8THK
 
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7PWD
 | | Structure of an inhibited GRK2-G-beta and G-gamma complex | | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | | Deposit date: | 2021-10-06 | | Release date: | 2021-10-20 | | Last modified: | 2022-05-18 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Monatsh Chem, 2022
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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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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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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 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Cryo-EM structure of Lys05 bound GPR30-Gq complex structure
To Be Published
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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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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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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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5UKK
 | | Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak) | | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(pyridin-2-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | | Deposit date: | 2017-01-23 | | Release date: | 2017-04-05 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
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7TYN
 | | Calcitonin Receptor in complex with Gs and salmon calcitonin peptide | | Descriptor: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-13 | | Release date: | 2022-03-30 | | Last modified: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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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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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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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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7V9L
 | | Cryo-EM structure of the SV1-Gs complex. | | Descriptor: | GHRH receptor splice variant 1,GHRH receptor splice variant 1,GHRH receptor splice variant 1,SV1, 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: | Cong, Z.T, Zhou, F.L, Zhang, C, Zou, X.Y, Zhang, H.B, Wang, Y.Z, Zhou, Q.T, Cai, X.Q, Liu, Q.F, Li, J, Shao, L.J, Mao, C.Y, Wang, X, Wu, J.H, Xia, T, Zhao, L.H, Jiang, H.L, Zhang, Y, Xu, H.E, Cheng, X, Yang, D.H, Wang, M.W. | | Deposit date: | 2021-08-26 | | Release date: | 2022-04-06 | | Last modified: | 2022-05-04 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Constitutive signal bias mediated by the human GHRHR splice variant 1.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7CZ5
 | | Cryo-EM structure of the human growth hormone-releasing hormone receptor-Gs protein complex | | Descriptor: | CHOLESTEROL, Growth hormone-releasing hormone receptor,growth hormone-releasing hormone receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Zhou, F, Zhang, H, Cong, Z, Zhao, L, Zhou, Q, Mao, C, Cheng, X, Shen, D, Cai, X, Ma, C, Wang, Y, Dai, A, Zhou, Y, Sun, W, Zhao, F, Zhao, S, Jiang, H, Jiang, Y, Yang, D, Xu, H.E, Zhang, Y, Wang, M. | | Deposit date: | 2020-09-07 | | Release date: | 2020-11-18 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structural basis for activation of the growth hormone-releasing hormone receptor.
Nat Commun, 11, 2020
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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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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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7DW9
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7K7Z
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8DZR
 | | GR89,696 bound Kappa Opioid Receptor in complex with gustducin | | Descriptor: | G alpha gustducin protein, 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: | Fay, J.F, Che, T. | | Deposit date: | 2022-08-08 | | Release date: | 2023-05-03 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (2.61 Å) | | Cite: | Ligand and G-protein selectivity in the kappa-opioid receptor.
Nature, 617, 2023
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7X8R
 | | Cryo-EM structure of the Boc5-bound hGLP-1R-Gs complex | | Descriptor: | 2,4-bis(3-methoxy-4-thiophen-2-ylcarbonyloxy-phenyl)-1,3-bis[[4-[(2-methylpropan-2-yl)oxycarbonylamino]phenyl]carbonylamino]cyclobutane-1,3-dicarboxylic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cong, Z.T, Zhou, Q.T, Li, Y, Chen, L.N, Zhang, Z.C, Liang, A.Y, Liu, Q, Wu, X.Y, Dai, A.T, Xia, T, Wu, W, Zhang, Y, Yang, D.H, Wang, M.W. | | Deposit date: | 2022-03-14 | | Release date: | 2022-06-29 | | Method: | ELECTRON MICROSCOPY (2.61 Å) | | Cite: | Structural basis of peptidomimetic agonism revealed by small- molecule GLP-1R agonists Boc5 and WB4-24.
Proc.Natl.Acad.Sci.USA, 119, 2022
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8HA0
 | | Molecular recognition of two endogenous hormones by the human parathyroid hormone receptor-1 | | 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: | Zhao, L, Xu, H.E, Yuan, Q. | | Deposit date: | 2022-10-26 | | Release date: | 2022-12-21 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (2.62 Å) | | Cite: | Molecular recognition of two endogenous hormones by the human parathyroid hormone receptor-1.
Acta Pharmacol.Sin., 44, 2023
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8XJK
 | | Cloprosetnol bound Prostaglandin F2-alpha receptor-Gq Protein Complex | | Descriptor: | (~{Z})-7-[(1~{R},2~{R},3~{R},5~{S})-2-[(~{E},3~{R})-4-(3-chloranylphenoxy)-3-oxidanyl-but-1-enyl]-3,5-bis(oxidanyl)cyclopentyl]hept-5-enoic acid, Antibody fragment scFv16, Engineered miniGq, ... | | Authors: | Zhang, X, Li, X, Liu, G, Gong, W. | | Deposit date: | 2023-12-21 | | Release date: | 2024-02-28 | | Last modified: | 2024-03-20 | | Method: | ELECTRON MICROSCOPY (2.63 Å) | | Cite: | Structural basis for ligand recognition and activation of the prostanoid receptors.
Cell Rep, 43, 2024
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8G59
 | | Cryo-EM structure of the TUG891 bound GPR120-Giq complex | | Descriptor: | 3-{4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]phenyl}propanoic acid, Free fatty acid receptor 4, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Mao, C, Xiao, P, Tao, X, Qin, J, He, Q, Zhang, C, Yu, X, Zhang, Y, Sun, J. | | Deposit date: | 2023-02-12 | | Release date: | 2023-03-08 | | Last modified: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (2.64 Å) | | Cite: | Unsaturated bond recognition leads to biased signal in a fatty acid receptor.
Science, 380, 2023
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8DZS
 | | GR89,696 bound Kappa Opioid Receptor in complex with Gz | | 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(z) subunit alpha, ... | | Authors: | Fay, J.F, Che, T. | | Deposit date: | 2022-08-08 | | Release date: | 2023-05-03 | | Last modified: | 2023-05-24 | | Method: | ELECTRON MICROSCOPY (2.65 Å) | | Cite: | Ligand and G-protein selectivity in the kappa-opioid receptor.
Nature, 617, 2023
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