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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6HHI
 | | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 30b | | Descriptor: | RAC-alpha serine/threonine-protein kinase, ~{N}-[1-[[4-(5-oxidanylidene-3-phenyl-6~{H}-1,6-naphthyridin-2-yl)phenyl]methyl]piperidin-4-yl]-3-(propanoylamino)benzamide | | Authors: | Landel, I, Weisner, J, Mueller, M.P, Scheinpflug, R, Rauh, D. | | Deposit date: | 2018-08-28 | | Release date: | 2019-02-20 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Chem Sci, 10, 2019
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2J59
 | | Crystal structure of the ARF1:ARHGAP21-ArfBD complex | | Descriptor: | 1,2-ETHANEDIOL, 1,4-DIETHYLENE DIOXIDE, ADP-RIBOSYLATION FACTOR 1, ... | | Authors: | Menetrey, J, Perderiset, M, Cicolari, J, Dubois, T, El Khatib, N, El Khadali, F, Franco, M, Chavrier, P, Houdusse, A. | | Deposit date: | 2006-09-13 | | Release date: | 2007-02-20 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structural Basis for Arf1-Mediated Recruitment of Arhgap21 to Golgi Membranes.
Embo J., 26, 2007
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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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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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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
 | | 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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2VRW
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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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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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3PVW
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4K81
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3UZT
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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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3UZS
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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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2BCJ
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