8JR9
 
 | | Small molecule agonist (PCO371) bound to human parathyroid hormone receptor type 1 (PTH1R) | | 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-1, ... | | Authors: | Zhao, L, He, Q, Yuan, Q, Gu, Y, He, X, Shan, H, Li, J, Wang, K, Li, Y, Hu, W, Wu, K, Shen, J, Xu, H.E. | | Deposit date: | 2023-06-16 | | Release date: | 2023-08-02 | | Last modified: | 2023-10-04 | | Method: | ELECTRON MICROSCOPY (2.57 Å) | | Cite: | Conserved class B GPCR activation by a biased intracellular agonist.
Nature, 621, 2023
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7S8O
 | | CryoEM structure of Gi-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, 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 (2.58 Å) | | Cite: | Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
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8FMZ
 | | Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator | | 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, MiniGq, ... | | Authors: | Krumm, B.E, Diberto, J.F, Olsen, R.H.J, Kang, H, Slocum, S.T, Zhang, S, Strachan, R.T, Fay, J.F, Roth, B.L. | | Deposit date: | 2022-12-26 | | Release date: | 2023-03-29 | | Last modified: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (2.59 Å) | | Cite: | Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator.
Biochemistry, 62, 2023
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9BKJ
 | | Cholecystokinin 1 receptor (CCK1R) Y140A mutant, Gq chimera (mGsqi) complex | | Descriptor: | AMINO GROUP, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | Authors: | Cary, B.P, Harikumar, K.G, Zhao, P, Desai, A.J, Mobbs, J.M, Toufaily, C, Furness, S.G.B, Christopoulos, A, Belousoff, M.J, Wootten, D, Sexton, P.M, Miller, L.J. | | Deposit date: | 2024-04-29 | | Release date: | 2024-05-22 | | Method: | ELECTRON MICROSCOPY (2.59 Å) | | Cite: | Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling
To Be Published
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8THK
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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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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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8W88
 | | Cryo-EM structure of the SEP363856-bound TAAR1-Gs complex | | Descriptor: | 1-[(7~{S})-5,7-dihydro-4~{H}-thieno[2,3-c]pyran-7-yl]-~{N}-methyl-methanamine, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, H, Zheng, Y, Wang, Y, Wang, Y, He, X, Xu, P, Huang, S, Yuan, Q, Zhang, X, Wang, S, Xu, H.E, Xu, F. | | Deposit date: | 2023-09-01 | | Release date: | 2023-11-22 | | Last modified: | 2024-01-03 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Recognition of methamphetamine and other amines by trace amine receptor TAAR1.
Nature, 624, 2023
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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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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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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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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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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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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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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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8FYX
 | | Buspirone-bound serotonin 1A (5-HT1A) receptor-Gi1 protein complex | | Descriptor: | Buspirone, CHOLESTEROL HEMISUCCINATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Warren, A.L, Zilberg, G, Capper, M.J, Wacker, D. | | Deposit date: | 2023-01-26 | | Release date: | 2024-05-15 | | Last modified: | 2024-06-19 | | Method: | ELECTRON MICROSCOPY (2.62 Å) | | Cite: | Structural pharmacology and therapeutic potential of 5-methoxytryptamines.
Nature, 630, 2024
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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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8FYT
 | | LSD-bound serotonin 1A (5-HT1A) receptor-Gi1 protein complex | | Descriptor: | (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide, CHOLESTEROL HEMISUCCINATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Warren, A.L, Zilberg, G, Capper, M.J, Wacker, D. | | Deposit date: | 2023-01-26 | | Release date: | 2024-05-15 | | Last modified: | 2024-06-19 | | Method: | ELECTRON MICROSCOPY (2.64 Å) | | Cite: | Structural pharmacology and therapeutic potential of 5-methoxytryptamines.
Nature, 630, 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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8XIO
 | | Structure of L797591-SSTR1 G protein complex | | Descriptor: | (2~{S})-~{N}-[(4~{S})-6-azanyl-2,2,4-trimethyl-hexyl]-3-naphthalen-1-yl-2-[[2-phenylethyl(2-pyridin-2-ylethyl)carbamoyl]amino]propanamide, G-alpha-i, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Wang, Y, Xu, Y, Xu, H.E, Zhuang, Y. | | Deposit date: | 2023-12-19 | | Release date: | 2024-07-03 | | Method: | ELECTRON MICROSCOPY (2.65 Å) | | Cite: | Selective ligand recognition and activation of somatostatin receptors SSTR1 and SSTR3
To Be Published
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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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8IUK
 | | Cryo-EM structure of the PGF2-alpha-bound human PTGFR-Gq 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, G subunit alpha (q), ... | | Authors: | Wu, C, Xu, Y, Xu, H.E. | | Deposit date: | 2023-03-24 | | Release date: | 2023-07-12 | | Last modified: | 2023-11-08 | | Method: | ELECTRON MICROSCOPY (2.67 Å) | | Cite: | Ligand-induced activation and G protein coupling of prostaglandin F 2 alpha receptor.
Nat Commun, 14, 2023
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