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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3KY9
 | | Autoinhibited Vav1 | | 分子名称: | Proto-oncogene vav, ZINC ION | | 著者 | Tomchick, D.R, Rosen, M.K, Machius, M, Yu, B. | | 登録日 | 2009-12-04 | | 公開日 | 2010-02-23 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.731 Å) | | 主引用文献 | Structural and Energetic Mechanisms of Cooperative Autoinhibition and Activation of Vav1
Cell(Cambridge,Mass.), 140, 2010
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3KRX
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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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7CSR
 | | Structure of Ephexin4 R676L | | 分子名称: | Rho guanine nucleotide exchange factor 16 | | 著者 | Zhang, M, Lin, L, Wang, C, Zhu, J. | | 登録日 | 2020-08-17 | | 公開日 | 2021-02-24 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Double inhibition and activation mechanisms of Ephexin family RhoGEFs.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7CSO
 | | Structure of Ephexin4 DH-PH-SH3 | | 分子名称: | Rho guanine nucleotide exchange factor 16, SULFATE ION | | 著者 | Zhang, M, Lin, L, Wang, C, Zhu, J. | | 登録日 | 2020-08-15 | | 公開日 | 2021-02-24 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (2.39 Å) | | 主引用文献 | Double inhibition and activation mechanisms of Ephexin family RhoGEFs.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7CSP
 | | Structure of Ephexin4 IDPSH | | 分子名称: | Rho guanine nucleotide exchange factor 16 | | 著者 | Zhang, M, Lin, L, Wang, C, Zhu, J. | | 登録日 | 2020-08-15 | | 公開日 | 2021-02-24 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Double inhibition and activation mechanisms of Ephexin family RhoGEFs.
Proc.Natl.Acad.Sci.USA, 118, 2021
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8JPC
 | | cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 2 | | 分子名称: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, Beta-adrenergic receptor kinase 1, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | | 登録日 | 2023-06-11 | | 公開日 | 2023-08-09 | | 最終更新日 | 2023-08-30 | | 実験手法 | ELECTRON MICROSCOPY (3.07 Å) | | 主引用文献 | GPCR activation and GRK2 assembly by a biased intracellular agonist.
Nature, 620, 2023
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8JPD
 | | Focused refinement structure of GRK2 in NTSR1-GRK2-Galpha(q) complexes | | 分子名称: | Beta-adrenergic receptor kinase 1, STAUROSPORINE | | 著者 | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | | 登録日 | 2023-06-11 | | 公開日 | 2023-08-09 | | 最終更新日 | 2023-08-30 | | 実験手法 | ELECTRON MICROSCOPY (2.81 Å) | | 主引用文献 | GPCR activation and GRK2 assembly by a biased intracellular agonist.
Nature, 620, 2023
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8JPB
 | | cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 1 | | 分子名称: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, Beta-adrenergic receptor kinase 1, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | | 登録日 | 2023-06-11 | | 公開日 | 2023-08-09 | | 最終更新日 | 2023-08-30 | | 実験手法 | ELECTRON MICROSCOPY (3.07 Å) | | 主引用文献 | GPCR activation and GRK2 assembly by a biased intracellular agonist.
Nature, 620, 2023
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4D0N
 | | AKAP13 (AKAP-Lbc) RhoGEF domain in complex with RhoA | | 分子名称: | 1,2-ETHANEDIOL, A-KINASE ANCHOR PROTEIN 13, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | 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. | | 登録日 | 2014-04-29 | | 公開日 | 2014-05-21 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | The Crystal Structure of the Rhoa : Akap-Lbc Dh-Ph Domain Complex.
Biochem.J., 464, 2014
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6HHI
 | | 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
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6HHF
 | | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor Borussertib | | 分子名称: | Borussertib, RAC-alpha serine/threonine-protein kinase | | 著者 | Landel, I, Weisner, J, Mueller, M.P, Scheinpflug, R, Rauh, D. | | 登録日 | 2018-08-28 | | 公開日 | 2019-03-20 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Preclinical Efficacy of Covalent-Allosteric AKT Inhibitor Borussertib in Combination with Trametinib inKRAS-Mutant Pancreatic and Colorectal Cancer.
Cancer Res., 79, 2019
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6NEW
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7APJ
 | | Structure of autoinhibited Akt1 reveals mechanism of PIP3-mediated activation | | 分子名称: | NB41, RAC-alpha serine/threonine-protein kinase,Non-specific serine/threonine protein kinase,RAC-alpha serine/threonine-protein kinase | | 著者 | Truebestein, L, Hornegger, H, Leonard, T.A. | | 登録日 | 2020-10-16 | | 公開日 | 2021-08-25 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | Structure of autoinhibited Akt1 reveals mechanism of PIP 3 -mediated activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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6NF1
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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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6HHJ
 | | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 24b | | 分子名称: | RAC-alpha serine/threonine-protein kinase, ~{N}-[1-methyl-2-oxidanylidene-3-[1-[[4-(5-oxidanylidene-3-phenyl-6~{H}-1,6-naphthyridin-2-yl)phenyl]methyl]piperidin-4-yl]benzimidazol-5-yl]propanamide | | 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 (2.3 Å) | | 主引用文献 | Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Chem Sci, 10, 2019
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6HHH
 | | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 31 | | 分子名称: | RAC-alpha serine/threonine-protein kinase, ~{N}-[4-[4-[[4-(5-oxidanylidene-3-phenyl-6~{H}-1,6-naphthyridin-2-yl)phenyl]methyl]piperazin-1-yl]phenyl]propanamide | | 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
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6NFA
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8Q61
 | | Co-crystal structure of human AKT2 with compound 3 | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 6-[4-(1-azanyl-3-methyl-3-oxidanyl-cyclobutyl)phenyl]-7-phenyl-1-propyl-pyrido[2,3-b][1,4]oxazin-2-one, GLYCEROL, ... | | 著者 | Harrison, T, Barker, O. | | 登録日 | 2023-08-10 | | 公開日 | 2023-08-16 | | 実験手法 | X-RAY DIFFRACTION (2.32 Å) | | 主引用文献 | Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development.
Sci Rep, 12, 2022
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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 | 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
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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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