UNY
 | | CryoEM structure of beta-2-adrenergic receptor in complex with GTP-bound Gs heterotrimer (Class N) | | 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: | 2023-10-19 | | Release date: | 2024-03-06 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 629, 2024
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8UO1
 | | CryoEM structure of beta-2-adrenergic receptor in complex with GTP-bound Gs heterotrimer (Class Q) | | 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: | 2023-10-19 | | Release date: | 2024-03-06 | | Last modified: | 2024-06-12 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 629, 2024
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5NDZ
 | | Crystal structure of a thermostabilised human protease-activated receptor-2 (PAR2) in complex with AZ3451 at 3.6 angstrom resolution | | Descriptor: | 2-(6-bromanyl-1,3-benzodioxol-5-yl)-~{N}-(4-cyanophenyl)-1-[(1~{S})-1-cyclohexylethyl]benzimidazole-5-carboxamide, Lysozyme,Proteinase-activated receptor 2,Soluble cytochrome b562,Proteinase-activated receptor 2, SODIUM ION | | Authors: | Cheng, R.K.Y, Fiez-Vandal, C, Schlenker, O, Edman, K, Aggeler, B, Brown, D.G, Brown, G, Cooke, R.M, Dumelin, C.E, Dore, A.S, Geschwindner, S, Grebner, C, Hermansson, N.-O, Jazayeri, A, Johansson, P, Leong, L, Prihandoko, R, Rappas, M, Soutter, H, Snijder, A, Sundstrom, L, Tehan, B, Thornton, P, Troast, D, Wiggin, G, Zhukov, A, Marshall, F.H, Dekker, N. | | Deposit date: | 2017-03-09 | | Release date: | 2017-05-03 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (3.6 Å) | | Cite: | Structural insight into allosteric modulation of protease-activated receptor 2.
Nature, 545, 2017
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8DPG
 | | Cryo-EM structure of the 5HT2C receptor (INI isoform) bound to psilocin | | Descriptor: | 3-[2-(dimethylamino)ethyl]-1~{H}-indol-4-ol, 5-hydroxytryptamine receptor 2C, Antibody fragment scFv16, ... | | Authors: | Gumpper, R.H, Fay, J.F, Roth, B.L. | | Deposit date: | 2022-07-15 | | Release date: | 2022-08-24 | | Last modified: | 2022-08-31 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Molecular insights into the regulation of constitutive activity by RNA editing of 5HT 2C serotonin receptors.
Cell Rep, 40, 2022
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7RKN
 | | Structure of CX3CL1-US28-Gi-scFv16 in OC-state | | Descriptor: | Antibody fragment scFv16, Fractalkine, G-protein coupled receptor homolog US28, ... | | Authors: | Tsutsumi, N, Qu, Q, Jude, K.M, Skiniotis, G, Garcia, K.C. | | Deposit date: | 2021-07-22 | | Release date: | 2022-01-26 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Atypical structural snapshots of human cytomegalovirus GPCR interactions with host G proteins
Sci Adv, 8, 2022
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2YCZ
 | | TURKEY BETA1 ADRENERGIC RECEPTOR WITH STABILISING MUTATIONS AND BOUND ANTAGONIST IODOCYANOPINDOLOL | | Descriptor: | 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3-iodo-1H-indole-2-carbonitrile, BETA-1 ADRENERGIC RECEPTOR, octyl 1-thio-beta-D-glucopyranoside | | Authors: | Moukhametzianov, R, Warne, T, Edwards, P.C, Serrano-Vega, M.J, Leslie, A.G.W, Tate, C.G, Schertler, G.F.X. | | Deposit date: | 2011-03-17 | | Release date: | 2011-06-01 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (3.65 Å) | | Cite: | Two Distinct Conformations of Helix 6 Observed in Antagonist-Bound Structures of a {Beta}1- Adrenergic Receptor.
Proc.Natl.Acad.Sci.USA, 108, 2011
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8JSP
 | | Ulotaront(SEP-363856)-bound Serotonin 1A (5-HT1A) receptor-Gi complex | | Descriptor: | 1-[(7~{S})-5,7-dihydro-4~{H}-thieno[2,3-c]pyran-7-yl]-~{N}-methyl-methanamine, 5-hydroxytryptamine receptor 1A, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Xu, Z, Guo, L.L, Zhao, C, Shen, S.Y, Sun, J.P, Shao, Z.H. | | Deposit date: | 2023-06-20 | | Release date: | 2023-11-15 | | Last modified: | 2024-01-03 | | Method: | ELECTRON MICROSCOPY (3.65 Å) | | Cite: | Ligand recognition and G-protein coupling of trace amine receptor TAAR1.
Nature, 624, 2023
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5X33
 | | Leukotriene B4 receptor BLT1 in complex with BIIL260 | | Descriptor: | 4-[[3-[[4-[2-(4-hydroxyphenyl)propan-2-yl]phenoxy]methyl]phenyl]methoxy]benzenecarboximidamide, LTB4 receptor,Lysozyme,LTB4 receptor | | Authors: | Hori, T, Hirata, K, Yamashita, K, Kawano, Y, Yamamoto, M, Yokoyama, S. | | Deposit date: | 2017-02-03 | | Release date: | 2018-01-03 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Na+-mimicking ligands stabilize the inactive state of leukotriene B4receptor BLT1.
Nat. Chem. Biol., 14, 2018
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8GEE
 | | CryoEM structure of beta-2-adrenergic receptor in complex with nucleotide-free Gs heterotrimer (#15 of 20) | | Descriptor: | (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol, Beta-2 adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Papasergi-Scott, M.M, Skiniotis, G. | | Deposit date: | 2023-03-06 | | Release date: | 2024-03-06 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 629, 2024
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4U16
 | | M3-mT4L receptor bound to NMS | | Descriptor: | D(-)-TARTARIC ACID, Muscarinic acetylcholine receptor M3,Lysozyme,Muscarinic acetylcholine receptor M3, N-methyl scopolamine | | Authors: | Thorsen, T.S, Matt, R, Weis, W.I, Kobilka, B. | | Deposit date: | 2014-07-15 | | Release date: | 2014-11-26 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Modified T4 Lysozyme Fusion Proteins Facilitate G Protein-Coupled Receptor Crystallogenesis.
Structure, 22, 2014
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6E67
 | | Structure of beta2 adrenergic receptor fused to a Gs peptide | | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Beta-2 adrenergic receptor,Endolysin,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short,Beta-2 adrenergic receptor chimera | | Authors: | Liu, X, Xu, X, Hilger, D, Tiemann, J, Liu, H, Du, Y, Hirata, K, Sun, X, Guixa-Gonzalez, R, Mathiesen, J, Hildebrand, P, Kobilka, B. | | Deposit date: | 2018-07-24 | | Release date: | 2019-06-05 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Structural Insights into the Process of GPCR-G Protein Complex Formation.
Cell, 177, 2019
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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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2ZIY
 | | Crystal structure of squid rhodopsin | | Descriptor: | PALMITIC ACID, RETINAL, Rhodopsin | | Authors: | Miyano, M, Shimamura, T. | | Deposit date: | 2008-02-27 | | Release date: | 2008-05-06 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Crystal structure of squid rhodopsin with intracellularly extended cytoplasmic region
J.Biol.Chem., 283, 2008
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8FCZ
 | | Crystal structure of ground-state rhodopsin in complex with a nanobody | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-3)-[alpha-D-mannopyranose-(1-6)]beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Nanobody Nb2, ... | | Authors: | Salom, D, Palczewski, K, Kiser, P.D. | | Deposit date: | 2022-12-01 | | Release date: | 2023-08-30 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Structural basis for the allosteric modulation of rhodopsin by nanobody binding to its extracellular domain.
Nat Commun, 14, 2023
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4MQT
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo and allosteric modulator LY2119620 | | Descriptor: | 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, ... | | Authors: | Kruse, A.C, Ring, A.M, Manglik, A, Hu, J, Hu, K, Eitel, K, Huebner, H, Pardon, E, Valant, C, Sexton, P.M, Christopoulos, A, Felder, C.C, Gmeiner, P, Steyaert, J, Weis, W.I, Garcia, K.C, Wess, J, Kobilka, B.K. | | Deposit date: | 2013-09-16 | | Release date: | 2013-11-27 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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8FD0
 | | Crystal structure of bovine rod opsin in complex with a nanobody | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-2)-alpha-D-mannopyranose-(1-3)-[alpha-D-mannopyranose-(1-6)]beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Nanobody Nb2, ... | | Authors: | Salom, D, Palczewski, K, Kiser, P.D. | | Deposit date: | 2022-12-01 | | Release date: | 2023-08-30 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.71 Å) | | Cite: | Structural basis for the allosteric modulation of rhodopsin by nanobody binding to its extracellular domain.
Nat Commun, 14, 2023
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7W0M
 | | Cryo-EM structure of a monomeric GPCR-Gi complex with small molecule | | Descriptor: | (1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide, 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, F, Yue, Y, Liu, L.E, Wu, L.J, Hanson, M. | | Deposit date: | 2021-11-18 | | Release date: | 2022-07-27 | | Method: | ELECTRON MICROSCOPY (3.71 Å) | | Cite: | Structural insight into apelin receptor-G protein stoichiometry.
Nat.Struct.Mol.Biol., 29, 2022
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