5C0V
| Structure of the LARP1-unique domain DM15 | Descriptor: | La-related protein 1, SULFATE ION | Authors: | Lahr, R.M, Berman, A.J. | Deposit date: | 2015-06-12 | Release date: | 2015-08-05 | Last modified: | 2017-11-01 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | The La-related protein 1-specific domain repurposes HEAT-like repeats to directly bind a 5'TOP sequence. Nucleic Acids Res., 43, 2015
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3L54
| Structure of Pi3K gamma with inhibitor | Descriptor: | 6-(1H-pyrazolo[3,4-b]pyridin-5-yl)-4-pyridin-4-ylquinoline, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | Authors: | Elkins, P.A, Smallwood, A.M. | Deposit date: | 2009-12-21 | Release date: | 2010-06-30 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett, 1, 2010
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3L08
| Structure of Pi3K gamma with a potent inhibitor: GSK2126458 | Descriptor: | 2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | Authors: | Elkins, P.A, Marrero, E.M. | Deposit date: | 2009-12-09 | Release date: | 2010-06-23 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett, 1, 2010
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2MX4
| NMR structure of Phosphorylated 4E-BP2 | Descriptor: | Eukaryotic translation initiation factor 4E-binding protein 2 | Authors: | Bah, A, Forman-Kay, J, Vernon, R, Siddiqui, Z, Krzeminski, M, Muhandiram, R, Zhao, C, Sonenberg, N, Kay, L. | Deposit date: | 2014-12-10 | Release date: | 2015-01-07 | Last modified: | 2015-03-18 | Method: | SOLUTION NMR | Cite: | Folding of an intrinsically disordered protein by phosphorylation as a regulatory switch. Nature, 519, 2015
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6XK9
| Cereblon in complex with DDB1, CC-90009, and GSPT1 | Descriptor: | 2-(4-chlorophenyl)-N-({2-[(3S)-2,6-dioxopiperidin-3-yl]-1-oxo-2,3-dihydro-1H-isoindol-5-yl}methyl)-2,2-difluoroacetamide, DNA damage-binding protein 1, Eukaryotic peptide chain release factor GTP-binding subunit ERF3A, ... | Authors: | Clayton, T.L, Tran, E.T, Zhu, J, Pagarigan, B.E, Matyskiela, M.E, Chamberlain, P.P. | Deposit date: | 2020-06-25 | Release date: | 2020-12-02 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (3.64 Å) | Cite: | CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells. Blood, 137, 2021
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4OYS
| CRYSTAL STRUCTURE OF VPS34 IN COMPLEX WITH SAR405. | Descriptor: | (8S)-9-[(5-chloranylpyridin-3-yl)methyl]-2-[(3R)-3-methylmorpholin-4-yl]-8-(trifluoromethyl)-6,7,8,9a-tetrahydro-3H-pyrimido[1,2-a]pyrimidin-4-one, Phosphatidylinositol 3-kinase catalytic subunit type 3, SULFATE ION | Authors: | Mathieu, M, Marquette, J.p. | Deposit date: | 2014-02-13 | Release date: | 2014-10-22 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy. Nat.Chem.Biol., 10, 2014
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5NVN
| Crystal structure of the human 4EHP-4E-BP1 complex | Descriptor: | Eukaryotic translation initiation factor 4E type 2, Eukaryotic translation initiation factor 4E-binding protein 1, FORMIC ACID | Authors: | Peter, D, Sandmeir, F, Valkov, E. | Deposit date: | 2017-05-04 | Release date: | 2017-07-26 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | GIGYF1/2 proteins use auxiliary sequences to selectively bind to 4EHP and repress target mRNA expression. Genes Dev., 31, 2017
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6Z6N
| Cryo-EM structure of human EBP1-80S ribosomes (focus on EBP1) | Descriptor: | 18S rRNA, 28S rRNA, 40S ribosomal protein S10, ... | Authors: | Wells, J.N, Buschauer, R, Mackens-Kiani, T, Best, K, Kratzat, H, Berninghausen, O, Becker, T, Cheng, J, Beckmann, R. | Deposit date: | 2020-05-28 | Release date: | 2020-07-29 | Last modified: | 2024-05-22 | Method: | ELECTRON MICROSCOPY (2.9 Å) | Cite: | Structure and function of yeast Lso2 and human CCDC124 bound to hibernating ribosomes. Plos Biol., 18, 2020
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6Z6M
| Cryo-EM structure of human 80S ribosomes bound to EBP1, eEF2 and SERBP1 | Descriptor: | 18S rRNA, 28S rRNA, 40S ribosomal protein S10, ... | Authors: | Wells, J.N, Buschauer, R, Mackens-Kiani, T, Best, K, Kratzat, H, Berninghausen, O, Becker, T, Cheng, J, Beckmann, R. | Deposit date: | 2020-05-28 | Release date: | 2020-07-29 | Last modified: | 2024-05-22 | Method: | ELECTRON MICROSCOPY (3.1 Å) | Cite: | Structure and function of yeast Lso2 and human CCDC124 bound to hibernating ribosomes. Plos Biol., 18, 2020
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7K6O
| Crystal structure of PI3Kalpha inhibitor 10-5429 | Descriptor: | (3S)-3-[4-(2-aminopyrimidin-5-yl)-2-(morpholin-4-yl)-5,6-dihydro-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-N-methylpyrrolidine-1-sulfonamide, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Authors: | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | Deposit date: | 2020-09-21 | Release date: | 2021-01-06 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.738 Å) | Cite: | Structure-Based Drug Design and Synthesis of PI3K alpha-Selective Inhibitor (PF-06843195). J.Med.Chem., 64, 2021
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7K71
| Crystal structure of PI3Kalpha inhibitor 4-0686 | Descriptor: | 2-(morpholin-4-yl)[4,5'-bipyrimidin]-2'-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Authors: | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | Deposit date: | 2020-09-21 | Release date: | 2021-01-06 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structure-Based Drug Design and Synthesis of PI3K alpha-Selective Inhibitor (PF-06843195). J.Med.Chem., 64, 2021
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7K6N
| Crystal structure of PI3Kalpha selective Inhibitor 11-1575 | Descriptor: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, tert-butyl (3S)-3-[4-(2-aminopyrimidin-5-yl)-2-(morpholin-4-yl)-5,6-dihydro-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-3-methylpyrrolidine-1-carboxylate | Authors: | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | Deposit date: | 2020-09-21 | Release date: | 2021-01-06 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.77 Å) | Cite: | Structure-Based Drug Design and Synthesis of PI3K alpha-Selective Inhibitor (PF-06843195). J.Med.Chem., 64, 2021
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7K6M
| Crystal structure of PI3Kalpha selective Inhibitor PF-06843195 | Descriptor: | 2,2-difluoroethyl (3S)-3-{[2'-amino-5-fluoro-2-(morpholin-4-yl)[4,5'-bipyrimidin]-6-yl]amino}-3-(hydroxymethyl)pyrrolidine-1-carboxylate, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Authors: | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | Deposit date: | 2020-09-21 | Release date: | 2021-01-06 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.413 Å) | Cite: | Structure-Based Drug Design and Synthesis of PI3K alpha-Selective Inhibitor (PF-06843195). J.Med.Chem., 64, 2021
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3NR5
| Crystal structure of human Maf1 | Descriptor: | Repressor of RNA polymerase III transcription MAF1 homolog | Authors: | Ringel, R, Vannini, A, Kusser, A.G, Berninghausen, O, Kassavetis, G.A, Cramer, P. | Deposit date: | 2010-06-30 | Release date: | 2010-10-13 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (1.55 Å) | Cite: | Molecular Basis of RNA Polymerase III Transcription Repression by Maf1 Cell(Cambridge,Mass.), 143, 2010
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6D5Y
| Crystal structure of ERK2 G169D mutant | Descriptor: | Mitogen-activated protein kinase 1 | Authors: | Yin, J, Jaiswal, B.S, Wang, W. | Deposit date: | 2018-04-19 | Release date: | 2019-02-27 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.86 Å) | Cite: | ERK Mutations and Amplification Confer Resistance to ERK-Inhibitor Therapy. Clin. Cancer Res., 24, 2018
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6CHZ
| Estrogen Receptor Alpha Y537S bound to antagonist H3B-9224. | Descriptor: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, Estrogen receptor | Authors: | Larsen, N.A. | Deposit date: | 2018-02-23 | Release date: | 2018-03-21 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.68 Å) | Cite: | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer. Cancer Discov, 8, 2018
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6CHW
| Estrogen Receptor Alpha Y537S covalently bound to antagonist H3B-5942. | Descriptor: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, DIMETHYL SULFOXIDE, ... | Authors: | Larsen, N.A. | Deposit date: | 2018-02-23 | Release date: | 2018-03-21 | Last modified: | 2020-02-26 | Method: | X-RAY DIFFRACTION (1.89 Å) | Cite: | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer. Cancer Discov, 8, 2018
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4DK5
| Crystal structure of human PI3K-gamma in complex with a pyridyl-triazine inhibitor | Descriptor: | 4-(2-[(6-methoxypyridin-3-yl)amino]-5-{[4-(methylsulfonyl)piperazin-1-yl]methyl}pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | Authors: | Whittington, D.A, Tang, J, Yakowec, P. | Deposit date: | 2012-02-03 | Release date: | 2012-05-16 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.95 Å) | Cite: | Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases. J.Med.Chem., 55, 2012
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1YZ1
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3SD5
| Crystal Structure of PI3K gamma with 5-(2,4-dimorpholinopyrimidin-6-yl)-4-(trifluoromethyl)pyridin-2-amine | Descriptor: | 5-[2,6-di(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Authors: | Knapp, M.S, Elling, R.A. | Deposit date: | 2011-06-08 | Release date: | 2012-01-04 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor. Mol.Cancer Ther., 11, 2012
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4ZVV
| Lactate dehydrogenase A in complex with a trisubstituted piperidine-2,4-dione inhibitor GNE-140 | Descriptor: | (2~{R})-5-(2-chlorophenyl)sulfanyl-2-(4-morpholin-4-ylphenyl)-4-oxidanyl-2-thiophen-3-yl-1,3-dihydropyridin-6-one, L-lactate dehydrogenase A chain, NICOTINAMIDE-ADENINE-DINUCLEOTIDE, ... | Authors: | Li, Y, Chen, Z, Eigenbrot, C. | Deposit date: | 2015-05-18 | Release date: | 2016-05-18 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition. Nat.Chem.Biol., 12, 2016
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5JXD
| Crystal structure of murine Tnfaip8 C165S mutant | Descriptor: | Tumor necrosis factor alpha-induced protein 8, [(2~{R})-1-[2-azanylethoxy(oxidanyl)phosphoryl]oxy-3-hexadecanoyloxy-propan-2-yl] (~{Z})-octadec-9-enoate | Authors: | Park, J, Kim, M.S, Lee, D, Shin, D.H. | Deposit date: | 2016-05-13 | Release date: | 2017-06-28 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.029 Å) | Cite: | The Tnfaip8-PE complex is a novel upstream effector in the anti-autophagic action of insulin Sci Rep, 7, 2017
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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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7Y62
| Crystal structure of human TFEB HLHLZ domain | Descriptor: | Transcription factor EB | Authors: | Yang, G, Li, P, Lin, Y, Liu, Z, Sun, H, Zhao, Z, Fang, P, Wang, J. | Deposit date: | 2022-06-18 | Release date: | 2023-03-22 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | A small-molecule drug inhibits autophagy gene expression through the central regulator TFEB. Proc.Natl.Acad.Sci.USA, 120, 2023
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