5HE0
 
 | | Bovine GRK2 in complex with Gbetagamma subunits and CCG215022 | | 分子名称: | (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, ... | | 著者 | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | | 登録日 | 2016-01-05 | | 公開日 | 2016-05-11 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.56 Å) | | 主引用文献 | 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
 | | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | | 分子名称: | (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, ... | | 著者 | Cato, M.C, Tesmer, J.J.G. | | 登録日 | 2016-01-05 | | 公開日 | 2016-05-11 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.74 Å) | | 主引用文献 | 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 | | 分子名称: | (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, ... | | 著者 | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | | 登録日 | 2016-01-05 | | 公開日 | 2016-05-11 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.79 Å) | | 主引用文献 | 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 | | 分子名称: | (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, ... | | 著者 | Cato, M.C, Tesmer, J.J.G. | | 登録日 | 2016-01-05 | | 公開日 | 2016-05-11 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (3.15 Å) | | 主引用文献 | 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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7NH4
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7NH5
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3O96
 | | 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 | 2024-10-16 | | 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
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6U7C
 | | 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
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3BJI
 | | 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
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3PSC
 | | 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
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3PVU
 | | 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
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3PVW
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3CIK
 | | Human 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 | Tesmer, J.J.G, Lodowski, D.T. | | 登録日 | 2008-03-11 | | 公開日 | 2009-02-17 | | 最終更新日 | 2012-03-07 | | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | | 主引用文献 | Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
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2J59
 | | 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
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2NZ8
 | | 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
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2VRW
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4KAX
 | | 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
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3V5W
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3UZT
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3UZS
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8UW9
 | | Structure of AKT1(E17K) with compound 4 | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, N-({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)-2-(2-fluoro-4-formyl-3-hydroxyphenyl)acetamide, ... | | 著者 | Craven, G.B, Taunton, J. | | 登録日 | 2023-11-06 | | 公開日 | 2024-09-04 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation
To Be Published
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8UW2
 | | Structure of AKT1(E17K) with compound 3 (zinc-free) | | 分子名称: | 1,2-ETHANEDIOL, 4-{2-[({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)amino]ethyl}-2-hydroxybenzaldehyde, NB41, ... | | 著者 | Craven, G.B, Taunton, J. | | 登録日 | 2023-11-05 | | 公開日 | 2024-09-04 | | 最終更新日 | 2024-10-16 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation
To Be Published
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8UVY
 | | Structure of AKT1(E17K) with compound 3 | | 分子名称: | 1,2-ETHANEDIOL, 4-{2-[({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)amino]ethyl}-2-hydroxybenzaldehyde, NB41, ... | | 著者 | Craven, G.B, Taunton, J. | | 登録日 | 2023-11-05 | | 公開日 | 2024-09-04 | | 実験手法 | X-RAY DIFFRACTION (2.11 Å) | | 主引用文献 | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation
To Be Published
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8UW7
 | | Structure of AKT1(WT) with compound 3 | | 分子名称: | 1,2-ETHANEDIOL, 4-{2-[({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)amino]ethyl}-2-hydroxybenzaldehyde, NB41, ... | | 著者 | Craven, G.B, Taunton, J. | | 登録日 | 2023-11-06 | | 公開日 | 2024-09-04 | | 実験手法 | X-RAY DIFFRACTION (1.972 Å) | | 主引用文献 | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation
To Be Published
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