3V5W
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3v5w by Molmil](/molmil-images/mine/3v5w) | |
1GP2
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 1gp2 by Molmil](/molmil-images/mine/1gp2) | |
5WG4
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5wg4 by Molmil](/molmil-images/mine/5wg4) | Human GRK2 in complex with Gbetagamma subunits and CCG257284 | Descriptor: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-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: | Bouley, R, Tesmer, J.J.G. | Deposit date: | 2017-07-13 | Release date: | 2017-12-27 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.31 Å) | Cite: | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
|
|
4MK0
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4mk0 by Molmil](/molmil-images/mine/4mk0) | |
1GG2
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 1gg2 by Molmil](/molmil-images/mine/1gg2) | |
6U7C
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6u7c by Molmil](/molmil-images/mine/6u7c) | Human GRK2 in complex with Gbetagamma subunits and CCG258747 | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-3-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Bouley, R, Tesmer, J.J.G. | Deposit date: | 2019-09-02 | Release date: | 2020-04-15 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.44 Å) | Cite: | A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor. Mol.Pharmacol., 97, 2020
|
|
8JIS
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8jis by Molmil](/molmil-images/mine/8jis) | Cryo-EM structure of the GLP-1R/GCGR dual agonist peptide15-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: | Yang, L, Zhou, Q.T, Dai, A.T, Zhao, F.H, Chang, R.L, Ying, T.L, Wu, B.L, Yang, D.H, Wang, M.W, Cong, Z.T. | Deposit date: | 2023-05-27 | Release date: | 2023-11-08 | Method: | ELECTRON MICROSCOPY (2.46 Å) | Cite: | Structural analysis of the dual agonism at GLP-1R and GCGR. Proc.Natl.Acad.Sci.USA, 120, 2023
|
|
8YKV
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8ykv by Molmil](/molmil-images/mine/8ykv) | Cryo-EM structure of succinate receptor SUCR1 bound to compound 31 | Descriptor: | (2~{S})-2-[[6-[4-(trifluoromethyloxy)phenyl]pyridin-2-yl]carbonylamino]butanedioic acid, Antibody fragment ScFv16, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Li, C, Liu, H, Li, J, Zhu, H, Fu, W, Xu, H.E. | Deposit date: | 2024-03-05 | Release date: | 2024-05-29 | Method: | ELECTRON MICROSCOPY (2.48 Å) | Cite: | Cryo-EM structure of succinate receptor SUCR1 bound to compound 31 To Be Published
|
|
3PVU
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3pvu by Molmil](/molmil-images/mine/3pvu) | Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101) | Descriptor: | 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Thal, D.M, Tesmer, J.J. | Deposit date: | 2010-12-07 | Release date: | 2011-06-01 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.48 Å) | Cite: | Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol.Pharmacol., 80, 2011
|
|
3PVW
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3pvw by Molmil](/molmil-images/mine/3pvw) | |
7DUQ
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7duq by Molmil](/molmil-images/mine/7duq) | Cryo-EM structure of the compound 2 and GLP-1-bound human GLP-1 receptor-Gs complex | Descriptor: | CHOLESTEROL, Glucagon-like peptide 1, Glucagon-like peptide 1 receptor, ... | Authors: | Cong, Z, Chen, L, Ma, H, Zhou, Q, Zou, X, Ye, C, Dai, A, Liu, Q, Huang, W, Sun, X, Wang, X, Xu, P, Zhao, L, Xia, T, Zhong, W, Yang, D, Xu, H.E, Zhang, Y, Wang, M. | Deposit date: | 2021-01-11 | Release date: | 2021-07-14 | Method: | ELECTRON MICROSCOPY (2.5 Å) | Cite: | Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor. Nat Commun, 12, 2021
|
|
8DCS
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8dcs by Molmil](/molmil-images/mine/8dcs) | Cryo-EM structure of cyanopindolol-bound beta1-adrenergic receptor in complex with heterotrimeric Gs-protein | Descriptor: | 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile, Endolysin,Endolysin,Beta-1 adrenergic receptor chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Su, M, Paknejad, N, Hite, R.K, Huang, X.Y. | Deposit date: | 2022-06-17 | Release date: | 2022-07-27 | Method: | ELECTRON MICROSCOPY (2.5 Å) | Cite: | Structures of beta 1 -adrenergic receptor in complex with Gs and ligands of different efficacies. Nat Commun, 13, 2022
|
|
7EVM
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7evm by Molmil](/molmil-images/mine/7evm) | Cryo-EM structure of the compound 2-bound human GLP-1 receptor-Gs complex | Descriptor: | CHOLESTEROL, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cong, Z, Chen, L, Ma, H, Zhou, Q, Zou, X, Ye, C, Dai, A, Liu, Q, Huang, W, Sun, X, Wang, X, Xu, P, Zhao, L, Xia, T, Zhong, W, Yang, D, Xu, H.E, Zhang, Y, Wang, M. | Deposit date: | 2021-05-21 | Release date: | 2021-08-11 | Method: | ELECTRON MICROSCOPY (2.5 Å) | Cite: | Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor. Nat Commun, 12, 2021
|
|
1OMW
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 1omw by Molmil](/molmil-images/mine/1omw) | Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits | Descriptor: | G-protein coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1 | Authors: | Lodowski, D.T, Pitcher, J.A, Capel, W.D, Lefkowitz, R.J, Tesmer, J.J.G. | Deposit date: | 2003-02-26 | Release date: | 2003-06-03 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Keeping G proteins at Bay: A Complex Between G Protein-Coupled Receptor Kinase 2 and G-Beta-Gamma Science, 300, 2003
|
|
8WG7
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8wg7 by Molmil](/molmil-images/mine/8wg7) | Cryo-EM structures of peptide free and Gs-coupled GLP-1R | 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: | Cong, Z.T, Zhao, F.H, Li, Y, Luo, G, Zhou, Q.T, Yang, D.H, Wang, M.W. | Deposit date: | 2023-09-20 | Release date: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (2.54 Å) | Cite: | Molecular features of the ligand-free GLP-1R, GCGR and GIPR in complex with G s proteins. Cell Discov, 10, 2024
|
|
4PNK
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4pnk by Molmil](/molmil-images/mine/4pnk) | G protein-coupled receptor kinase 2 in complex with GSK180736A | Descriptor: | (4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G. | Deposit date: | 2014-05-23 | Release date: | 2014-10-08 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors. Acs Chem.Biol., 10, 2015
|
|
8JIR
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8jir by Molmil](/molmil-images/mine/8jir) | Cryo-EM structure of the GLP-1R/GCGR dual agonist SAR425899-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: | Yang, L, Zhou, Q.T, Dai, A.T, Zhao, F.H, Chang, R.L, Ying, T.L, Wu, B.L, Yang, D.H, Wang, M.W, Cong, Z.T. | Deposit date: | 2023-05-27 | Release date: | 2023-09-06 | Method: | ELECTRON MICROSCOPY (2.57 Å) | Cite: | Structural analysis of the dual agonism at GLP-1R and GCGR. Proc.Natl.Acad.Sci.USA, 120, 2023
|
|
7PIU
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7piu by Molmil](/molmil-images/mine/7piu) | Cryo-EM structure of the agonist setmelanotide bound to the active melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein at 2.6 A resolution. | Descriptor: | CALCIUM ION, Camelid antibody fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P. | Deposit date: | 2021-08-23 | Release date: | 2021-11-17 | Method: | ELECTRON MICROSCOPY (2.58 Å) | Cite: | Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide. Cell Res., 31, 2021
|
|
8IOD
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8iod by Molmil](/molmil-images/mine/8iod) | Cryo-EM structure of the PG-901-bound human melanocortin receptor 5 (MC5R)-Gs 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,HiBiT, ... | Authors: | Feng, W.B, Zhou, Q.T, Chen, X.Y, Dai, A.T, Cai, X.Q, Liu, X, Zhao, F.H, Chen, Y, Ye, C.Y, Xu, Y.N, Cong, Z.T, Li, H, Lin, S, Yang, D.H, Wang, M.W. | Deposit date: | 2023-03-10 | Release date: | 2023-09-20 | Last modified: | 2023-11-15 | Method: | ELECTRON MICROSCOPY (2.59 Å) | Cite: | Structural insights into ligand recognition and subtype selectivity of the human melanocortin-3 and melanocortin-5 receptors. Cell Discov, 9, 2023
|
|
7V9L
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7v9l by Molmil](/molmil-images/mine/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
|
|
7PWD
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7pwd by Molmil](/molmil-images/mine/7pwd) | Structure of an inhibited GRK2-G-beta and G-gamma complex | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | Deposit date: | 2021-10-06 | Release date: | 2021-10-20 | Last modified: | 2024-06-19 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors Monatsh Chem, 2022
|
|
7WQ4
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7wq4 by Molmil](/molmil-images/mine/7wq4) | Galanin-bound galanin receptor 2 in complex with Gq | Descriptor: | CHOLESTEROL, Engineered Guanine nucleotide-binding protein G(q) subunit alpha, Galanin, ... | Authors: | Duan, J, Shen, D.D, Xu, H.E, Zhang, Y, Jiang, Y. | Deposit date: | 2022-01-24 | Release date: | 2022-04-20 | Last modified: | 2022-10-19 | Method: | ELECTRON MICROSCOPY (2.6 Å) | Cite: | Molecular basis for allosteric agonism and G protein subtype selectivity of galanin receptors Nat Commun, 13, 2022
|
|
7DW9
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7dw9 by Molmil](/molmil-images/mine/7dw9) | |
7TD4
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7td4 by Molmil](/molmil-images/mine/7td4) | Sphingosine-1-phosphate receptor 1-Gi complex bound to Siponimod | Descriptor: | 1-[[4-[(~{E})-~{N}-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-~{C}-methyl-carbonimidoyl]-2-ethyl-phenyl]methyl]azetidine-3-carboxylic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Liu, S, Paknejad, N, Zhu, L, Kihara, Y, Ray, D, Chun, J, Liu, W, Hite, R.K, Huang, X.Y. | Deposit date: | 2021-12-30 | Release date: | 2022-02-09 | Last modified: | 2022-02-23 | Method: | ELECTRON MICROSCOPY (2.6 Å) | Cite: | Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate. Nat Commun, 13, 2022
|
|
7JJO
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7jjo by Molmil](/molmil-images/mine/7jjo) | Structural Basis of the Activation of Heterotrimeric Gs-protein by Isoproterenol-bound Beta1-Adrenergic Receptor | Descriptor: | Beta1-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: | Su, M, Zhu, L, Zhang, Y, Paknejad, N, Dey, R, Huang, J, Lee, M.Y, Williams, D, Jordan, K.D, Eng, E.T, Ernst, O.P, Meyerson, J.R, Hite, R.K, Walz, T, Liu, W, Huang, X.Y. | Deposit date: | 2020-07-27 | Release date: | 2020-09-02 | Last modified: | 2020-10-14 | Method: | ELECTRON MICROSCOPY (2.6 Å) | Cite: | Structural Basis of the Activation of Heterotrimeric Gs-Protein by Isoproterenol-Bound beta 1 -Adrenergic Receptor. Mol.Cell, 80, 2020
|
|