3NR5
 
 | | Crystal structure of human Maf1 | | 分子名称: | Repressor of RNA polymerase III transcription MAF1 homolog | | 著者 | Ringel, R, Vannini, A, Kusser, A.G, Berninghausen, O, Kassavetis, G.A, Cramer, P. | | 登録日 | 2010-06-30 | | 公開日 | 2010-10-13 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Molecular Basis of RNA Polymerase III Transcription Repression by Maf1
Cell(Cambridge,Mass.), 143, 2010
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6XK9
 | | Cereblon in complex with DDB1, CC-90009, and GSPT1 | | 分子名称: | 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, ... | | 著者 | Clayton, T.L, Tran, E.T, Zhu, J, Pagarigan, B.E, Matyskiela, M.E, Chamberlain, P.P. | | 登録日 | 2020-06-25 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.64 Å) | | 主引用文献 | CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells.
Blood, 137, 2021
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6D5Y
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7K6O
 | | Crystal structure of PI3Kalpha inhibitor 10-5429 | | 分子名称: | (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 | | 著者 | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | | 登録日 | 2020-09-21 | | 公開日 | 2021-01-06 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.738 Å) | | 主引用文献 | 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 | | 分子名称: | 2-(morpholin-4-yl)[4,5'-bipyrimidin]-2'-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | | 登録日 | 2020-09-21 | | 公開日 | 2021-01-06 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | 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 | | 分子名称: | 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 | | 著者 | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | | 登録日 | 2020-09-21 | | 公開日 | 2021-01-06 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.77 Å) | | 主引用文献 | 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 | | 分子名称: | 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 | | 著者 | Chen, P, Brooun, A, Deng, Y.L, Grodsky, N, Kaiser, S.E. | | 登録日 | 2020-09-21 | | 公開日 | 2021-01-06 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.413 Å) | | 主引用文献 | Structure-Based Drug Design and Synthesis of PI3K alpha-Selective Inhibitor (PF-06843195).
J.Med.Chem., 64, 2021
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6Z6M
 | | Cryo-EM structure of human 80S ribosomes bound to EBP1, eEF2 and SERBP1 | | 分子名称: | 18S rRNA, 28S rRNA, 40S ribosomal protein S10, ... | | 著者 | Wells, J.N, Buschauer, R, Mackens-Kiani, T, Best, K, Kratzat, H, Berninghausen, O, Becker, T, Cheng, J, Beckmann, R. | | 登録日 | 2020-05-28 | | 公開日 | 2020-07-29 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | | 主引用文献 | Structure and function of yeast Lso2 and human CCDC124 bound to hibernating ribosomes.
Plos Biol., 18, 2020
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6Z6N
 | | Cryo-EM structure of human EBP1-80S ribosomes (focus on EBP1) | | 分子名称: | 18S rRNA, 28S rRNA, 40S ribosomal protein S10, ... | | 著者 | Wells, J.N, Buschauer, R, Mackens-Kiani, T, Best, K, Kratzat, H, Berninghausen, O, Becker, T, Cheng, J, Beckmann, R. | | 登録日 | 2020-05-28 | | 公開日 | 2020-07-29 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (2.9 Å) | | 主引用文献 | Structure and function of yeast Lso2 and human CCDC124 bound to hibernating ribosomes.
Plos Biol., 18, 2020
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6CHZ
 | | Estrogen Receptor Alpha Y537S bound to antagonist H3B-9224. | | 分子名称: | 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 | | 著者 | Larsen, N.A. | | 登録日 | 2018-02-23 | | 公開日 | 2018-03-21 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (1.68 Å) | | 主引用文献 | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer.
Cancer Discov, 8, 2018
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4ZVV
 | | Lactate dehydrogenase A in complex with a trisubstituted piperidine-2,4-dione inhibitor GNE-140 | | 分子名称: | (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, ... | | 著者 | Li, Y, Chen, Z, Eigenbrot, C. | | 登録日 | 2015-05-18 | | 公開日 | 2016-05-18 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.
Nat.Chem.Biol., 12, 2016
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4OYS
 | | CRYSTAL STRUCTURE OF VPS34 IN COMPLEX WITH SAR405. | | 分子名称: | (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 | | 著者 | Mathieu, M, Marquette, J.p. | | 登録日 | 2014-02-13 | | 公開日 | 2014-10-22 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy.
Nat.Chem.Biol., 10, 2014
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1YZ1
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8K2C
 | | Cryo-EM structure of the human 80S ribosome with Tigecycline | | 分子名称: | 18S rRNA, 28S rRNA, 40S ribosomal protein S10, ... | | 著者 | Li, X, Wang, M, Cheng, J. | | 登録日 | 2023-07-12 | | 公開日 | 2024-07-10 | | 実験手法 | ELECTRON MICROSCOPY (2.4 Å) | | 主引用文献 | Structural basis for differential inhibition of eukaryotic ribosomes by tigecycline.
Nat Commun, 15, 2024
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4DK5
 | | Crystal structure of human PI3K-gamma in complex with a pyridyl-triazine inhibitor | | 分子名称: | 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 | | 著者 | Whittington, D.A, Tang, J, Yakowec, P. | | 登録日 | 2012-02-03 | | 公開日 | 2012-05-16 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | 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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3SD5
 | | Crystal Structure of PI3K gamma with 5-(2,4-dimorpholinopyrimidin-6-yl)-4-(trifluoromethyl)pyridin-2-amine | | 分子名称: | 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 | | 著者 | Knapp, M.S, Elling, R.A. | | 登録日 | 2011-06-08 | | 公開日 | 2012-01-04 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor.
Mol.Cancer Ther., 11, 2012
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4FUL
 | | PI3 Kinase Gamma bound to a pyrmidine inhibitor | | 分子名称: | 4-({4-[3-(piperidin-1-ylcarbonyl)phenyl]pyrimidin-2-yl}amino)benzenesulfonamide, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Gopalsamy, A, Bennett, E.M, Shi, M, Zhang, W.G, Bard, J, Yu, K. | | 登録日 | 2012-06-28 | | 公開日 | 2012-10-17 | | 最終更新日 | 2012-10-31 | | 実験手法 | X-RAY DIFFRACTION (2.47 Å) | | 主引用文献 | Identification of pyrimidine derivatives as hSMG-1 inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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5OBM
 | | Crystal structure of Gentamicin bound to the yeast 80S ribosome | | 分子名称: | (2R,3R,4R,5R)-2-((1S,2S,3R,4S,6R)-4,6-DIAMINO-3-((2R,3R,6S)-3-AMINO-6-(AMINOMETHYL)-TETRAHYDRO-2H-PYRAN-2-YLOXY)-2-HYDR OXYCYCLOHEXYLOXY)-5-METHYL-4-(METHYLAMINO)-TETRAHYDRO-2H-PYRAN-3,5-DIOL, 18S ribosomal RNA, 25S ribosomal RNA, ... | | 著者 | Prokhorova, I, Djumagulov, M, Urzhumtsev, A, Yusupov, M, Yusupova, G. | | 登録日 | 2017-06-28 | | 公開日 | 2017-12-13 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Aminoglycoside interactions and impacts on the eukaryotic ribosome.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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1EJH
 | | EIF4E/EIF4G PEPTIDE/7-METHYL-GDP | | 分子名称: | 7N-METHYL-8-HYDROGUANOSINE-5'-DIPHOSPHATE, EUKARYOTIC INITIATION FACTOR 4E, EUKARYOTIC INITIATION FACTOR 4GII | | 著者 | Marcotrigiano, J, Gingras, A.-C, Sonenberg, N, Burley, S.K. | | 登録日 | 2000-03-02 | | 公開日 | 2000-03-10 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Cap-dependent translation initiation in eukaryotes is regulated by a molecular mimic of eIF4G.
Mol.Cell, 3, 1999
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2VKI
 | | Structure of the PDK1 PH domain K465E mutant | | 分子名称: | 3-PHOPSHOINOSITIDE DEPENDENT PROTEIN KINASE 1, GLYCEROL, SULFATE ION | | 著者 | Komander, D, Bayascas, J.R, Deak, M, Alessi, D.R, van Aalten, D.M.F. | | 登録日 | 2007-12-19 | | 公開日 | 2008-05-13 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | 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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1WKW
 | | Crystal structure of the ternary complex of eIF4E-m7GpppA-4EBP1 peptide | | 分子名称: | Eukaryotic translation initiation factor 4E, Eukaryotic translation initiation factor 4E binding protein 1, P1-7-METHYLGUANOSINE-P3-ADENOSINE-5',5'-TRIPHOSPHATE | | 著者 | Tomoo, K, Matsushita, Y, Fujisaki, H, Shen, X, Miyagawa, H, Kitamura, K, Miura, K, Ishida, T. | | 登録日 | 2004-06-10 | | 公開日 | 2005-06-10 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | 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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7Y62
 | | Crystal structure of human TFEB HLHLZ domain | | 分子名称: | Transcription factor EB | | 著者 | Yang, G, Li, P, Lin, Y, Liu, Z, Sun, H, Zhao, Z, Fang, P, Wang, J. | | 登録日 | 2022-06-18 | | 公開日 | 2023-03-22 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | A small-molecule drug inhibits autophagy gene expression through the central regulator TFEB.
Proc.Natl.Acad.Sci.USA, 120, 2023
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6FO1
 | | Human R2TP subcomplex containing 1 RUVBL1-RUVBL2 hexamer bound to 1 RBD domain from RPAP3. | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, RNA polymerase II-associated protein 3, RuvB-like 1, ... | | 著者 | Martino, F, Munoz-Hernandez, H, Rodriguez, C.F, Pearl, L.H, Llorca, O. | | 登録日 | 2018-02-05 | | 公開日 | 2018-04-04 | | 最終更新日 | 2019-12-11 | | 実験手法 | ELECTRON MICROSCOPY (3.57 Å) | | 主引用文献 | RPAP3 provides a flexible scaffold for coupling HSP90 to the human R2TP co-chaperone complex.
Nat Commun, 9, 2018
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3CQW
 | | 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
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4U4U
 | | Crystal structure of Lycorine bound to the yeast 80S ribosome | | 分子名称: | (1S,2S,12bS,12cS)-2,4,5,7,12b,12c-hexahydro-1H-[1,3]dioxolo[4,5-j]pyrrolo[3,2,1-de]phenanthridine-1,2-diol, 18S ribosomal RNA, 25S ribosomal RNA, ... | | 著者 | Garreau de Loubresse, N, Prokhorova, I, Yusupova, G, Yusupov, M. | | 登録日 | 2014-07-24 | | 公開日 | 2014-10-22 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Structural basis for the inhibition of the eukaryotic ribosome.
Nature, 513, 2014
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