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PDB: 244 件

5UKL
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Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd)
分子名称: 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, ...
著者Cato, M.C, Homan, K.T, Tesmer, J.J.G.
登録日2017-01-23
公開日2017-04-05
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.15 Å)
主引用文献Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
6HHI
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Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 30b
分子名称: 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
著者Landel, I, Weisner, J, Mueller, M.P, Scheinpflug, R, Rauh, D.
登録日2018-08-28
公開日2019-02-20
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Chem Sci, 10, 2019
2J59
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Crystal structure of the ARF1:ARHGAP21-ArfBD complex
分子名称: 1,2-ETHANEDIOL, 1,4-DIETHYLENE DIOXIDE, ADP-RIBOSYLATION FACTOR 1, ...
著者Menetrey, J, Perderiset, M, Cicolari, J, Dubois, T, El Khatib, N, El Khadali, F, Franco, M, Chavrier, P, Houdusse, A.
登録日2006-09-13
公開日2007-02-20
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Structural Basis for Arf1-Mediated Recruitment of Arhgap21 to Golgi Membranes.
Embo J., 26, 2007
6U7C
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Human GRK2 in complex with Gbetagamma subunits and CCG258747
分子名称: 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, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2019-09-02
公開日2020-04-15
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.44 Å)
主引用文献A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor.
Mol.Pharmacol., 97, 2020
3O96
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Crystal Structure of Human AKT1 with an Allosteric Inhibitor
分子名称: 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
著者Voegtli, W.C, Wu, W.-I, Lord-Ondash, H.A, Dizon, F.P, Vigers, G.P.A, Brandhuber, B.J.
登録日2010-08-03
公開日2010-10-13
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition.
Plos One, 5, 2010
3PSC
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Bovine GRK2 in complex with Gbetagamma subunits
分子名称: 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
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-01
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.67 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
3PVU
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Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101)
分子名称: 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, ...
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.48 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
2VRW
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Critical structural role for the PH and C1 domains of the Vav1 exchange factor
分子名称: PROTO-ONCOGENE VAV, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1, ZINC ION
著者Rapley, J, Tybulewicz, V, Rittinger, K.
登録日2008-04-16
公開日2008-06-17
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (1.85 Å)
主引用文献Crucial Structural Role for the Ph and C1 Domains of the Vav1 Exchange Factor.
Embo Rep., 9, 2008
4KVG
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Crystal structure of RIAM RA-PH domains in complex with GTP bound Rap1
分子名称: 1,2-ETHANEDIOL, Amyloid beta A4 precursor protein-binding family B member 1-interacting protein, GUANOSINE-5'-TRIPHOSPHATE, ...
著者Zhang, H, Chang, Y.E, Brennan, M.L, Wu, J.
登録日2013-05-22
公開日2014-03-05
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (1.65 Å)
主引用文献The structure of Rap1 in complex with RIAM reveals specificity determinants and recruitment mechanism.
J Mol Cell Biol, 6, 2014
4MK0
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Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative
分子名称: 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-1H-isoindol-1-one, Beta-adrenergic receptor kinase 1, GLYCEROL, ...
著者Homan, K.T, Tesmer, J.J.G.
登録日2013-09-04
公開日2014-01-22
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog.
Mol.Pharmacol., 85, 2014
4KAX
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Crystal structure of the Grp1 PH domain in complex with Arf6-GTP
分子名称: ADP-ribosylation factor 6, CITRIC ACID, Cytohesin-3, ...
著者Lambright, D.G, Malaby, A.W, van den Berg, B.
登録日2013-04-23
公開日2013-08-14
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (1.85 Å)
主引用文献Structural basis for membrane recruitment and allosteric activation of cytohesin family Arf GTPase exchange factors.
Proc.Natl.Acad.Sci.USA, 110, 2013
3PVW
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Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD103A)
分子名称: 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, ...
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.49 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
4K81
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Crystal structure of the Grb14 RA and PH domains in complex with GTP-loaded H-Ras
分子名称: GLYCEROL, GTPase HRas, GUANOSINE-5'-TRIPHOSPHATE, ...
著者Qamra, R, Hubbard, S.R.
登録日2013-04-17
公開日2013-09-04
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structural basis for the interaction of the adaptor protein grb14 with activated ras.
Plos One, 8, 2013
3UZT
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BU of 3uzt by Molmil
Structure of the C13.18 RNA Aptamer in Complex with G Protein-Coupled Receptor Kinase 2
分子名称: Beta-adrenergic receptor kinase 1, C13.18 RNA Aptamer, MAGNESIUM ION
著者Tesmer, J.J.G, Tesmer, V.M.
登録日2011-12-07
公開日2012-07-11
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (3.51 Å)
主引用文献Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.
Structure, 20, 2012
2NZ8
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N-terminal DHPH cassette of Trio in complex with nucleotide-free Rac1
分子名称: ras-related C3 botulinum toxin substrate 1 isoform Rac1, triple functional domain protein
著者Chhatriwala, M.K, Betts, L, Worthylake, D.K, Sondek, J.
登録日2006-11-22
公開日2007-04-10
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献The DH and PH Domains of Trio Coordinately Engage Rho GTPases for their Efficient Activation
J.Mol.Biol., 368, 2007
1YM7
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BU of 1ym7 by Molmil
G Protein-Coupled Receptor Kinase 2 (GRK2)
分子名称: Beta-adrenergic receptor kinase 1
著者Lodowski, D.T, Barnhill, J.F, Pyskadlo, R.M, Ghirlando, R, Sterne-Marr, R, Tesmer, J.J.G.
登録日2005-01-20
公開日2005-07-05
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (4.5 Å)
主引用文献The role of Gbetagamma and domain interfaces in the activation of G protein-coupled receptor kinase 2
Biochemistry, 44, 2005
3UZS
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Structure of the C13.28 RNA Aptamer Bound to the G Protein-Coupled Receptor Kinase 2-Heterotrimeric G Protein Beta 1 and Gamma 2 Subunit Complex
分子名称: Beta-adrenergic receptor kinase 1, C13.28 RNA Aptamer, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G, Tesmer, V.M.
登録日2011-12-07
公開日2012-07-11
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (4.52 Å)
主引用文献Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.
Structure, 20, 2012
3BJI
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Structural Basis of Promiscuous Guanine Nucleotide Exchange by the T-Cell Essential Vav1
分子名称: Proto-oncogene vav, Ras-related C3 botulinum toxin substrate 1 precursor, ZINC ION
著者Chrencik, J.E, Brooun, A, Kuhn, P, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D)
登録日2007-12-04
公開日2008-07-15
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Structural basis of guanine nucleotide exchange mediated by the T-cell essential Vav1.
J.Mol.Biol., 380, 2008
2BCJ
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Crystal Structure of G Protein-Coupled Receptor Kinase 2 in Complex with Galpha-q and Gbetagamma Subunits
分子名称: G-protein-coupled receptor kinase 2, GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G.
登録日2005-10-19
公開日2005-12-20
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (3.061 Å)
主引用文献Snapshot of Activated G Proteins at the Membrane: The Gq-GRK2-G Complex
Science, 310, 2005

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