3C4X
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5HE2
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![BU of 5he2 by Molmil](/molmil-images/mine/5he2) | Bovine GRK2 in complex with Gbetagamma subunits and CCG224406 | Descriptor: | (4~{S})-4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.79 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE1
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![BU of 5he1 by Molmil](/molmil-images/mine/5he1) | Human GRK2 in complex with Gbetagamma subunits and CCG224062 | Descriptor: | (4~{S})-4-[4-fluoranyl-3-(isoquinolin-1-ylmethylcarbamoyl)phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (3.15 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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6D8Z
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5HE0
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![BU of 5he0 by Molmil](/molmil-images/mine/5he0) | Bovine GRK2 in complex with Gbetagamma subunits and CCG215022 | Descriptor: | (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-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: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5HE3
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![BU of 5he3 by Molmil](/molmil-images/mine/5he3) | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | Descriptor: | (4~{S})-4-[3-[2-(2,6-dimethylphenyl)ethylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Tesmer, J.J.G. | Deposit date: | 2016-01-05 | Release date: | 2016-05-11 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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5FI1
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![BU of 5fi1 by Molmil](/molmil-images/mine/5fi1) | Crystal Structure of the P-Rex1 DH/PH tandem in complex with Cdc42 | Descriptor: | Cell division control protein 42 homolog, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein,Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-12-22 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.203 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5FI0
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![BU of 5fi0 by Molmil](/molmil-images/mine/5fi0) | Crystal Structure of the P-Rex1 DH/PH tandem in complex with Rac1 | Descriptor: | PHOSPHATE ION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein,Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein, Ras-related C3 botulinum toxin substrate 1 | Authors: | Cash, J.N, Tesmer, J.J.G. | Deposit date: | 2015-12-22 | Release date: | 2016-04-20 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.282 Å) | Cite: | Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3. Structure, 24, 2016
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5UKL
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![BU of 5ukl by Molmil](/molmil-images/mine/5ukl) | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | Descriptor: | 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2017-01-23 | Release date: | 2017-04-05 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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5UKM
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![BU of 5ukm by Molmil](/molmil-images/mine/5ukm) | bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as) | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(1H-pyrazol-5-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Cruz-Rodriguez, O, Tesmer, J.J.G. | Deposit date: | 2017-01-23 | Release date: | 2017-04-12 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (3.03 Å) | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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5UKK
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![BU of 5ukk by Molmil](/molmil-images/mine/5ukk) | Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak) | Descriptor: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-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: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | Deposit date: | 2017-01-23 | Release date: | 2017-04-05 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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3PUI
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![BU of 3pui by Molmil](/molmil-images/mine/3pui) | Cocaine Esterase with mutations G4C, S10C | Descriptor: | CHLORIDE ION, Cocaine esterase, SODIUM ION | Authors: | Nance, M.R, Tesmer, J.J.G. | Deposit date: | 2010-12-04 | Release date: | 2011-09-21 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.53 Å) | Cite: | Subunit stabilization and polyethylene glycolation of cocaine esterase improves in vivo residence time. Mol.Pharmacol., 80, 2011
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3PUH
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![BU of 3puh by Molmil](/molmil-images/mine/3puh) | |
3QC9
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![BU of 3qc9 by Molmil](/molmil-images/mine/3qc9) | |
1APB
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![BU of 1apb by Molmil](/molmil-images/mine/1apb) | |
1BAP
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![BU of 1bap by Molmil](/molmil-images/mine/1bap) | |
3PSC
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![BU of 3psc by Molmil](/molmil-images/mine/3psc) | Bovine GRK2 in complex with Gbetagamma subunits | Descriptor: | Beta-adrenergic receptor kinase 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: | Thal, D.M, Tesmer, J.J. | Deposit date: | 2010-12-01 | Release date: | 2011-06-01 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.67 Å) | Cite: | Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol.Pharmacol., 80, 2011
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3PVU
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![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
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3PVW
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5WG3
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![BU of 5wg3 by Molmil](/molmil-images/mine/5wg3) | Human GRK2 in complex with Gbetagamma subunits and CCG258748 | Descriptor: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(1H-pyrazol-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: | 2017-07-13 | Release date: | 2017-12-27 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.896 Å) | Cite: | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
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6PCV
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![BU of 6pcv by Molmil](/molmil-images/mine/6pcv) | Single Particle Reconstruction of Phosphatidylinositol (3,4,5) trisphosphate-dependent Rac exchanger 1 bound to G protein beta gamma subunits | 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, Phosphatidylinositol (3,4,5) trisphosphate-dependent Rac exchanger 1 | Authors: | Cash, J.N, Cianfrocco, M.A, Tesmer, J.J.G. | Deposit date: | 2019-06-18 | Release date: | 2019-10-23 | Last modified: | 2024-03-20 | Method: | ELECTRON MICROSCOPY (3.2 Å) | Cite: | Cryo-electron microscopy structure and analysis of the P-Rex1-G beta gamma signaling scaffold. Sci Adv, 5, 2019
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6O5G
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![BU of 6o5g by Molmil](/molmil-images/mine/6o5g) | Calmodulin in complex with isomalbrancheamide D | Descriptor: | (5aS,12aS,13aS)-9-bromo-8-chloro-12,12-dimethyl-2,3,11,12,12a,13-hexahydro-1H,5H,6H-5a,13a-(epiminomethano)indolizino[7 ,6-b]carbazol-14-one, CALCIUM ION, Calmodulin-1, ... | Authors: | Beyett, T.S, Fraley, A.E, Tesmer, J.J.G. | Deposit date: | 2019-03-02 | Release date: | 2019-08-07 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.89 Å) | Cite: | Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe. Proc.Natl.Acad.Sci.USA, 116, 2019
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6MTW
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![BU of 6mtw by Molmil](/molmil-images/mine/6mtw) | Lysosomal Phospholipase A2 in complex with Zinc | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHLORIDE ION, Group XV phospholipase A2, ... | Authors: | Bouley, R, Tesmer, J.J.G. | Deposit date: | 2018-10-22 | Release date: | 2019-03-20 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.999 Å) | Cite: | Structural Basis of Lysosomal Phospholipase A2Inhibition by Zn2. Biochemistry, 58, 2019
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7MTB
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![BU of 7mtb by Molmil](/molmil-images/mine/7mtb) | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab6 | Descriptor: | Fab6 heavy chain, Fab6 light chain, RETINAL, ... | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | Deposit date: | 2021-05-13 | Release date: | 2021-07-07 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (4 Å) | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1. Nature, 595, 2021
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7MT8
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![BU of 7mt8 by Molmil](/molmil-images/mine/7mt8) | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin | Descriptor: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | Deposit date: | 2021-05-13 | Release date: | 2021-07-07 | Last modified: | 2021-08-25 | Method: | ELECTRON MICROSCOPY (5.8 Å) | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1. Nature, 595, 2021
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