7W41
 
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7VOE
 | | Crystal structure of 5-HT2AR in complex with aripiprazole | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, 7-[4-[4-[2,3-bis(chloranyl)phenyl]piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one, ... | | Authors: | Chen, Z, Fan, L, Wang, H, Yu, J, Lu, D, Qi, J, Nie, F, Luo, Z, Liu, Z, Cheng, J, Wang, S. | | Deposit date: | 2021-10-13 | | Release date: | 2021-12-22 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties.
Nat.Neurosci., 25, 2022
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7VUY
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7VV3
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7VOD
 | | Crystal structure of 5-HT2AR in complex with cariprazine | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 3-[4-[2-[4-[2,3-bis(chloranyl)phenyl]piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethyl-urea, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, ... | | Authors: | Chen, Z, Fan, L, Wang, H, Yu, J, Lu, D, Qi, J, Nie, F, Luo, Z, Liu, Z, Cheng, J, Wang, S. | | Deposit date: | 2021-10-13 | | Release date: | 2021-12-22 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties.
Nat.Neurosci., 25, 2022
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7VUH
 | | Cryo-EM structure of a class A orphan GPCR | | Descriptor: | 3-chloranyl-N-[2-oxidanylidene-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide, 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, Zhou, Y.L, Wu, L.J. | | Deposit date: | 2021-11-02 | | Release date: | 2021-12-29 | | Last modified: | 2025-06-18 | | Method: | ELECTRON MICROSCOPY (3.22 Å) | | Cite: | Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139.
Cell Res., 32, 2022
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7VUG
 | | Cryo-EM structure of a class A orphan GPCR in complex with Gi | | Descriptor: | 3-chloranyl-N-[2-oxidanylidene-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide, Chimera of Endo-1,4-beta-xylanase and Probable G-protein coupled receptor 139, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liu, Z.J, Hua, T, Zhou, Y.L, Wu, L.J. | | Deposit date: | 2021-11-02 | | Release date: | 2021-12-29 | | Last modified: | 2025-06-18 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139.
Cell Res., 32, 2022
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7WF7
 | | Cryo-EM of Sphingosine 1-phosphate receptor 1 / Gi complex bound to S1P | | Descriptor: | (2S,3R,4E)-2-amino-3-hydroxyoctadec-4-en-1-yl dihydrogen phosphate, 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: | He, Y, Xu, Z. | | Deposit date: | 2021-12-26 | | Release date: | 2022-01-05 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism.
Nat.Chem.Biol., 18, 2022
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7W2Z
 | | Cryo-EM structure of the ghrelin-bound human ghrelin receptor-Go complex | | Descriptor: | Appetite-regulating hormone, CHOLESTEROL, Growth hormone secretagogue receptor type 1, ... | | Authors: | Qin, J, Ming, Q, Ji, S, Mao, C, Shen, D, Zhang, Y. | | Deposit date: | 2021-11-24 | | Release date: | 2022-01-19 | | Last modified: | 2022-02-16 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Molecular mechanism of agonism and inverse agonism in ghrelin receptor.
Nat Commun, 13, 2022
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7WC6
 | | Crystal structure of serotonin 2A receptor in complex with LSD | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (8alpha)-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide, 5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, ... | | Authors: | Cao, D, Yu, J, Wang, H, Luo, Z, Liu, X, He, L, Qi, J, Fan, L, Tang, L, Chen, Z, Li, J, Cheng, J, Wang, S. | | Deposit date: | 2021-12-18 | | Release date: | 2022-01-26 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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7WC9
 | | Crystal structure of serotonin 2A receptor in complex with non-hallucinogenic psychedelic analog | | Descriptor: | (10~{R},15~{S})-12-[3-(2-methoxyphenyl)propyl]-4-methyl-1,4,12-triazatetracyclo[7.6.1.0^{5,16}.0^{10,15}]hexadeca-5(16),6,8-triene, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2A,5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, ... | | Authors: | Cao, D, Yu, J, Wang, H, Luo, Z, Liu, X, He, L, Qi, J, Fan, L, Tang, L, Chen, Z, Li, J, Cheng, J, Wang, S. | | Deposit date: | 2021-12-18 | | Release date: | 2022-01-26 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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7WC7
 | | Crystal structure of serotonin 2A receptor in complex with lisuride | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2A,5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, CHOLESTEROL, ... | | Authors: | Cao, D, Yu, J, Wang, H, Luo, Z, Liu, X, He, L, Qi, J, Fan, L, Tang, L, Chen, Z, Li, J, Cheng, J, Wang, S. | | Deposit date: | 2021-12-18 | | Release date: | 2022-01-26 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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7WC8
 | | Crystal structure of serotonin 2A receptor in complex with lumateperone | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-(4-fluorophenyl)-4-[(10~{R},15~{S})-4-methyl-1,4,12-triazatetracyclo[7.6.1.0^{5,16}.0^{10,15}]hexadeca-5,7,9(16)-trien-12-yl]butan-1-one, 5-hydroxytryptamine receptor 2A,5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, ... | | Authors: | Cao, D, Yu, J, Wang, H, Luo, Z, Liu, X, He, L, Qi, J, Fan, L, Tang, L, Chen, Z, Li, J, Cheng, J, Wang, S. | | Deposit date: | 2021-12-18 | | Release date: | 2022-01-26 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Structure-based discovery of nonhallucinogenic psychedelic analogs.
Science, 375, 2022
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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: | 2025-05-21 | | 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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7VIG
 | | Cryo-EM structure of Gi coupled Sphingosine 1-phosphate receptor bound with CBP-307 | | Descriptor: | 1-[[2-fluoranyl-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-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: | Yu, L.Y, Gan, B, Xiao, Q.J, Ren, R.B. | | Deposit date: | 2021-09-26 | | Release date: | 2022-09-28 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structural insights into sphingosine-1-phosphate receptor activation.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7VIE
 | | Cryo-EM structure of Gi coupled Sphingosine 1-phosphate receptor bound with S1P | | Descriptor: | (2S,3R,4E)-2-amino-3-hydroxyoctadec-4-en-1-yl dihydrogen phosphate, 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: | Yu, L.Y, Gan, B, Xiao, Q.J, Ren, R.B. | | Deposit date: | 2021-09-26 | | Release date: | 2022-09-28 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.86 Å) | | Cite: | Structural insights into sphingosine-1-phosphate receptor activation.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7VIF
 | | Cryo-EM structure of Gi coupled Sphingosine 1-phosphate receptor bound with (S)-FTY720-P | | Descriptor: | (2~{S})-2-azanyl-4-(4-octylphenyl)-2-[[oxidanyl-bis(oxidanylidene)-$l^{6}-phosphanyl]oxymethyl]butan-1-ol, 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: | Yu, L.Y, Gan, B, Xiao, Q.J, Ren, R.B. | | Deposit date: | 2021-09-26 | | Release date: | 2022-09-28 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (2.83 Å) | | Cite: | Structural insights into sphingosine-1-phosphate receptor activation.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7VIH
 | | Cryo-EM structure of Gi coupled Sphingosine 1-phosphate receptor bound with CBP-307 | | Descriptor: | 1-[[2-fluoranyl-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-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: | Yu, L.Y, Gan, B, Xiao, Q.J, Ren, R.B. | | Deposit date: | 2021-09-26 | | Release date: | 2022-09-28 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.98 Å) | | Cite: | Structural insights into sphingosine-1-phosphate receptor activation.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7X9B
 | | Cryo-EM structure of neuropeptide Y Y2 receptor in complex with NPY and 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(i) subunit alpha-1, ... | | Authors: | Tang, T, Han, S, Zhao, Q, Wu, B. | | Deposit date: | 2022-03-15 | | Release date: | 2022-05-18 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Receptor-specific recognition of NPY peptides revealed by structures of NPY receptors.
Sci Adv, 8, 2022
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7X9A
 | | Cryo-EM structure of neuropeptide Y Y1 receptor in complex with NPY and 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(i) subunit alpha-1, ... | | Authors: | Tang, T, Han, S, Zhao, Q, Wu, B. | | Deposit date: | 2022-03-15 | | Release date: | 2022-05-18 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Receptor-specific recognition of NPY peptides revealed by structures of NPY receptors.
Sci Adv, 8, 2022
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7X9C
 | | Cryo-EM structure of neuropeptide Y Y4 receptor in complex with PP and 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(i) subunit alpha-1, ... | | Authors: | Tang, T, Han, S, Zhao, Q, Wu, B. | | Deposit date: | 2022-03-15 | | Release date: | 2022-05-18 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Receptor-specific recognition of NPY peptides revealed by structures of NPY receptors.
Sci Adv, 8, 2022
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7WV9
 | | Allosteric modulator ZCZ011 binding to CP55940-bound cannabinoid receptor 1 in complex with Gi protein | | Descriptor: | 2-[(1R,2R,5R)-5-hydroxy-2-(3-hydroxypropyl)cyclohexyl]-5-(2-methyloctan-2-yl)phenol, 6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole, Cannabinoid receptor 1, ... | | Authors: | Xu, Z, Shao, Z. | | Deposit date: | 2022-02-10 | | Release date: | 2022-06-15 | | Last modified: | 2024-11-13 | | Method: | ELECTRON MICROSCOPY (3.36 Å) | | Cite: | Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1.
Nat.Chem.Biol., 18, 2022
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7X2F
 | | Cryo-EM structure of the dopamine and LY3154207-bound D1 dopamine receptor and mini-Gs complex | | Descriptor: | 2-[2,6-bis(chloranyl)phenyl]-1-[(1S,3R)-3-(hydroxymethyl)-1-methyl-5-(3-methyl-3-oxidanyl-butyl)-3,4-dihydro-1H-isoquinolin-2-yl]ethanone, CHOLESTEROL, D(1A) dopamine receptor, ... | | Authors: | Teng, X, Zheng, S. | | Deposit date: | 2022-02-25 | | Release date: | 2022-06-15 | | Last modified: | 2025-06-18 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Ligand recognition and biased agonism of the D1 dopamine receptor.
Nat Commun, 13, 2022
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7WKD
 | | TRH-TRHR G protein complex | | Descriptor: | Gq, 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, Y, Cai, H, You, C, He, X, Yuan, Q, Jiang, H, Cheng, X, Jiang, Y, Xu, H.E. | | Deposit date: | 2022-01-09 | | Release date: | 2022-06-15 | | Last modified: | 2022-09-14 | | Method: | ELECTRON MICROSCOPY (3.01 Å) | | Cite: | Structural insights into ligand binding and activation of the human thyrotropin-releasing hormone receptor.
Cell Res., 32, 2022
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7UTZ
 | | Human thyrotropin analog TR1402 bound to human Thyrotropin receptor in complex with miniGs399 (composite structure) | | Descriptor: | (2S)-3-hydroxypropane-1,2-diyl dihexadecanoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glycoprotein hormones alpha chain analog TR1402, ... | | Authors: | Faust, B, Cheng, Y, Manglik, A. | | Deposit date: | 2022-04-28 | | Release date: | 2022-08-03 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Autoantibody mimicry of hormone action at the thyrotropin receptor.
Nature, 609, 2022
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