8XWQ
 
 | | Cryo-EM structure of ET-1 bound ETBR-DNGI complex | | Descriptor: | Endothelin receptor type B, Endothelin-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Tani, K, Maki-Yonekura, S, Kanno, R, Negami, T, Hamaguchi, T, Hall, M, Mizoguchi, A, Humbel, B.M, Terada, T, Yonekura, K, Doi, T. | | Deposit date: | 2024-01-16 | | Release date: | 2024-10-02 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (4.6 Å) | | Cite: | Structure of endothelin ET B receptor-G i complex in a conformation stabilized by unique NPxxL motif.
Commun Biol, 7, 2024
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8ZRT
 | | Cryo-EM structure focused on the receptor of the ET-1 bound ETBR-DNGI complex | | Descriptor: | Endothelin receptor type B, Endothelin-1 | | Authors: | Tani, K, Maki-Yonekura, S, Kanno, R, Negami, T, Hamaguchi, T, Hall, M, Mizoguchi, A, Humbel, B.M, Terada, T, Yonekura, K, Doi, T. | | Deposit date: | 2024-06-05 | | Release date: | 2024-10-02 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.62 Å) | | Cite: | Structure of endothelin ET B receptor-G i complex in a conformation stabilized by unique NPxxL motif.
Commun Biol, 7, 2024
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8QJ2
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8ZPS
 | | Cryo-EM structure of prolactin-releasing peptide recognition with Gi | | 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, Li, Y, Yuan, Q, Xu, H.E. | | Deposit date: | 2024-05-31 | | Release date: | 2024-09-25 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Molecular mechanism of prolactin-releasing peptide recognition and signaling via its G protein-coupled receptor.
Cell Discov, 10, 2024
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8ZPT
 | | Cryo-EM structure of prolactin-releasing peptide recognition with Gq | | Descriptor: | Guanine nucleotide-binding protein G(324) subunit alpha-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: | Zhao, L, Li, Y, Yuan, Q, Xu, H.E. | | Deposit date: | 2024-05-31 | | Release date: | 2024-09-25 | | Last modified: | 2024-11-13 | | Method: | ELECTRON MICROSCOPY (2.96 Å) | | Cite: | Molecular mechanism of prolactin-releasing peptide recognition and signaling via its G protein-coupled receptor.
Cell Discov, 10, 2024
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9F34
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9F33
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8XOR
 | | Cryo-EM structure of the tethered agonist-bound human PAR1-Gq complex | | Descriptor: | CHOLESTEROL, G subunit q (Gi1-Gq chimeric), Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Guo, J, Zhang, Y. | | Deposit date: | 2024-01-02 | | Release date: | 2024-09-18 | | Last modified: | 2024-10-16 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural basis of tethered agonism and G protein coupling of protease-activated receptors.
Cell Res., 34, 2024
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8XOS
 | | Cryo-EM structure of the tethered agonist-bound human PAR1-Gi complex | | 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: | Guo, J, Zhang, Y. | | Deposit date: | 2024-01-02 | | Release date: | 2024-09-18 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural basis of tethered agonism and G protein coupling of protease-activated receptors.
Cell Res., 34, 2024
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8WP1
 | | Cryo-EM structure of SUCR1 in complex with cis-epoxysuccinic acid and Gi proteins | | Descriptor: | (2R,3S)-oxirane-2,3-dicarboxylic 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: | Liu, A, Ye, R.D. | | Deposit date: | 2023-10-08 | | Release date: | 2024-09-11 | | Last modified: | 2024-11-13 | | Method: | ELECTRON MICROSCOPY (3.15 Å) | | Cite: | Structural insights into ligand recognition and activation of the succinate receptor SUCNR1.
Cell Rep, 43, 2024
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8WOG
 | | Cryo-EM structure of SUCR1 in complex with succinate and Gi protein | | 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: | Liu, A, Ye, R.D. | | Deposit date: | 2023-10-07 | | Release date: | 2024-09-11 | | Last modified: | 2024-11-06 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Structural insights into ligand recognition and activation of the succinate receptor SUCNR1.
Cell Rep, 43, 2024
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8Y52
 | | Cryo-EM structure of the BA1-bound BRS3-Gq complex | | Descriptor: | BA1, Bombesin receptor subtype-3, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, C, Xu, Y, Yin, W, Xu, H.E. | | Deposit date: | 2024-01-31 | | Release date: | 2024-09-11 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural insights into ligand recognition, selectivity, and activation of bombesin receptor subtype-3.
Cell Rep, 43, 2024
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8Y53
 | | Cryo-EM structure of the MK-5046-bound BRS3-Gq complex | | Descriptor: | (2~{S})-1,1,1-tris(fluoranyl)-2-(4-pyrazol-1-ylphenyl)-3-[5-[[1-(trifluoromethyl)cyclopropyl]methyl]-1~{H}-imidazol-2-yl]propan-2-ol, Bombesin receptor subtype-3, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, C, Xu, Y, Yin, W, Xu, H.E. | | Deposit date: | 2024-01-31 | | Release date: | 2024-09-11 | | Method: | ELECTRON MICROSCOPY (2.93 Å) | | Cite: | Structural insights into ligand recognition, selectivity, and activation of bombesin receptor subtype-3.
Cell Rep, 43, 2024
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9BQJ
 | | RO76 bound muOR-Gi1-scFv16 complex structure | | 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: | Wang, H, Majumdar, S, Kobilka, B.K. | | Deposit date: | 2024-05-10 | | Release date: | 2024-09-11 | | Last modified: | 2024-10-09 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Signaling Modulation Mediated by Ligand Water Interactions with the Sodium Site at mu OR.
Acs Cent.Sci., 10, 2024
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9CBL
 | | Cryo-EM structure of epinephrine-bound alpha-2A-adrenergic receptor in complex with heterotrimeric Gi-protein | | Descriptor: | Endolysin,Alpha-2A 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: | Lou, J.S, Su, M, Wang, J, Do, H.N, Miao, Y, Huang, X.Y. | | Deposit date: | 2024-06-19 | | Release date: | 2024-09-11 | | Last modified: | 2024-10-16 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Distinct binding conformations of epinephrine with alpha- and beta-adrenergic receptors.
Exp.Mol.Med., 56, 2024
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9CBM
 | | Cryo-EM structure of dexmedetomidine-bound alpha-2A-adrenergic receptor in complex with heterotrimeric Gi-protein | | Descriptor: | 4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole, Endolysin,Alpha-2A adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Lou, J.S, Su, M, Wang, J, Do, H.N, Miao, Y, Huang, X.Y. | | Deposit date: | 2024-06-19 | | Release date: | 2024-09-11 | | Last modified: | 2024-10-16 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Distinct binding conformations of epinephrine with alpha- and beta-adrenergic receptors.
Exp.Mol.Med., 56, 2024
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8JXR
 | | Structure of nanobody-bound DRD1_LSD complex | | Descriptor: | (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide, D(1A) dopamine receptor, Fab 8D3 heavy chain, ... | | Authors: | Zhuang, Y, Xu, Y, Fan, L, Wang, S, Xu, H.E. | | Deposit date: | 2023-07-01 | | Release date: | 2024-09-04 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.57 Å) | | Cite: | Structural basis of psychedelic LSD recognition at dopamine D 1 receptor.
Neuron, 112, 2024
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8XVJ
 | | Cryo-EM structure of ETAR bound with Macitentan | | Descriptor: | 6-[2-(5-bromanylpyrimidin-2-yl)oxyethoxy]-5-(4-bromophenyl)-~{N}-(propylsulfamoyl)pyrimidin-4-amine, Endoglucanase H,Endothelin-1 receptor,Soluble cytochrome b562, anti-BRIL Fab Heavy chain, ... | | Authors: | Hou, J.Y, Liu, S.H, Wu, L.J, Liu, Z.J, Hua, T. | | Deposit date: | 2024-01-15 | | Release date: | 2024-08-28 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.26 Å) | | Cite: | Structural basis of antagonist selectivity in endothelin receptors.
Cell Discov, 10, 2024
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8XVK
 | | Cryo-EM structure of ETAR bound with Ambrisentan | | Descriptor: | (2~{S})-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenyl-propanoic acid, Endoglucanase H,Endothelin-1 receptor,Soluble cytochrome b562, anti-BRIL Fab Heavy chain, ... | | Authors: | Hou, J.Y, Liu, S.H, Wu, L.J, Liu, Z.J, Hua, T. | | Deposit date: | 2024-01-15 | | Release date: | 2024-08-28 | | Method: | ELECTRON MICROSCOPY (3.21 Å) | | Cite: | Structural basis of antagonist selectivity in endothelin receptors.
Cell Discov, 10, 2024
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8XVL
 | | Cryo-EM structure of ETAR bound with Zibotentan | | Descriptor: | Endoglucanase H,Endothelin-1 receptor,Soluble cytochrome b562, anti-BRIL Fab Heavy chain, anti-BRIL Fab Light chain, ... | | Authors: | Hou, J.Y, Liu, S.H, Wu, L.J, Liu, Z.J, Hua, T. | | Deposit date: | 2024-01-15 | | Release date: | 2024-08-28 | | Last modified: | 2024-11-06 | | Method: | ELECTRON MICROSCOPY (3.22 Å) | | Cite: | Structural basis of antagonist selectivity in endothelin receptors.
Cell Discov, 10, 2024
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8XVI
 | | Cryo-EM structure of ETAR bound with Endothelin1 | | Descriptor: | Endoglucanase H,Endothelin-1 receptor, Endothelin-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hou, J.Y, Liu, S.H, Wu, L.J, Liu, Z.J, Hua, T. | | Deposit date: | 2024-01-15 | | Release date: | 2024-08-28 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.32 Å) | | Cite: | Structural basis of antagonist selectivity in endothelin receptors.
Cell Discov, 10, 2024
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8XVH
 | | Cryo-EM structure of ETBR bound with Endothelin1 | | Descriptor: | Endothelin-1, Exo-alpha-sialidase,Endothelin receptor type B, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hou, J.Y, Liu, S.H, Wu, L.J, Liu, Z.J, Hua, T. | | Deposit date: | 2024-01-15 | | Release date: | 2024-08-28 | | Last modified: | 2024-11-13 | | Method: | ELECTRON MICROSCOPY (3.26 Å) | | Cite: | Structural basis of antagonist selectivity in endothelin receptors.
Cell Discov, 10, 2024
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8XVE
 | | Cryo-EM structure of ETBR bound with BQ3020 | | Descriptor: | BQ3020, Exo-alpha-sialidase,Endothelin receptor type B, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hou, J.Y, Liu, S.H, Wu, L.J, Liu, Z.J, Hua, T. | | Deposit date: | 2024-01-15 | | Release date: | 2024-08-28 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural basis of antagonist selectivity in endothelin receptors.
Cell Discov, 10, 2024
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8ZMF
 | | Crystal structure of an inverse agonist antipsychotic drug derivative-bound 5-HT2C | | Descriptor: | 1-[(4-fluorophenyl)methyl]-1-[(8~{S})-5-methyl-5-azaspiro[2.5]octan-8-yl]-3-[[4-(2-methylpropoxy)phenyl]methyl]urea, 5-hydroxytryptamine receptor 2C,Soluble cytochrome b562 | | Authors: | Oguma, T, Asada, H, Sekiguchi, Y, Imono, M, Iwata, S, Kusakabe, K. | | Deposit date: | 2024-05-23 | | Release date: | 2024-08-28 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (3.6 Å) | | Cite: | Dual 5-HT 2A and 5-HT 2C Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis.
J.Med.Chem., 67, 2024
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8ZMG
 | | Crystal structure of an inverse agonist antipsychotic drug pimavanserin-bound 5-HT2A | | Descriptor: | 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, Pimavanserin | | Authors: | Oguma, T, Asada, H, Sekiguchi, Y, Imono, M, Iwata, S, Kusakabe, K. | | Deposit date: | 2024-05-23 | | Release date: | 2024-08-28 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Dual 5-HT 2A and 5-HT 2C Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis.
J.Med.Chem., 67, 2024
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