8CU6
 
 | | Crystal structure of A2AAR-StaR2-S277-bRIL in complex with a novel A2a antagonist, LJ-4517 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2R,3R,4R)-2-[(8P)-6-amino-2-(hex-1-yn-1-yl)-8-(thiophen-2-yl)-9H-purin-9-yl]oxolane-3,4-diol, Adenosine receptor A2a,Soluble cytochrome b562, ... | | Authors: | Shiriaeva, A, Park, D.-J, Kim, G, Lee, Y, Hou, X, Jarhad, D.B, Kim, G, Yu, J, Hyun, Y.E, Kim, W, Gao, Z.-G, Jacobson, K.A, Han, G.W, Stevens, R.C, Jeong, L.S, Choi, S, Cherezov, V. | | Deposit date: | 2022-05-16 | | Release date: | 2022-08-31 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A 2A Adenosine Receptor.
J.Med.Chem., 65, 2022
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8CU7
 | | Crystal structure of A2AAR-StaR2-bRIL in complex with a novel A2a antagonist, LJ-4517 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2R,3R,4R)-2-[(8P)-6-amino-2-(hex-1-yn-1-yl)-8-(thiophen-2-yl)-9H-purin-9-yl]oxolane-3,4-diol, Adenosine receptor A2a,Soluble cytochrome b562, ... | | Authors: | Shiriaeva, A, Park, D.-J, Kim, G, Lee, Y, Hou, X, Jarhad, D.B, Kim, G, Yu, J, Hyun, Y.E, Kim, W, Gao, Z.-G, Jacobson, K.A, Han, G.W, Stevens, R.C, Jeong, L.S, Choi, S, Cherezov, V. | | Deposit date: | 2022-05-16 | | Release date: | 2022-08-31 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A 2A Adenosine Receptor.
J.Med.Chem., 65, 2022
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7XAT
 | | Structure of somatostatin receptor 2 bound with SST14. | | 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: | Bo, Q, Yang, F, Li, Y.G, Meng, X.Y, Zhang, H.H, Zhou, Y.X, Ling, S.L, Sun, D.M, Lv, P, Liu, L, Shi, P, Tian, C.L. | | Deposit date: | 2022-03-19 | | Release date: | 2022-08-31 | | Method: | ELECTRON MICROSCOPY (2.85 Å) | | Cite: | Structural insights into the activation of somatostatin receptor 2 by cyclic SST analogues.
Cell Discov, 8, 2022
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7X1U
 | | Structure of Thyrotropin-Releasing Hormone Receptor bound with an Endogenous Peptide Agonist TRH. | | Descriptor: | Endogenous Peptide Agonist TRH, 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, F, Zhang, H.H, Meng, X.Y, Li, Y.G, Zhou, Y.X, Ling, S.L, Liu, L, Shi, P, Tian, C.L. | | Deposit date: | 2022-02-24 | | Release date: | 2022-08-31 | | Last modified: | 2022-09-14 | | Method: | ELECTRON MICROSCOPY (3.19 Å) | | Cite: | Structural insights into thyrotropin-releasing hormone receptor activation by an endogenous peptide agonist or its orally administered analogue.
Cell Res., 32, 2022
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7XAV
 | | Structure of somatostatin receptor 2 bound with lanreotide. | | 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: | Bo, Q, Yang, F, Li, Y.G, Meng, X.Y, Zhang, H.H, Zhou, Y.X, Ling, S.L, Sun, D.M, Lv, P, Liu, L, Shi, P, Tian, C.L. | | Deposit date: | 2022-03-19 | | Release date: | 2022-08-31 | | Method: | ELECTRON MICROSCOPY (2.87 Å) | | Cite: | Structural insights into the activation of somatostatin receptor 2 by cyclic SST analogues.
Cell Discov, 8, 2022
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7XAU
 | | Structure of somatostatin receptor 2 bound with octreotide. | | 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: | Bo, Q, Yang, F, Li, Y.G, Meng, X.Y, Zhang, H.H, Zhou, Y.X, Ling, S.L, Sun, D.M, Lv, P, Liu, L, Shi, P, Tian, C.L. | | Deposit date: | 2022-03-19 | | Release date: | 2022-08-31 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Structural insights into the activation of somatostatin receptor 2 by cyclic SST analogues.
Cell Discov, 8, 2022
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7X1T
 | | Structure of Thyrotropin-Releasing Hormone Receptor bound with Taltirelin. | | 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, ScFv16, ... | | Authors: | Yang, F, Zhang, H.H, Meng, X.Y, Li, Y.G, Zhou, Y.X, Ling, S.L, Liu, L, Shi, P, Tian, C.L. | | Deposit date: | 2022-02-24 | | Release date: | 2022-08-31 | | Last modified: | 2022-09-14 | | Method: | ELECTRON MICROSCOPY (3.26 Å) | | Cite: | Structural insights into thyrotropin-releasing hormone receptor activation by an endogenous peptide agonist or its orally administered analogue.
Cell Res., 32, 2022
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7XW5
 | | TSHR-thyroid stimulating hormone-Gs-ML109 complex | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL, Glycoprotein hormones alpha chain, ... | | 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: | 2022-08-24 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (2.96 Å) | | Cite: | Hormone- and antibody-mediated activation of the thyrotropin receptor.
Nature, 609, 2022
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7XZ6
 | | GPR119-Gs-APD668 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(s) subunit alpha isoforms short, ... | | Authors: | Xu, P, Huang, S, Jiang, Y, Xu, H.E. | | Deposit date: | 2022-06-02 | | Release date: | 2022-08-24 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Structural identification of lysophosphatidylcholines as activating ligands for orphan receptor GPR119.
Nat.Struct.Mol.Biol., 29, 2022
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7XZ5
 | | GPR119-Gs-LPC complex | | Descriptor: | (4R,7R,18E)-4,7-dihydroxy-N,N,N-trimethyl-10-oxo-3,5,9-trioxa-4-phosphaheptacos-18-en-1-aminium 4-oxide, 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, P, Huang, S, Jiang, Y, Xu, H.E. | | Deposit date: | 2022-06-02 | | Release date: | 2022-08-24 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural identification of lysophosphatidylcholines as activating ligands for orphan receptor GPR119.
Nat.Struct.Mol.Biol., 29, 2022
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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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8DPH
 | | Cryo-EM structure of the 5HT2C receptor (VGV isoform) bound to lorcaserin | | Descriptor: | (1R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 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 (3.2 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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8DPF
 | | Cryo-EM structure of the 5HT2C receptor (INI isoform) bound to lorcaserin | | Descriptor: | (1R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 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 (2.84 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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8DPI
 | | Cryo-EM structure of the 5HT2C receptor (VSV isoform) bound to lorcaserin | | Descriptor: | (1R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 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 (3.4 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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7XA3
 | | Cryo-EM structure of the CCL2 bound CCR2-Gi complex | | Descriptor: | C-C motif chemokine 2, 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: | Shao, Z, Tan, Y, Shen, Q, Yao, B, Hou, L, Qin, J, Xu, P, Mao, C, Chen, L, Zhang, H, Shen, D, Zhang, C, Li, W, Du, X, Li, F, Chen, Z, Jiang, Y, Xu, H.E, Ying, S, Ma, H, Zhang, Y, Shen, H. | | Deposit date: | 2022-03-17 | | Release date: | 2022-08-24 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Molecular insights into ligand recognition and activation of chemokine receptors CCR2 and CCR3.
Cell Discov, 8, 2022
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7X9Y
 | | Cryo-EM structure of the apo CCR3-Gi complex | | Descriptor: | C-C chemokine receptor type 3, 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: | Shao, Z, Tan, Y, Shen, Q, Yao, B, Hou, L, Qin, J, Xu, P, Mao, C, Chen, L, Zhang, H, Shen, D, Zhang, C, Li, W, Du, X, Li, F, Chen, Z, Jiang, Y, Xu, H.E, Ying, S, Ma, H, Zhang, Y, Shen, H. | | Deposit date: | 2022-03-16 | | Release date: | 2022-08-24 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Molecular insights into ligand recognition and activation of chemokine receptors CCR2 and CCR3.
Cell Discov, 8, 2022
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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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7XW7
 | | TSHR-K1-70 complex | | Descriptor: | K1-70 scFv, Thyrotropin receptor | | 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: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (5.5 Å) | | Cite: | Hormone- and antibody-mediated activation of the thyrotropin receptor.
Nature, 609, 2022
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7WU9
 | | Cryo-EM structure of the human EP3-Gi signaling 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: | Suno, R, Sugita, Y, Morimoto, K, Iwasaki, K, Kato, T, Kobayashi, T. | | Deposit date: | 2022-02-07 | | Release date: | 2022-08-17 | | Last modified: | 2023-10-04 | | Method: | ELECTRON MICROSCOPY (3.375 Å) | | Cite: | Structural insights into the G protein selectivity revealed by the human EP3-G i signaling complex.
Cell Rep, 40, 2022
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7T32
 | | CryoEM structure of the adenosine 2A receptor-BRIL/Anti BRIL Fab complex with ZM241385 | | Descriptor: | 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol, Adenosine receptor A2a/Soluble cytochrome b562 Fusion Protein | | Authors: | Zhang, K.H, Wu, H, Hoppe, N, Manglik, A, Cheng, Y.F. | | Deposit date: | 2021-12-06 | | Release date: | 2022-08-10 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Fusion protein strategies for cryo-EM study of G protein-coupled receptors.
Nat Commun, 13, 2022
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7T9M
 | | Human Thyrotropin receptor bound by CS-17 Inverse Agonist Fab/Org 274179-0 Antagonist | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, CS-17 Heavy Chain, ... | | Authors: | Faust, B, Cheng, Y, Manglik, A. | | Deposit date: | 2021-12-19 | | Release date: | 2022-08-10 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Autoantibody mimicry of hormone action at the thyrotropin receptor.
Nature, 609, 2022
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7QVM
 | | Human Oxytocin receptor (OTR) oxytocin Gq chimera (mGoqi) complex | | Descriptor: | Antibody fragment scFv16, 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: | Waltenspuhl, Y, Ehrenmann, J, Vacca, S, Thom, C, Medalia, O, Pluckthun, A. | | Deposit date: | 2022-01-21 | | Release date: | 2022-08-10 | | Method: | ELECTRON MICROSCOPY (3.25 Å) | | Cite: | Structural basis for the activation and ligand recognition of the human oxytocin receptor.
Nat Commun, 13, 2022
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7YXA
 | | XFEL crystal structure of the human sphingosine 1 phosphate receptor 5 in complex with ONO-5430608 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, 4-[6-(2-naphthalen-1-ylethoxy)-2,3,4,5-tetrahydro-1H-3-benzazepin-3-ium-3-yl]butanoic acid, ... | | Authors: | Lyapina, E, Marin, E, Gusach, A, Orekhov, P, Gerasimov, A, Luginina, A, Vakhrameev, D, Ergasheva, M, Kovaleva, M, Khusainov, G, Khorn, P, Shevtsov, M, Kovalev, K, Okhrimenko, I, Bukhdruker, S, Popov, P, Hu, H, Weierstall, U, Liu, W, Cho, Y, Gushchin, I, Rogachev, A, Bourenkov, G, Park, S, Park, G, Huyn, H.J, Park, J, Gordeliy, V, Borshchevskiy, V, Mishin, A, Cherezov, V. | | Deposit date: | 2022-02-15 | | Release date: | 2022-08-10 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structural basis for receptor selectivity and inverse agonism in S1P 5 receptors.
Nat Commun, 13, 2022
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8DU3
 | | Crystal structure of A2AAR-StaR2-bRIL in complex with compound 21a | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (4M)-6-bromo-4-(furan-2-yl)quinazolin-2-amine, Adenosine receptor A2a, ... | | Authors: | Shiriaeva, A, Stauch, B, Han, G.W, Cherezov, V. | | Deposit date: | 2022-07-26 | | Release date: | 2022-08-10 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | High ligand efficiency quinazoline compounds as novel A 2A adenosine receptor antagonists.
Eur.J.Med.Chem., 241, 2022
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7T9I
 | | Native human TSH bound to human Thyrotropin receptor in complex with miniGs399 (composite structure) | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Glycoprotein hormones alpha chain, ... | | Authors: | Faust, B, Cheng, Y, Manglik, A. | | Deposit date: | 2021-12-19 | | Release date: | 2022-08-03 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Autoantibody mimicry of hormone action at the thyrotropin receptor.
Nature, 609, 2022
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