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1GZK
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Molecular mechanism for the regulation of protein kinase B/Akt by hydrophobic motif phosphorylation
分子名称: RAC-BETA SERINE/THREONINE PROTEIN KINASE
著者Barford, D, Yang, J, Hemmings, B.A.
登録日2002-05-23
公開日2003-05-22
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Molecular Mechanism for the Regulation of Protein Kinase B/Akt by Hydrophobic Motif Phosphorylation
Mol.Cell, 9, 2002
1GZN
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Structure of PKB kinase domain
分子名称: RAC-BETA SERINE/THREONINE PROTEIN KINASE
著者Barford, D, Yang, J, Hemmings, B.A.
登録日2002-05-24
公開日2003-05-22
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Molecular Mechanism for the Regulation of Protein Kinase B/Akt by Hydrophobic Motif Phosphorylation
Mol.Cell, 9, 2002
1GZO
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Structure of protein kinase B unphosphorylated
分子名称: RAC-BETA SERINE/THREONINE PROTEIN KINASE
著者Barford, D, Yang, J, Hemmings, B.A.
登録日2002-05-24
公開日2003-05-22
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.75 Å)
主引用文献Molecular Mechanism for the Regulation of Protein Kinase B/Akt by Hydrophobic Motif Phosphorylation
Mol.Cell, 9, 2002
1MRV
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crystal structure of an inactive Akt2 kinase domain
分子名称: RAC-beta serine/threonine kinase
著者Huang, X, Begley, M, Morgenstern, K.A, Gu, Y, Rose, P, Zhao, H, Zhu, X.
登録日2002-09-18
公開日2003-09-23
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Crystal structure of an inactive akt2 kinase domain
Structure, 11, 2003
1MRY
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crystal structure of an inactive akt2 kinase domain
分子名称: RAC-beta serine/threonine kinase
著者Huang, X, Begley, M, Morgenstern, K.A, Gu, Y, Rose, P, Zhao, H, Zhu, X.
登録日2002-09-18
公開日2003-09-23
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Crystal structure of an inactive akt2 kinase domain
Structure, 11, 2003
1O6K
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Structure of activated form of PKB kinase domain S474D with GSK3 peptide and AMP-PNP
分子名称: GLYCOGEN SYNTHASE KINASE-3 BETA, MANGANESE (II) ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ...
著者Yang, J, Cron, P, Good, V.M, Thompson, V, Hemmings, B.A, Barford, D.
登録日2002-10-08
公開日2002-11-19
最終更新日2024-10-16
実験手法X-RAY DIFFRACTION (1.7 Å)
主引用文献Crystal Structure of an Activated Akt/Protein Kinase B Ternary Complex with Gsk-3 Peptide and AMP-Pnp
Nat.Struct.Biol., 9, 2002
1O6L
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Crystal structure of an activated Akt/protein kinase B (PKB-PIF chimera) ternary complex with AMP-PNP and GSK3 peptide
分子名称: GLYCOGEN SYNTHASE KINASE-3 BETA, MANGANESE (II) ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ...
著者Yang, J, Cron, P, Good, V.M, Thompson, V, Hemmings, B.A, Barford, D.
登録日2002-10-08
公開日2002-11-19
最終更新日2024-05-01
実験手法X-RAY DIFFRACTION (1.6 Å)
主引用文献Crystal Structure of an Activated Akt/Protein Kinase B Ternary Complex with Gsk-3 Peptide and AMP-Pnp
Nat.Struct.Biol., 9, 2002
1XJD
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Crystal Structure of PKC-theta complexed with Staurosporine at 2A resolution
分子名称: Protein kinase C, theta type, STAUROSPORINE
著者Xu, Z.B.
登録日2004-09-23
公開日2004-10-19
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Catalytic domain crystal structure of protein kinase C-theta (PKCtheta)
J.Biol.Chem., 279, 2004
1ZRZ
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Crystal Structure of the Catalytic Domain of Atypical Protein Kinase C-iota
分子名称: 3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE, Protein kinase C, iota
著者Messerschmidt, A, Macieira, S, Velarde, M, Baedeker, M, Benda, C, Jestel, A, Brandstetter, H, Neuefeind, T, Blaesse, M, Structural Proteomics in Europe (SPINE)
登録日2005-05-23
公開日2005-09-13
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献Crystal Structure of the Catalytic Domain of Human Atypical Protein Kinase C-iota Reveals Interaction Mode of Phosphorylation Site in Turn Motif
J.Mol.Biol., 352, 2005
2I0E
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BU of 2i0e by Molmil
Structure of catalytic domain of human protein kinase C beta II complexed with a bisindolylmaleimide inhibitor
分子名称: 3-{1-[3-(DIMETHYLAMINO)PROPYL]-2-METHYL-1H-INDOL-3-YL}-4-(2-METHYL-1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE, Protein Kinase C-beta II
著者Grodsky, N.B, Love, R.L.
登録日2006-08-10
公開日2006-11-14
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Structure of the Catalytic Domain of Human Protein Kinase C beta II Complexed with a Bisindolylmaleimide Inhibitor
Biochemistry, 45, 2006
2JDO
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STRUCTURE OF PKB-BETA (AKT2) COMPLEXED WITH ISOQUINOLINE-5-SULFONIC ACID (2-(2-(4-CHLOROBENZYLOXY) ETHYLAMINO)ETHYL)AMIDE
分子名称: 1,2-ETHANEDIOL, GLYCOGEN SYNTHASE KINASE-3 BETA, ISOQUINOLINE-5-SULFONIC ACID (2-(2-(4-CHLOROBENZYLOXY)ETHYLAMINO)ETHYL)AMIDE, ...
著者Davies, T.G, Verdonk, M.L, Graham, B, Saalau-Bethell, S, Hamlett, C.C.F, Mchardy, T, Collins, I, Garrett, M.D, Workman, P, Woodhead, S.J, Jhoti, H, Barford, D.
登録日2007-01-11
公開日2007-02-13
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献A Structural Comparison of Inhibitor Binding to Pkb, Pka and Pka-Pkb Chimera
J.Mol.Biol., 367, 2007
2JDR
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STRUCTURE OF PKB-BETA (AKT2) COMPLEXED WITH THE INHIBITOR A-443654
分子名称: (2S)-1-(1H-INDOL-3-YL)-3-{[5-(3-METHYL-1H-INDAZOL-5-YL)PYRIDIN-3-YL]OXY}PROPAN-2-AMINE, GLYCOGEN SYNTHASE KINASE-3 BETA, RAC-BETA SERINE/THREONINE-PROTEIN KINASE
著者Davies, T.G, Verdonk, M.L, Graham, B, Saalau-Bethell, S, Hamlett, C.C.F, McHardy, T, Collins, I, Garrett, M.D, Workman, P, Woodhead, S.J, Jhoti, H, Barford, D.
登録日2007-01-12
公開日2007-02-13
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献A Structural Comparison of Inhibitor Binding to Pkb, Pka and Pka-Pkb Chimera
J.Mol.Biol., 367, 2007
2JED
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The crystal structure of the kinase domain of the protein kinase C theta in complex with NVP-XAA228 at 2.32A resolution.
分子名称: (4S)-2-METHYL-2,4-PENTANEDIOL, 3-(8-DIMETHYLAMINOMETHYL-6,7,8,9-TETRAHYDRO-PYRIDO[1,2-A]INDOL-10-YL)-4-(1-METHYL-1H-INDOL-3-YL)-PYRROLE-2,5-DIONE, PROTEIN KINASE C THETA
著者Stark, W, Bitsch, F, Berner, A, Buelens, F, Graff, P, Depersin, H, Geiser, M, Knecht, R, Rahuel, J, Rummel, G, Schlaeppi, J.M, Schmitz, R, Strauss, A, Wagner, J.
登録日2007-01-16
公開日2008-02-05
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.32 Å)
主引用文献The Crystal Structure of the Kinase Domain of the Protein Kinase C Theta in Complex with Nvp-Xaa228
To be Published
2R5T
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Crystal Structure of Inactive Serum and Glucocorticoid- Regulated Kinase 1 in Complex with AMP-PNP
分子名称: MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, SULFATE ION, ...
著者Zhao, B, Lehr, R, Smallwood, A.M, Ho, T.F, Maley, K, Randall, T, Head, M.S, Koretke, K.K, Schnackenberg, C.G.
登録日2007-09-04
公開日2008-09-09
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Crystal structure of the kinase domain of serum and glucocorticoid-regulated kinase 1 in complex with AMP PNP.
Protein Sci., 16, 2007
2UW9
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STRUCTURE OF PKB-BETA (AKT2) COMPLEXED WITH 4-(4-chloro-phenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine
分子名称: 4-(4-CHLOROPHENYL)-4-[4-(1H-PYRAZOL-4-YL)PHENYL]PIPERIDINE, GLYCOGEN SYNTHASE KINASE-3 BETA, RAC-BETA SERINE/THREONINE-PROTEIN KINASE
著者Davies, T.G, Saxty, G, Woodhead, S.J, Berdini, V, Verdonk, M.L, Wyatt, P.G, Boyle, R.G, Barford, D, Downham, R, Garrett, M.D, Carr, R.A.
登録日2007-03-19
公開日2007-05-08
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery.
J.Med.Chem., 50, 2007
2X39
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Structure of 4-Amino-N-(4-chlorobenzyl)-1-(7H-pyrrolo(2,3-d)pyrimidin- 4-yl)piperidine-4-carboxamide bound to PKB
分子名称: 4-AMINO-N-(4-CHLOROBENZYL)-1-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PIPERIDINE-4-CARBOXAMIDE, GLYCOGEN SYNTHASE KINASE-3 BETA, RAC-BETA SERINE/THREONINE-PROTEIN KINASE
著者Davies, T.G, McHardy, T, Caldwell, J.J, Cheung, K.M, Hunter, L.J, Taylor, K, Rowlands, M, Ruddle, R, Henley, A, Brandon, A.D, Valenti, M, Fazal, L, Seavers, L, Raynaud, F.I, Eccles, S.A, Aherne, G.W, Garrett, M.D, Collins, I.
登録日2010-01-22
公開日2010-02-23
最終更新日2011-09-21
実験手法X-RAY DIFFRACTION (1.93 Å)
主引用文献Discovery of 4-Amino-1-(7H-Pyrrolo[2,3-D]Pyrimidin-4-Yl)Piperidine-4-Carboxamides as Selective, Orally Active Inhibitors of Protein Kinase B (Akt).
J.Med.Chem., 53, 2010
2XH5
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Structure of 4-(4-tert-Butylbenzyl)-1-(7H-pyrrolo(2,3-d)pyrimidin-4- yl)piperidin-4-amine bound to PKB
分子名称: 4-(4-tert-butylbenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-aminium, GLYCOGEN SYNTHASE KINASE-3 BETA, RAC-BETA SERINE/THREONINE-PROTEIN KINASE
著者Davies, T.G, McHardy, T, Caldwell, J.J, Cheung, K.M, Hunter, L.J, Taylor, K, Rowlands, M, Ruddle, R, Henley, A, Brandon, A.D, Valenti, M, Fazal, L, Seavers, L, Raynaud, F.I, Eccles, S.A, Aherne, G.W, Garrett, M.D, Collins, I.
登録日2010-06-09
公開日2010-06-16
最終更新日2024-10-16
実験手法X-RAY DIFFRACTION (2.72 Å)
主引用文献Discovery of 4-Amino-1-(7H-Pyrrolo[2,3-D]Pyrimidin-4-Yl)Piperidine-4-Carboxamides as Selective, Orally Active Inhibitors of Protein Kinase B (Akt).
J.Med.Chem., 53, 2010
3A60
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Crystal structure of unphosphorylated p70S6K1 (Form I)
分子名称: Ribosomal protein S6 kinase beta-1, STAUROSPORINE
著者Sunami, T, Byrne, N, Diehl, R.E, Funabashi, K, Hall, D.L, Ikuta, M, Patel, S.B, Shipman, J.M, Smith, R.F, Takahashi, I, Zugay-Murphy, J, Iwasawa, Y, Lumb, K.J, Munshi, S.K, Sharma, S.
登録日2009-08-17
公開日2009-10-27
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation.
J.Biol.Chem., 285, 2010
3A61
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Crystal structure of unphosphorylated p70S6K1 (Form II)
分子名称: Ribosomal protein S6 kinase beta-1, STAUROSPORINE
著者Sunami, T, Byrne, N, Diehl, R.E, Funabashi, K, Hall, D.L, Ikuta, M, Patel, S.B, Shipman, J.M, Smith, R.F, Takahashi, I, Zugay-Murphy, J, Iwasawa, Y, Lumb, K.J, Munshi, S.K, Sharma, S.
登録日2009-08-18
公開日2009-10-27
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (3.43 Å)
主引用文献Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation.
J.Biol.Chem., 285, 2010
3A62
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Crystal structure of phosphorylated p70S6K1
分子名称: MANGANESE (II) ION, Ribosomal protein S6 kinase beta-1, STAUROSPORINE
著者Sunami, T, Byrne, N, Diehl, R.E, Funabashi, K, Hall, D.L, Ikuta, M, Patel, S.B, Shipman, J.M, Smith, R.F, Takahashi, I, Zugay-Murphy, J, Iwasawa, Y, Lumb, K.J, Munshi, S.K, Sharma, S.
登録日2009-08-18
公開日2009-10-27
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.35 Å)
主引用文献Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation.
J.Biol.Chem., 285, 2010
3A8W
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Crystal Structure of PKCiota kinase domain
分子名称: ADENOSINE-5'-TRIPHOSPHATE, Protein kinase C iota type, SULFATE ION
著者Takimura, T, Kamata, K.
登録日2009-10-11
公開日2010-05-05
最終更新日2017-10-11
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Structures of the PKC-iota kinase domain in its ATP-bound and apo forms reveal defined structures of residues 533-551 in the C-terminal tail and their roles in ATP binding
Acta Crystallogr.,Sect.D, 66, 2010
3A8X
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Crystal Structure of PKCiota kinase domain
分子名称: Protein kinase C iota type, SULFATE ION
著者Takimura, T, Kamata, K.
登録日2009-10-11
公開日2010-05-05
最終更新日2017-10-11
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structures of the PKC-iota kinase domain in its ATP-bound and apo forms reveal defined structures of residues 533-551 in the C-terminal tail and their roles in ATP binding
Acta Crystallogr.,Sect.D, 66, 2010
3CQU
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Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor
分子名称: Glycogen synthase kinase-3 beta, N-[2-(5-methyl-4H-1,2,4-triazol-3-yl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine, RAC-alpha serine/threonine-protein kinase
著者Pandit, J.
登録日2008-04-03
公開日2008-05-27
最終更新日2021-10-20
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Synthesis and structure based optimization of novel Akt inhibitors
Bioorg.Med.Chem.Lett., 18, 2008
3CQW
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Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor
分子名称: 5-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine, Glycogen synthase kinase-3 beta, MANGANESE (II) ION, ...
著者Pandit, J.
登録日2008-04-03
公開日2008-05-27
最終更新日2021-10-20
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Synthesis and structure based optimization of novel Akt inhibitors
Bioorg.Med.Chem.Lett., 18, 2008
3D0E
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Crystal structure of human Akt2 in complex with GSK690693
分子名称: 4-{2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-piperidin-3-ylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl}-2-methylbut-3 -yn-2-ol, RAC-beta serine/threonine-protein kinase
著者Concha, N.O, Smallwood, A.
登録日2008-05-01
公開日2008-10-21
最終更新日2024-10-16
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
J.Med.Chem., 51, 2008

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