8JPD
 
 | | Focused refinement structure of GRK2 in NTSR1-GRK2-Galpha(q) complexes | | Descriptor: | Beta-adrenergic receptor kinase 1, STAUROSPORINE | | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | | Deposit date: | 2023-06-11 | | Release date: | 2023-08-09 | | Last modified: | 2023-08-30 | | Method: | ELECTRON MICROSCOPY (2.81 Å) | | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist.
Nature, 620, 2023
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8J7S
 | | Structure of the SPARTA complex | | Descriptor: | DNA (5'-D(P*TP*AP*AP*TP*AP*GP*AP*TP*TP*AP*GP*AP*GP*CP*CP*GP*TP*CP*AP*AP*TP*AP*GP*A)-3'), Piwi domain-containing protein, RNA (5'-R(P*UP*GP*AP*CP*GP*GP*CP*UP*CP*UP*AP*AP*UP*CP*UP*AP*UP*UP*A)-3'), ... | | Authors: | Guo, M, Zhu, Y, Lin, Z, Huang, Z. | | Deposit date: | 2023-04-28 | | Release date: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (2.84 Å) | | Cite: | Cryo-EM structure of the ssDNA-activated SPARTA complex.
Cell Res., 33, 2023
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7E9G
 | | Cryo-EM structure of Gi-bound metabotropic glutamate receptor mGlu2 | | Descriptor: | (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 1-butyl-3-chloranyl-4-(4-phenylpiperidin-1-yl)pyridin-2-one, DN13, ... | | Authors: | Lin, S, Han, S, Zhao, Q, Wu, B. | | Deposit date: | 2021-03-04 | | Release date: | 2021-06-23 | | Last modified: | 2021-08-04 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structures of G i -bound metabotropic glutamate receptors mGlu2 and mGlu4.
Nature, 594, 2021
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7E9H
 | | Cryo-EM structure of Gi-bound metabotropic glutamate receptor mGlu4 | | 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-3, ... | | Authors: | Lin, S, Han, S, Zhao, Q, Wu, B. | | Deposit date: | 2021-03-04 | | Release date: | 2021-06-23 | | Last modified: | 2021-07-07 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structures of G i -bound metabotropic glutamate receptors mGlu2 and mGlu4.
Nature, 594, 2021
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2N87
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6ILQ
 | | Crystal structure of PPARgamma with compound BR101549 | | Descriptor: | Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma, ethyl [2-butyl-6-oxo-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl}-4-(propan-2-yl)-1,6-dihydropyrimidin-5-yl]acetate | | Authors: | Hong, E, Jang, T.H, Chin, J, Kim, K.H, Jung, W, Kim, S.H. | | Deposit date: | 2018-10-19 | | Release date: | 2019-09-11 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.408 Å) | | Cite: | Identification of BR101549 as a lead candidate of non-TZD PPAR gamma agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
Bioorg.Med.Chem.Lett., 29, 2019
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5WUZ
 | | Morintides mO1 | | Descriptor: | Morintide mO1 | | Authors: | Xiao, T, Tam, J.P. | | Deposit date: | 2016-12-21 | | Release date: | 2017-01-25 | | Last modified: | 2023-06-14 | | Method: | SOLUTION NMR | | Cite: | Morintides: 8C-Hevein-like peptides without a protein cargo from the drumstick tree Moringa oleifera
To Be Published
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7UYB
 | | Inhibitor bound VIM1 | | Descriptor: | (2M)-4'-(piperidin-4-yl)-2-(1H-tetrazol-5-yl)-4-(trifluoromethyl)[1,1'-biphenyl]-3-sulfonamide, Beta-lactamase VIM-1, ZINC ION | | Authors: | Fischmann, T.O, Scapin, G. | | Deposit date: | 2022-05-06 | | Release date: | 2023-05-24 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (1.11 Å) | | Cite: | Structure Guided Discovery of Novel Pan Metallo-beta-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
J.Med.Chem., 67, 2024
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7UYC
 | | Inhibitor bound VIM1 | | Descriptor: | (2P)-4'-(piperidin-4-yl)-4-[(piperidin-4-yl)methyl]-2-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-sulfonamide, Beta-lactamase VIM-1, MAGNESIUM ION, ... | | Authors: | Fischmann, T.O, Scapin, G. | | Deposit date: | 2022-05-06 | | Release date: | 2023-05-24 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (1.02 Å) | | Cite: | Structure Guided Discovery of Novel Pan Metallo-beta-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
J.Med.Chem., 67, 2024
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6A6O
 | | Crystal structure of acetyl ester-xyloside bifunctional hydrolase from Caldicellulosiruptor lactoaceticus | | Descriptor: | Esterase/lipase-like protein | | Authors: | Cao, H, Huang, Y, Sun, L.C, Liu, X, Liu, T.F, Wang, F.Z, Xin, F.J. | | Deposit date: | 2018-06-28 | | Release date: | 2019-06-12 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structural Insights into the Dual-Substrate Recognition and Catalytic Mechanisms of a Bifunctional Acetyl Ester-Xyloside Hydrolase from Caldicellulosiruptor lactoaceticus.
Acs Catalysis, 9, 2019
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7VAB
 | | Cryo-EM structure of the non-acylated tirzepatide (LY3298176)-bound human GIPR-Gs complex | | Descriptor: | CHOLESTEROL, Gastric inhibitory polypeptide receptor,Gastric inhibitory polypeptide receptor,Gastric inhibitory polypeptide receptor,human glucose-dependent insulinotropic polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Zhao, F.H, Zhou, Q.T, Cong, Z.T, Hang, K.N, Zou, X.Y, Zhang, C, Chen, Y, Dai, A.T, Liang, A.Y, Ming, Q.Q, Wang, M, Chen, L.N, Xu, P.Y, Chang, R.L, Feng, W.B, Xia, T, Zhang, Y, Wu, B.L, Yang, D.H, Zhao, L.H, Xu, H.E, Wang, M.W. | | Deposit date: | 2021-08-28 | | Release date: | 2022-03-02 | | Last modified: | 2022-03-16 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors.
Nat Commun, 13, 2022
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7VBI
 | | Cryo-EM structure of the non-acylated tirzepatide (LY3298176)-bound human GLP-1R-Gs complex | | Descriptor: | Glucagon-like peptide 1 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: | Zhao, F.H, Zhou, Q.T, Cong, Z.T, Hang, K.N, Zou, X.Y, Zhang, C, Chen, Y, Dai, A.T, Liang, A.Y, Ming, Q.Q, Wang, M, Chen, L.N, Xu, P.Y, Chang, R.L, Feng, W.B, Xia, T, Zhang, Y, Wu, B.L, Yang, D.H, Zhao, L.H, Xu, H.E, Wang, M.W. | | Deposit date: | 2021-08-31 | | Release date: | 2022-03-02 | | Last modified: | 2022-03-16 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors.
Nat Commun, 13, 2022
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7VQX
 | | Cryo-EM structure of human vasoactive intestinal polypeptide receptor 2 (VIP2R) in complex with PACAP27 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: | Xu, Y.N, Feng, W.B, Zhou, Q.T, Liang, A.Y, Li, J, Dai, A.T, Zhao, F.H, Yan, J.H, Chen, C.W, Li, H, Zhao, L.H, Xia, T, Jiang, Y, Xu, H.E, Yang, D.H, Wang, M.W. | | Deposit date: | 2021-10-21 | | Release date: | 2022-05-18 | | Method: | ELECTRON MICROSCOPY (2.74 Å) | | Cite: | A distinctive ligand recognition mechanism by the human vasoactive intestinal polypeptide receptor 2.
Nat Commun, 13, 2022
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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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7X8S
 | | Cryo-EM structure of the WB4-24-bound hGLP-1R-Gs complex | | Descriptor: | 2,4-bis(3-methoxy-4-thiophen-2-ylcarbonyloxy-phenyl)-1,3-bis[[4-(2-methylpropanoylamino)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 (3.09 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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7WBJ
 | | Cryo-EM structure of N-terminal modified human vasoactive intestinal polypeptide receptor 2 (VIP2R) in complex with PACAP27 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: | Xu, Y.N, Feng, W.B, Zhou, Q.T, Liang, A.Y, Li, J, Dai, A.T, Zhao, F.H, Yan, J.H, Chen, C.W, Li, H, Zhao, L.H, Xia, T, Jiang, Y, Xu, H.E, Yang, D.H, Wang, M.W. | | Deposit date: | 2021-12-16 | | Release date: | 2022-05-18 | | Method: | ELECTRON MICROSCOPY (3.42 Å) | | Cite: | A distinctive ligand recognition mechanism by the human vasoactive intestinal polypeptide receptor 2.
Nat Commun, 13, 2022
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7V9L
 | | Cryo-EM structure of the SV1-Gs complex. | | Descriptor: | GHRH receptor splice variant 1,GHRH receptor splice variant 1,GHRH receptor splice variant 1,SV1, 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: | Cong, Z.T, Zhou, F.L, Zhang, C, Zou, X.Y, Zhang, H.B, Wang, Y.Z, Zhou, Q.T, Cai, X.Q, Liu, Q.F, Li, J, Shao, L.J, Mao, C.Y, Wang, X, Wu, J.H, Xia, T, Zhao, L.H, Jiang, H.L, Zhang, Y, Xu, H.E, Cheng, X, Yang, D.H, Wang, M.W. | | Deposit date: | 2021-08-26 | | Release date: | 2022-04-06 | | Last modified: | 2022-05-04 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Constitutive signal bias mediated by the human GHRHR splice variant 1.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7VBH
 | | Cryo-EM structure of the GIPR/GLP-1R/GCGR triagonist peptide 20-bound human GLP-1R-Gs complex | | Descriptor: | Glucagon-like peptide 1 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: | Zhao, F.H, Zhou, Q.T, Cong, Z.T, Hang, K.N, Zou, X.Y, Zhang, C, Chen, Y, Dai, A.T, Liang, A.Y, Ming, Q.Q, Wang, M, Chen, L.N, Xu, P.Y, Chang, R.L, Feng, W.B, Xia, T, Zhang, Y, Wu, B.L, Yang, D.H, Zhao, L.H, Xu, H.E, Wang, M.W. | | Deposit date: | 2021-08-31 | | Release date: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors.
Nat Commun, 13, 2022
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7YK6
 | | Cryo-EM structure of the compound 4-bound human relaxin family peptide receptor 4 (RXFP4)-Gi complex | | Descriptor: | 1-[2-(4-chlorophenyl)ethyl]-3-[(7-ethyl-5-oxidanyl-1H-indol-3-yl)methylideneamino]guanidine, 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: | Chen, Y, Zhou, Q.T, Wang, J, Xu, Y.W, Wang, Y, Yan, J.H, Wang, Y.B, Zhu, Q, Zhao, F.H, Li, C.H, Chen, C.W, Cai, X.Q, Bathgate, R.A.D, Shen, C, Liu, H, Xu, H.E, Yang, D.H, Wang, M.W. | | Deposit date: | 2022-07-21 | | Release date: | 2023-03-01 | | Method: | ELECTRON MICROSCOPY (3.03 Å) | | Cite: | Ligand recognition mechanism of the human relaxin family peptide receptor 4 (RXFP4).
Nat Commun, 14, 2023
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7YJ4
 | | Cryo-EM structure of the INSL5-bound human relaxin family peptidereceptor 4 (RXFP4)-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-2, ... | | Authors: | Chen, Y, Zhou, Q.T, Wang, J, Xu, Y.W, Wang, Y, Yan, J.H, Wang, Y.B, Zhu, Q, Zhao, F.H, Li, C.H, Chen, C.W, Cai, X.Q, Bathgate, R.A.D, Shen, C, Liu, H, Xu, H.E, Yang, D.H, Wang, M.W. | | Deposit date: | 2022-07-19 | | Release date: | 2023-03-01 | | Method: | ELECTRON MICROSCOPY (3.19 Å) | | Cite: | Ligand recognition mechanism of the human relaxin family peptide receptor 4 (RXFP4).
Nat Commun, 14, 2023
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7YK7
 | | Cryo-EM structure of the DC591053-bound human relaxin family peptide receptor 4 (RXFP4)-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-2, ... | | Authors: | Chen, Y, Zhou, Q.T, Wang, J, Xu, Y.W, Wang, Y, Yan, J.H, Wang, Y.B, Zhu, Q, Zhao, F.H, Li, C.H, Chen, C.W, Cai, X.Q, Bathgate, R.A.D, Shen, C, Xu, H.E, Yang, D.H, Liu, H, Wang, M.W. | | Deposit date: | 2022-07-21 | | Release date: | 2023-03-01 | | Method: | ELECTRON MICROSCOPY (2.75 Å) | | Cite: | Ligand recognition mechanism of the human relaxin family peptide receptor 4 (RXFP4).
Nat Commun, 14, 2023
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7V9M
 | | Cryo-EM structure of the GHRH-bound human GHRHR splice variant 1 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: | Cong, Z.T, Zhou, F.L, Zhang, C, Zou, X.Y, Zhang, H.B, Wang, Y.Z, Zhou, Q.T, Cai, X.Q, Liu, Q.F, Li, J, Shao, L.J, Mao, C.Y, Wang, X, Wu, J.H, Xia, T, Zhao, L.H, Jiang, H.L, Zhang, Y, Xu, H.E, Chen, X, Yang, D.H, Wang, M.W. | | Deposit date: | 2021-08-26 | | Release date: | 2021-10-20 | | Last modified: | 2024-06-19 | | Method: | ELECTRON MICROSCOPY (3.29 Å) | | Cite: | Constitutive signal bias mediated by the human GHRHR splice variant 1.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7DWS
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7DW9
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7E4M
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