3L13
| Crystal Structures of Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors | Descriptor: | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, [3-(6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenyl]methanol | Authors: | Murray, J.M, Wiesmann, C. | Deposit date: | 2009-12-10 | Release date: | 2010-02-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer. J.Med.Chem., 53, 2010
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3A60
| Crystal structure of unphosphorylated p70S6K1 (Form I) | Descriptor: | Ribosomal protein S6 kinase beta-1, STAUROSPORINE | Authors: | 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. | Deposit date: | 2009-08-17 | Release date: | 2009-10-27 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation. J.Biol.Chem., 285, 2010
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3A61
| Crystal structure of unphosphorylated p70S6K1 (Form II) | Descriptor: | Ribosomal protein S6 kinase beta-1, STAUROSPORINE | Authors: | 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. | Deposit date: | 2009-08-18 | Release date: | 2009-10-27 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (3.43 Å) | Cite: | Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation. J.Biol.Chem., 285, 2010
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3A62
| Crystal structure of phosphorylated p70S6K1 | Descriptor: | MANGANESE (II) ION, Ribosomal protein S6 kinase beta-1, STAUROSPORINE | Authors: | 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. | Deposit date: | 2009-08-18 | Release date: | 2009-10-27 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Structural basis of human p70 ribosomal S6 kinase-1 regulation by activation loop phosphorylation. J.Biol.Chem., 285, 2010
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3IBE
| Crystal Structure of a Pyrazolopyrimidine Inhibitor Bound to PI3 Kinase Gamma | Descriptor: | 1-(4-{4-morpholin-4-yl-1-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl}phenyl)-3-pyridin-4-ylurea, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | Authors: | Bard, J, Svenson, K. | Deposit date: | 2009-07-15 | Release date: | 2009-09-01 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.798 Å) | Cite: | ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines. J.Med.Chem., 52, 2009
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3HXI
| Crystal structure of Schistosome eIF4E complexed with m7GpppG and 4E-BP | Descriptor: | 7-METHYL-GUANOSINE-5'-TRIPHOSPHATE-5'-GUANOSINE, Eukaryotic Translation Initiation 4E, Eukaryotic translation initiation factor 4E-binding protein 1 | Authors: | Liu, W, Zhao, R, Jones, D.N.M, Davis, R.E. | Deposit date: | 2009-06-20 | Release date: | 2009-08-25 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Structural insights into parasite EIF4E binding specificity for m7G and m2,2,7G mRNA cap. J.Biol.Chem., 284, 2009
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3HXG
| Crystal structure of Schistsome eIF4E complexed with m7GpppA and 4E-BP | Descriptor: | Eukaryotic Translation Initiation Factor 4E, Eukaryotic translation initiation factor 4E-binding protein 1, P1-7-METHYLGUANOSINE-P3-ADENOSINE-5',5'-TRIPHOSPHATE | Authors: | Liu, W, Zhao, R, Jones, D.N.M, Davis, R.E. | Deposit date: | 2009-06-20 | Release date: | 2009-08-25 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Structural insights into parasite EIF4E binding specificity for m7G and m2,2,7G mRNA cap. J.Biol.Chem., 284, 2009
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3CQW
| Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor | Descriptor: | 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, ... | Authors: | Pandit, J. | Deposit date: | 2008-04-03 | Release date: | 2008-05-27 | Last modified: | 2021-10-20 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Synthesis and structure based optimization of novel Akt inhibitors Bioorg.Med.Chem.Lett., 18, 2008
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3CQU
| Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor | Descriptor: | 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 | Authors: | Pandit, J. | Deposit date: | 2008-04-03 | Release date: | 2008-05-27 | Last modified: | 2021-10-20 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Synthesis and structure based optimization of novel Akt inhibitors Bioorg.Med.Chem.Lett., 18, 2008
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2VKI
| Structure of the PDK1 PH domain K465E mutant | Descriptor: | 3-PHOPSHOINOSITIDE DEPENDENT PROTEIN KINASE 1, GLYCEROL, SULFATE ION | Authors: | Komander, D, Bayascas, J.R, Deak, M, Alessi, D.R, van Aalten, D.M.F. | Deposit date: | 2007-12-19 | Release date: | 2008-05-13 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Mutation of the Pdk1 Ph Domain Inhibits Protein Kinase B/Akt, Leading to Small Size and Insulin Resistance. Mol.Cell.Biol., 28, 2008
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2NPU
| The solution structure of the rapamycin-binding domain of mTOR (FRB) | Descriptor: | FKBP12-rapamycin complex-associated protein | Authors: | Veverka, V, Crabbe, T, Bird, I, Lennie, G, Muskett, F.W, Taylor, R.J, Carr, M.D. | Deposit date: | 2006-10-30 | Release date: | 2007-09-18 | Last modified: | 2024-05-15 | Method: | SOLUTION NMR | Cite: | Structural characterization of the interaction of mTOR with phosphatidic acid and a novel class of inhibitor: compelling evidence for a central role of the FRB domain in small molecule-mediated regulation of mTOR. Oncogene, 27, 2008
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2JGC
| Structure of the human eIF4E homologous protein, 4EHP without ligand bound | Descriptor: | EUKARYOTIC TRANSLATION INITIATION FACTOR 4E TYPE 2, EUKARYOTIC TRANSLATION INITIATION FACTOR 4E-BINDING PROTEIN 1 | Authors: | Cameron, A.D, Rosettani, P, Knapp, S, Vismara, M.G, Rusconi, L. | Deposit date: | 2007-02-12 | Release date: | 2007-02-27 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structures of the human eIF4E homologous protein, h4EHP, in its m7GTP-bound and unliganded forms. J. Mol. Biol., 368, 2007
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2JGB
| Structure of human eIF4E homologous protein 4EHP with m7GTP | Descriptor: | 7N-METHYL-8-HYDROGUANOSINE-5'-TRIPHOSPHATE, EUKARYOTIC TRANSLATION INITIATION FACTOR 4E TYPE 2, EUKARYOTIC TRANSLATION INITIATION FACTOR 4E-BINDING PROTEIN 1 | Authors: | Cameron, A.D, Rosettani, P, Knapp, S, Vismara, M.G, Rusconi, L. | Deposit date: | 2007-02-12 | Release date: | 2007-02-27 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Structures of the human eIF4E homologous protein, h4EHP, in its m7GTP-bound and unliganded forms. J. Mol. Biol., 368, 2007
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2GAQ
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1YZ1
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1WKW
| Crystal structure of the ternary complex of eIF4E-m7GpppA-4EBP1 peptide | Descriptor: | Eukaryotic translation initiation factor 4E, Eukaryotic translation initiation factor 4E binding protein 1, P1-7-METHYLGUANOSINE-P3-ADENOSINE-5',5'-TRIPHOSPHATE | Authors: | Tomoo, K, Matsushita, Y, Fujisaki, H, Shen, X, Miyagawa, H, Kitamura, K, Miura, K, Ishida, T. | Deposit date: | 2004-06-10 | Release date: | 2005-06-10 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Structural basis for mRNA Cap-Binding regulation of eukaryotic initiation factor 4E by 4E-binding protein, studied by spectroscopic, X-ray crystal structural, and molecular dynamics simulation methods Biochim.Biophys.Acta, 1753, 2005
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1EJH
| EIF4E/EIF4G PEPTIDE/7-METHYL-GDP | Descriptor: | 7N-METHYL-8-HYDROGUANOSINE-5'-DIPHOSPHATE, EUKARYOTIC INITIATION FACTOR 4E, EUKARYOTIC INITIATION FACTOR 4GII | Authors: | Marcotrigiano, J, Gingras, A.-C, Sonenberg, N, Burley, S.K. | Deposit date: | 2000-03-02 | Release date: | 2000-03-10 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Cap-dependent translation initiation in eukaryotes is regulated by a molecular mimic of eIF4G. Mol.Cell, 3, 1999
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