3O96
| Crystal Structure of Human AKT1 with an Allosteric Inhibitor | Descriptor: | 1-(1-(4-(7-phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one, RAC-alpha serine/threonine-protein kinase | Authors: | Voegtli, W.C, Wu, W.-I, Lord-Ondash, H.A, Dizon, F.P, Vigers, G.P.A, Brandhuber, B.J. | Deposit date: | 2010-08-03 | Release date: | 2010-10-13 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition. Plos One, 5, 2010
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7K7L
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7K7Z
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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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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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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
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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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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
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3V5W
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3UZT
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2VRW
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3UZS
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4D0N
| AKAP13 (AKAP-Lbc) RhoGEF domain in complex with RhoA | Descriptor: | 1,2-ETHANEDIOL, A-KINASE ANCHOR PROTEIN 13, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Abdul Azeez, K.R, Shrestha, L, Krojer, T, Allerston, C, von Delft, F, Bountra, C, Arrowsmith, C, Edwards, A.M, Knapp, S, Klussmann, E, Elkins, J.M. | Deposit date: | 2014-04-29 | Release date: | 2014-05-21 | Last modified: | 2014-11-26 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | The Crystal Structure of the Rhoa : Akap-Lbc Dh-Ph Domain Complex. Biochem.J., 464, 2014
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4KVG
| Crystal structure of RIAM RA-PH domains in complex with GTP bound Rap1 | Descriptor: | 1,2-ETHANEDIOL, Amyloid beta A4 precursor protein-binding family B member 1-interacting protein, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Zhang, H, Chang, Y.E, Brennan, M.L, Wu, J. | Deposit date: | 2013-05-22 | Release date: | 2014-03-05 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.65 Å) | Cite: | The structure of Rap1 in complex with RIAM reveals specificity determinants and recruitment mechanism. J Mol Cell Biol, 6, 2014
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4MK0
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4K81
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4KAX
| Crystal structure of the Grp1 PH domain in complex with Arf6-GTP | Descriptor: | ADP-ribosylation factor 6, CITRIC ACID, Cytohesin-3, ... | Authors: | Lambright, D.G, Malaby, A.W, van den Berg, B. | Deposit date: | 2013-04-23 | Release date: | 2013-08-14 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Structural basis for membrane recruitment and allosteric activation of cytohesin family Arf GTPase exchange factors. Proc.Natl.Acad.Sci.USA, 110, 2013
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4EJN
| Crystal structure of autoinhibited form of AKT1 in complex with N-(4-(5-(3-acetamidophenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-3-yl)benzyl)-3-fluorobenzamide | Descriptor: | 1,2-ETHANEDIOL, 2-BUTANOL, N-(4-{5-[3-(acetylamino)phenyl]-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-3-yl}benzyl)-3-fluorobenzamide, ... | Authors: | Eathiraj, S. | Deposit date: | 2012-04-06 | Release date: | 2012-05-23 | Last modified: | 2013-01-02 | Method: | X-RAY DIFFRACTION (2.19 Å) | Cite: | Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. J.Med.Chem., 55, 2012
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2NZ8
| N-terminal DHPH cassette of Trio in complex with nucleotide-free Rac1 | Descriptor: | ras-related C3 botulinum toxin substrate 1 isoform Rac1, triple functional domain protein | Authors: | Chhatriwala, M.K, Betts, L, Worthylake, D.K, Sondek, J. | Deposit date: | 2006-11-22 | Release date: | 2007-04-10 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | The DH and PH Domains of Trio Coordinately Engage Rho GTPases for their Efficient Activation J.Mol.Biol., 368, 2007
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1YM7
| G Protein-Coupled Receptor Kinase 2 (GRK2) | Descriptor: | Beta-adrenergic receptor kinase 1 | Authors: | Lodowski, D.T, Barnhill, J.F, Pyskadlo, R.M, Ghirlando, R, Sterne-Marr, R, Tesmer, J.J.G. | Deposit date: | 2005-01-20 | Release date: | 2005-07-05 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (4.5 Å) | Cite: | The role of Gbetagamma and domain interfaces in the activation of G protein-coupled receptor kinase 2 Biochemistry, 44, 2005
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2PZ1
| Crystal Structure of Auto-inhibited Asef | Descriptor: | Rho guanine nucleotide exchange factor 4 | Authors: | Betts, L, Sondek, J, Rossman, K.L. | Deposit date: | 2007-05-17 | Release date: | 2007-08-21 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.25 Å) | Cite: | Release of autoinhibition of ASEF by APC leads to CDC42 activation and tumor suppression. Nat.Struct.Mol.Biol., 14, 2007
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3BJI
| Structural Basis of Promiscuous Guanine Nucleotide Exchange by the T-Cell Essential Vav1 | Descriptor: | Proto-oncogene vav, Ras-related C3 botulinum toxin substrate 1 precursor, ZINC ION | Authors: | Chrencik, J.E, Brooun, A, Kuhn, P, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D) | Deposit date: | 2007-12-04 | Release date: | 2008-07-15 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Structural basis of guanine nucleotide exchange mediated by the T-cell essential Vav1. J.Mol.Biol., 380, 2008
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2DX1
| Crystal structure of RhoGEF protein Asef | Descriptor: | Rho guanine nucleotide exchange factor 4 | Authors: | Murayama, K, Kato-Murayama, M, Terada, T, Shirouzu, M, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | Deposit date: | 2006-08-22 | Release date: | 2007-01-02 | Last modified: | 2011-07-13 | Method: | X-RAY DIFFRACTION (2.36 Å) | Cite: | Crystal structure of the rac activator, Asef, reveals its autoinhibitory mechanism J.Biol.Chem., 282, 2007
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