7F58
 
 | | Cryo-EM structure of THIQ-MC4R-Gs_Nb35 complex | | Descriptor: | (3R)-N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxidanylidene-propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, CALCIUM ION, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Zhang, H, Chen, L, Mao, C, Shen, Q, Yang, D, Shen, D, Qin, J. | | Deposit date: | 2021-06-21 | | Release date: | 2021-11-03 | | Last modified: | 2022-02-16 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural insights into ligand recognition and activation of the melanocortin-4 receptor.
Cell Res., 31, 2021
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7F54
 | | Cryo-EM structure of afamelanotide-MC4R-Gs_Nb35 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, ... | | Authors: | Zhang, H, Chen, L, Mao, C, Shen, Q, Yang, D, Shen, D, Qin, J. | | Deposit date: | 2021-06-21 | | Release date: | 2021-11-03 | | Last modified: | 2022-02-16 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural insights into ligand recognition and activation of the melanocortin-4 receptor.
Cell Res., 31, 2021
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7F55
 | | Cryo-EM structure of bremelanotide-MC4R-Gs_Nb35 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, ... | | Authors: | Zhang, H, Chen, L, Mao, C, Shen, Q, Yang, D, Shen, D, Qin, J. | | Deposit date: | 2021-06-21 | | Release date: | 2021-11-03 | | Last modified: | 2022-02-16 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural insights into ligand recognition and activation of the melanocortin-4 receptor.
Cell Res., 31, 2021
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7F53
 | | Cryo-EM structure of a-MSH-MC4R-Gs_Nb35 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, ... | | Authors: | Zhang, H, Chen, L, Mao, C, Shen, Q, Yang, D, Shen, D, Qin, J. | | Deposit date: | 2021-06-21 | | Release date: | 2021-11-03 | | Last modified: | 2022-02-16 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural insights into ligand recognition and activation of the melanocortin-4 receptor.
Cell Res., 31, 2021
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8HCX
 | | Cryo-EM structure of Endothelin1-bound ETBR-Gq complex | | Descriptor: | Endothelin receptor type B,Oplophorus-luciferin 2-monooxygenase catalytic subunit chimera, Endothelin-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Yuan, Q, Jiang, Y, Xu, H.E, Ji, Y, Duan, J. | | Deposit date: | 2022-11-03 | | Release date: | 2023-03-22 | | Last modified: | 2023-10-04 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structural basis of peptide recognition and activation of endothelin receptors.
Nat Commun, 14, 2023
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4A16
 | | Structure of mouse Acetylcholinesterase complex with Huprine derivative | | Descriptor: | (1-{4-[(7S,11S)-12-AMINO-3-CHLORO-6,7,10,11-TETRAHYDRO-7,11-METHANOCYCLOOCTA[B]QUINOLIN-9-YL]BUTYL}-1H-1,2,3-TRIAZOL-4-YL)METHANOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ACETYLCHOLINESTERASE, ... | | Authors: | Carletti, E, Colletier, J.P, Nachon, F, Weik, M, Ronco, C, Jean, L, Renard, P.Y. | | Deposit date: | 2011-09-14 | | Release date: | 2012-03-28 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | Huprine Derivatives as Sub-Nanomolar Human Acetylcholinesterase Inhibitors: From Rational Design to Validation by X-Ray Crystallography.
Chemmedchem, 7, 2012
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5UKL
 | | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | | Descriptor: | 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, 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 (2.15 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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8SG1
 | | Cryo-EM structure of CMKLR1 signaling complex | | Descriptor: | CHOLESTEROL, Chemerin 9, Chemerin-like receptor 1, ... | | Authors: | Zhang, X, Zhang, C. | | Deposit date: | 2023-04-11 | | Release date: | 2023-11-01 | | Last modified: | 2023-12-20 | | Method: | ELECTRON MICROSCOPY (2.94 Å) | | Cite: | Structural basis of G protein-Coupled receptor CMKLR1 activation and signaling induced by a chemerin-derived agonist.
Plos Biol., 21, 2023
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8HCQ
 | | Cryo-EM structure of endothelin1-bound ETAR-Gq complex | | Descriptor: | Endothelin-1, Endothelin-1 receptor,Oplophorus-luciferin 2-monooxygenase catalytic subunit chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Yuan, Q, Jiang, Y, Xu, H.E, Ji, Y, Duan, J. | | Deposit date: | 2022-11-02 | | Release date: | 2023-03-22 | | Last modified: | 2023-10-04 | | Method: | ELECTRON MICROSCOPY (3.01 Å) | | Cite: | Structural basis of peptide recognition and activation of endothelin receptors.
Nat Commun, 14, 2023
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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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8HN8
 | | Cryo-EM structure of ligand histamine-bound Histamine H4 receptor 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-1, ... | | Authors: | Tang, W.Q, Sun, X.Y, Li, F.H, Wang, J.Y. | | Deposit date: | 2022-12-07 | | Release date: | 2023-12-20 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structure insights into Histamine H4 receptor activation by an endogenous ligand histamine and agonist imetit
To Be Published
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8HOC
 | | Cryo-EM structure of ligand histamine-bound Histamine H4 receptor Gi complex | | Descriptor: | 2-(1~{H}-imidazol-5-yl)ethyl carbamimidothioate, 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: | Tang, W.Q, Sun, X.Y, Li, F.H, Wang, J.Y. | | Deposit date: | 2022-12-09 | | Release date: | 2023-12-20 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structure insights into Histamine H4 receptor activation by an endogenous ligand histamine and agonist imetit
To Be Published
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5UKM
 | | bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as) | | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(1H-pyrazol-5-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cruz-Rodriguez, O, Tesmer, J.J.G. | | Deposit date: | 2017-01-23 | | Release date: | 2017-04-12 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.03 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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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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7NA8
 | | Structures of human ghrelin receptor-Gi complexes with ghrelin and a synthetic agonist | | Descriptor: | 1-(methanesulfonyl)-1'-(2-methyl-L-alanyl-O-benzyl-D-seryl)-1,2-dihydrospiro[indole-3,4'-piperidine], Antibody fragment, CHOLESTEROL, ... | | Authors: | Liu, H, Sun, D, Sun, J, Zhang, C. | | Deposit date: | 2021-06-20 | | Release date: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
Nat Commun, 12, 2021
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7NA7
 | | Structures of human ghrelin receptor-Gi complexes with ghrelin and a synthetic agonist | | Descriptor: | Antibody fragment, CHOLESTEROL, Ghrelin-27, ... | | Authors: | Liu, H, Sun, D, Sun, J, Zhang, C. | | Deposit date: | 2021-06-20 | | Release date: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
Nat Commun, 12, 2021
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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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8FLR
 | | Human PTH1R in complex with PTHrP 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 (2.94 Å) | | Cite: | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLT
 | | Human PTH1R in complex with M-PTH(1-14) 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 (3.03 Å) | | Cite: | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLQ
 | | Human PTH1R in complex with PTH(1-34) 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 (2.55 Å) | | Cite: | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLS
 | | Human PTH1R in complex with Abaloparatide and Gs | | Descriptor: | Abaloparatide, 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: | 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 (3.09 Å) | | Cite: | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8DWH
 | | CryoEM structure of Gq-coupled MRGPRX1 with ligand Compound-16 | | 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: | 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 (3.25 Å) | | Cite: | Ligand recognition and allosteric modulation of the human MRGPRX1 receptor.
Nat.Chem.Biol., 19, 2023
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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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8DWC
 | | CryoEM structure of Gq-coupled MRGPRX1 with peptide agonist BAM8-22 | | 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: | 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 (2.87 Å) | | Cite: | Ligand recognition and allosteric modulation of the human MRGPRX1 receptor.
Nat.Chem.Biol., 19, 2023
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2X8B
 | | Crystal structure of human acetylcholinesterase inhibited by aged tabun and complexed with fasciculin-II | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, ACETHYLCHOLINESTERASE, CHLORIDE ION, ... | | Authors: | Carletti, E, Colletier, J.P, Nachon, F. | | Deposit date: | 2010-03-08 | | Release date: | 2010-04-28 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | Structural evidence that human acetylcholinesterase inhibited by tabun ages through O-dealkylation.
J. Med. Chem., 53, 2010
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