8DZP
 
 | | momSalB bound Kappa Opioid Receptor in complex with Gi1 | | 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: | Fay, J.F, Che, T. | | Deposit date: | 2022-08-08 | | Release date: | 2023-05-03 | | Last modified: | 2023-05-24 | | Method: | ELECTRON MICROSCOPY (2.71 Å) | | Cite: | Ligand and G-protein selectivity in the kappa-opioid receptor.
Nature, 617, 2023
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8WG8
 | | Cryo-EM structures of peptide free and Gs-coupled GCGR | | Descriptor: | Glucagon 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: | Cong, Z.T, Zhao, F.H, Li, Y, Luo, G, Zhou, Q.T, Yang, D.H, Wang, M.W. | | Deposit date: | 2023-09-20 | | Release date: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (2.71 Å) | | Cite: | Molecular features of the ligand-free GLP-1R, GCGR and GIPR in complex with G s proteins.
Cell Discov, 10, 2024
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8DWG
 | | CryoEM structure of Gq-coupled MRGPRX1 with peptide ligand BAM8-22 and positive allosteric modulator ML382 | | Descriptor: | 2-[(cyclopropanesulfonyl)amino]-N-(2-ethoxyphenyl)benzamide, Gs-mini-Gq chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, Y, Cao, C, Fay, J.F, Roth, B.L. | | Deposit date: | 2022-08-01 | | Release date: | 2022-11-02 | | Last modified: | 2023-04-12 | | Method: | ELECTRON MICROSCOPY (2.71 Å) | | Cite: | Ligand recognition and allosteric modulation of the human MRGPRX1 receptor.
Nat.Chem.Biol., 19, 2023
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8U4N
 | | Structure of Apo CXCR4/Gi complex | | Descriptor: | C-X-C chemokine receptor type 4, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Saotome, K, McGoldrick, L.L, Franklin, M.C. | | Deposit date: | 2023-09-11 | | Release date: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (2.72 Å) | | Cite: | Structural insights into CXCR4 modulation and oligomerization
Biorxiv, 2024
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8INR
 | | Cryo-EM structure of the alpha-MSH-bound human melanocortin receptor 5 (MC5R)-Gs complex | | Descriptor: | CALCIUM ION, 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,HiBiT, ... | | Authors: | Feng, W.B, Zhou, Q.T, Chen, X.Y, Dai, A.T, Cai, X.Q, Liu, X, Zhao, F.H, Chen, Y, Ye, C.Y, Xu, Y.N, Cong, Z.T, Li, H, Lin, S, Yang, D.H, Wang, M.W. | | Deposit date: | 2023-03-10 | | Release date: | 2023-09-20 | | Method: | ELECTRON MICROSCOPY (2.73 Å) | | Cite: | Structural insights into ligand recognition and subtype selectivity of the human melanocortin-3 and melanocortin-5 receptors.
Cell Discov, 9, 2023
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7UM5
 | | CryoEM structure of Go-coupled 5-HT5AR in complex with 5-CT | | Descriptor: | 3-(2-azanylethyl)-1H-indole-5-carboxamide, 5-hydroxytryptamine receptor 5A, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Zhang, S, Fay, J.F, Roth, B.L. | | Deposit date: | 2022-04-06 | | Release date: | 2022-07-20 | | Last modified: | 2022-07-27 | | Method: | ELECTRON MICROSCOPY (2.73 Å) | | Cite: | Inactive and active state structures template selective tools for the human 5-HT 5A receptor.
Nat.Struct.Mol.Biol., 29, 2022
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5HE3
 | | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | | Descriptor: | (4~{S})-4-[3-[2-(2,6-dimethylphenyl)ethylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Tesmer, J.J.G. | | Deposit date: | 2016-01-05 | | Release date: | 2016-05-11 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.74 Å) | | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J.Med.Chem., 59, 2016
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8SMV
 | | GPR161 Gs heterotrimer | | Descriptor: | CHOLESTEROL, G-protein coupled receptor 161, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hoppe, N, Manglik, A, Harrison, S. | | Deposit date: | 2023-04-26 | | Release date: | 2024-02-21 | | Last modified: | 2024-03-20 | | Method: | ELECTRON MICROSCOPY (2.74 Å) | | Cite: | GPR161 structure uncovers the redundant role of sterol-regulated ciliary cAMP signaling in the Hedgehog pathway.
Biorxiv, 2023
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6C2Y
 | | Human GRK2 in complex with Gbetagamma subunits and CCG257142 | | Descriptor: | (4R,5R,6S)-4-[4-fluoro-3-({[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl]methyl}carbamoyl)phenyl]-N-(2H-indazol-5-yl)-6-methyl-2-oxohexahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Bouley, R, Tesmer, J.J.G. | | Deposit date: | 2018-01-09 | | Release date: | 2018-04-25 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.74 Å) | | Cite: | Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.
Bioorg. Med. Chem. Lett., 28, 2018
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7VQX
 | | Cryo-EM structure of human vasoactive intestinal polypeptide receptor 2 (VIP2R) in complex with PACAP27 and Gs | | 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(s) subunit alpha isoforms short, ... | | Authors: | Xu, Y.N, Feng, W.B, Zhou, Q.T, Liang, A.Y, Li, J, Dai, A.T, Zhao, F.H, Yan, J.H, Chen, C.W, Li, H, Zhao, L.H, Xia, T, Jiang, Y, Xu, H.E, Yang, D.H, Wang, M.W. | | Deposit date: | 2021-10-21 | | Release date: | 2022-05-18 | | Method: | ELECTRON MICROSCOPY (2.74 Å) | | Cite: | A distinctive ligand recognition mechanism by the human vasoactive intestinal polypeptide receptor 2.
Nat Commun, 13, 2022
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3CIK
 | | Human GRK2 in Complex with Gbetagamma subunits | | Descriptor: | Beta-adrenergic receptor kinase 1, 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: | Tesmer, J.J.G, Lodowski, D.T. | | Deposit date: | 2008-03-11 | | Release date: | 2009-02-17 | | Last modified: | 2012-03-07 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
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7UM7
 | | CryoEM structure of Go-coupled 5-HT5AR in complex with Methylergometrine | | Descriptor: | (8beta)-N-[(2S)-1-hydroxybutan-2-yl]-6-methyl-9,10-didehydroergoline-8-carboxamide, 5-hydroxytryptamine receptor 5A, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Zhang, S, Fay, J.F, Roth, B.L. | | Deposit date: | 2022-04-06 | | Release date: | 2022-07-20 | | Last modified: | 2022-07-27 | | Method: | ELECTRON MICROSCOPY (2.75 Å) | | Cite: | Inactive and active state structures template selective tools for the human 5-HT 5A receptor.
Nat.Struct.Mol.Biol., 29, 2022
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7YK7
 | | Cryo-EM structure of the DC591053-bound human relaxin family peptide receptor 4 (RXFP4)-Gi 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-2, ... | | Authors: | Chen, Y, Zhou, Q.T, Wang, J, Xu, Y.W, Wang, Y, Yan, J.H, Wang, Y.B, Zhu, Q, Zhao, F.H, Li, C.H, Chen, C.W, Cai, X.Q, Bathgate, R.A.D, Shen, C, Xu, H.E, Yang, D.H, Liu, H, Wang, M.W. | | Deposit date: | 2022-07-21 | | Release date: | 2023-03-01 | | Method: | ELECTRON MICROSCOPY (2.75 Å) | | Cite: | Ligand recognition mechanism of the human relaxin family peptide receptor 4 (RXFP4).
Nat Commun, 14, 2023
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8FLU
 | | Human PTH1R in complex with LA-PTH and Gs | | 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(s) subunit alpha isoforms short, ... | | Authors: | Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M. | | Deposit date: | 2022-12-22 | | Release date: | 2023-04-26 | | Last modified: | 2023-06-14 | | Method: | ELECTRON MICROSCOPY (2.76 Å) | | Cite: | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8J6R
 | | Cryo-EM structure of the MK-6892-bound human HCAR2-Gi1 complex | | Descriptor: | 2-[[2,2-dimethyl-3-[3-(5-oxidanylpyridin-2-yl)-1,2,4-oxadiazol-5-yl]propanoyl]amino]cyclohexene-1-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 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 (2.76 Å) | | Cite: | Orthosteric and allosteric modulation of human HCAR2 signaling complex.
Nat Commun, 14, 2023
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8JIU
 | | Cryo-EM structure of the GLP-1R/GCGR dual agonist SAR425899-bound human GCGR-Gs complex | | Descriptor: | Glucagon 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: | Yang, L, Zhou, Q.T, Dai, A.T, Zhao, F.H, Chang, R.L, Ying, T.L, Wu, B.L, Yang, D.H, Wang, M.W, Cong, Z.T. | | Deposit date: | 2023-05-27 | | Release date: | 2023-09-13 | | Method: | ELECTRON MICROSCOPY (2.76 Å) | | Cite: | Structural analysis of the dual agonism at GLP-1R and GCGR.
Proc.Natl.Acad.Sci.USA, 120, 2023
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7XV3
 | | Cryo-EM structure of LPS-bound GPR174 in complex with Gs protein | | Descriptor: | (2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid, Engineered G protein subunit S (mini-Gs), Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | He, Y, Liang, J. | | Deposit date: | 2022-05-20 | | Release date: | 2023-02-15 | | Last modified: | 2023-03-08 | | Method: | ELECTRON MICROSCOPY (2.76 Å) | | Cite: | Structural basis of lysophosphatidylserine receptor GPR174 ligand recognition and activation.
Nat Commun, 14, 2023
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7VV5
 | | Cryo-EM structure of pseudoallergen receptor MRGPRX2 complex with C48/80, state1 | | 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: | 2021-11-04 | | Release date: | 2021-12-01 | | Last modified: | 2022-07-20 | | Method: | ELECTRON MICROSCOPY (2.76 Å) | | Cite: | Structure, function and pharmacology of human itch receptor complexes.
Nature, 600, 2021
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8I7V
 | | Cryo-EM structure of Acipimox bound human hydroxy-carboxylic acid receptor 2 in complex with Gi heterotrimer | | Descriptor: | 5-methyl-4-oxidanyl-pyrazin-4-ium-2-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: | Park, J.H, Ishimoto, N, Park, S.Y. | | Deposit date: | 2023-02-02 | | Release date: | 2024-02-07 | | Method: | ELECTRON MICROSCOPY (2.77 Å) | | Cite: | Structural basis for ligand recognition and signaling of hydroxy-carboxylic acid receptor 2.
Nat Commun, 14, 2023
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8XJL
 | | PGF2-alpha bound Prostaglandin F2-alpha receptor-Gq Protein Complex | | Descriptor: | (Z)-7-[(1R,2R,3R,5S)-3,5-bis(oxidanyl)-2-[(E,3S)-3-oxidanyloct-1-enyl]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 (2.77 Å) | | Cite: | Structural basis for ligand recognition and activation of the prostanoid receptors.
Cell Rep, 43, 2024
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7Y3G
 | | Cryo-EM structure of a class A orphan GPCR | | Descriptor: | G-protein coupled receptor 12, 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: | Liu, Z.J, Hua, T, Li, H, Zhang, J.Y, Luo, F. | | Deposit date: | 2022-06-10 | | Release date: | 2023-06-07 | | Method: | ELECTRON MICROSCOPY (2.77 Å) | | Cite: | Structural insight into the constitutive activity of human orphan receptor GPR12.
Sci Bull (Beijing), 68, 2023
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8HMP
 | | GPR52 with Gs and c17 | | Descriptor: | G-protein coupled receptor 52, 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: | Chen, B, Xu, F. | | Deposit date: | 2022-12-05 | | Release date: | 2023-06-21 | | Method: | ELECTRON MICROSCOPY (2.77 Å) | | Cite: | Allosteric coupling between G-protein binding and extracellular ligand binding sites in GPR52 revealed by 19 F-NMR and cryo-electron microscopy.
MedComm (2020), 4, 2023
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8IUL
 | | Cryo-EM structure of the latanoprost-bound human PTGFR-Gq complex | | Descriptor: | Antibody fragment scFv16, G subunit alpha (q), Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Wu, C, Xu, Y, Xu, H.E. | | Deposit date: | 2023-03-24 | | Release date: | 2023-07-12 | | Last modified: | 2023-08-30 | | Method: | ELECTRON MICROSCOPY (2.78 Å) | | Cite: | Ligand-induced activation and G protein coupling of prostaglandin F 2 alpha receptor.
Nat Commun, 14, 2023
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7XW6
 | | TSHR-Gs-M22 antibody-ML109 complex | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Duan, J, Xu, P, Luan, X, Ji, Y, Yuan, Q, He, X, Ye, J, Cheng, X, Jiang, H, Zhang, S, Jiang, Y, Xu, H.E. | | Deposit date: | 2022-05-26 | | Release date: | 2022-08-17 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (2.78 Å) | | Cite: | Hormone- and antibody-mediated activation of the thyrotropin receptor.
Nature, 609, 2022
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5HE2
 | | Bovine GRK2 in complex with Gbetagamma subunits and CCG224406 | | Descriptor: | (4~{S})-4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | | Deposit date: | 2016-01-05 | | Release date: | 2016-05-11 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.79 Å) | | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J.Med.Chem., 59, 2016
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