3V5W
 
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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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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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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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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
 | | 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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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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2I1K
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2I1J
 | | Moesin from Spodoptera frugiperda at 2.1 angstroms resolution | | Descriptor: | CHLORIDE ION, GLYCEROL, Moesin, ... | | Authors: | Li, Q, Nance, M.R, Tesmer, J.J.G. | | Deposit date: | 2006-08-14 | | Release date: | 2006-12-19 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Self-masking in an Intact ERM-merlin Protein: An Active Role for the Central alpha-Helical Domain.
J.Mol.Biol., 365, 2007
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4X96
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4X95
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4X97
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4BEZ
 | | Night blindness causing G90D rhodopsin in the active conformation | | Descriptor: | ACETATE ION, PALMITIC ACID, RHODOPSIN, ... | | Authors: | Singhal, A, Ostermaier, M.K, Vishnivetskiy, S.A, Panneels, V, Homan, K.T, Tesmer, J.J.G, Veprintsev, D, Deupi, X, Gurevich, V.V, Schertler, G.F.X, Standfuss, J. | | Deposit date: | 2013-03-12 | | Release date: | 2013-04-24 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Insights Into Congenital Stationary Night Blindness Based on the Structure of G90D Rhodopsin.
Embo Rep., 14, 2013
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4BEY
 | | Night blindness causing G90D rhodopsin in complex with GaCT2 peptide | | Descriptor: | ACETATE ION, Guanine nucleotide-binding protein G(t) subunit alpha-1, PALMITIC ACID, ... | | Authors: | Singhal, A, Ostermaier, M.K, Vishnivetskiy, S.A, Panneels, V, Homan, K.T, Tesmer, J.J.G, Veprintsev, D, Deupi, X, Gurevich, V.V, Schertler, G.F.X, Standfuss, J. | | Deposit date: | 2013-03-12 | | Release date: | 2013-05-08 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Insights Into Congenital Stationary Night Blindness Based on the Structure of G90D Rhodopsin.
Embo Rep., 14, 2013
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5D3W
 | | Crystal Structure of the P-Rex1 PH domain with Sulfate Bound | | Descriptor: | Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein, SULFATE ION | | Authors: | Cash, J.N, Tesmer, J.J.G. | | Deposit date: | 2015-08-06 | | Release date: | 2016-04-20 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.852 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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5D3Y
 | | Crystal Structure of the P-Rex1 PH domain with Inositol-(1,3,4,5)-Tetrakisphosphate Bound | | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | Authors: | Cash, J.N, Tesmer, J.J.G. | | Deposit date: | 2015-08-06 | | Release date: | 2016-04-20 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.95 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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5D3V
 | | Crystal Structure of the P-Rex1 PH domain with Citrate Bound | | Descriptor: | CITRATE ANION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | Authors: | Cash, J.N, Tesmer, J.J.G. | | Deposit date: | 2015-08-06 | | Release date: | 2016-04-20 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.852 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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5D3X
 | | Crystal Structure of the P-Rex1 PH domain with Inositol-(1,3,4,5)-Tetrakisphosphate Bound | | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | Authors: | Cash, J.N, Tesmer, J.J.G. | | Deposit date: | 2015-08-06 | | Release date: | 2016-04-20 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.69 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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5D27
 | | Crystal Structure of the P-Rex1 PH domain | | Descriptor: | NICKEL (II) ION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | Authors: | Cash, J.N, Tesmer, J.J.G. | | Deposit date: | 2015-08-05 | | Release date: | 2016-04-20 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.92 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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1ZCA
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5DO9
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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
 | | 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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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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1ZCB
 | | Crystal structure of G alpha 13 in complex with GDP | | Descriptor: | G alpha i/13, GUANOSINE-5'-DIPHOSPHATE | | Authors: | Nance, M.R, Tesmer, J.J.G. | | Deposit date: | 2005-04-11 | | Release date: | 2005-11-15 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A new approach to producing functional G alpha subunits yields the activated and deactivated structures of G alpha(12/13) proteins.
Biochemistry, 45, 2006
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