6XOG
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![BU of 6xog by Molmil](/molmil-images/mine/6xog) | Structure of SUMO1-ML786519 adduct bound to SAE | 分子名称: | SULFATE ION, SUMO-activating enzyme subunit 1, SUMO-activating enzyme subunit 2, ... | 著者 | Sintchak, M, Lane, W, Bump, N. | 登録日 | 2020-07-07 | 公開日 | 2021-03-10 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (1.98 Å) | 主引用文献 | Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer. J.Med.Chem., 64, 2021
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6XOH
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![BU of 6xoh by Molmil](/molmil-images/mine/6xoh) | Structure of SUMO1-ML00789344 adduct bound to SAE | 分子名称: | SULFATE ION, SUMO-activating enzyme subunit 1, SUMO-activating enzyme subunit 2, ... | 著者 | Sintchak, M, Lane, W, Bump, N. | 登録日 | 2020-07-07 | 公開日 | 2021-03-24 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2.226 Å) | 主引用文献 | Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer. J.Med.Chem., 64, 2021
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6XOI
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![BU of 6xoi by Molmil](/molmil-images/mine/6xoi) | Structure of SUMO1-ML00752641 adduct bound to SAE | 分子名称: | SULFATE ION, SUMO-activating enzyme subunit 1, SUMO-activating enzyme subunit 2, ... | 著者 | Sintchak, M, Lane, W, Bump, N. | 登録日 | 2020-07-07 | 公開日 | 2021-03-24 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer. J.Med.Chem., 64, 2021
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5TR4
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![BU of 5tr4 by Molmil](/molmil-images/mine/5tr4) | Structure of Ubiquitin activating enzyme (Uba1) in complex with ubiquitin and TAK-243 | 分子名称: | Ubiquitin, Ubiquitin-activating enzyme E1 1, [(1~{R},2~{R},3~{S},4~{R})-2,3-bis(oxidanyl)-4-[[2-[3-(trifluoromethylsulfanyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl sulfamate | 著者 | Sintchak, M.D. | 登録日 | 2016-10-25 | 公開日 | 2017-11-01 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | Identification and Characterization of a Small Molecule Inhibitor of the Ubiquitin Activating Enzyme (TAK-243) To be published
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3MG7
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![BU of 3mg7 by Molmil](/molmil-images/mine/3mg7) | Structure of yeast 20S open-gate proteasome with Compound 8 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-(benzyloxy)-N-[(1S,2R)-2-hydroxy-1-({(1S)-1-[(2-methylbenzyl)carbamoyl]-3-phenylpropyl}carbamoyl)propyl]benzamide, MAGNESIUM ION, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-04-05 | 公開日 | 2011-05-18 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.78 Å) | 主引用文献 | Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. Biochem.J., 430, 2010
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3SDK
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![BU of 3sdk by Molmil](/molmil-images/mine/3sdk) | Structure of yeast 20S open-gate proteasome with Compound 34 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N-[(2S)-3-(3-tert-butyl-1,2,4-oxadiazol-5-yl)-1-({(2S)-1-[(4-methylbenzyl)amino]-1-oxo-4-phenylbutan-2-yl}amino)-1-oxopropan-2-yl]-5-methyl-1,2-oxazole-3-carboxamide, ... | 著者 | Sintchak, M.D. | 登録日 | 2011-06-09 | 公開日 | 2012-06-13 | 最終更新日 | 2023-09-13 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome. Bioorg.Med.Chem.Lett., 20, 2010
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3SDI
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![BU of 3sdi by Molmil](/molmil-images/mine/3sdi) | Structure of yeast 20S open-gate proteasome with Compound 20 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N~4~-(2,2-dimethylpropyl)-N~1~-{(2S)-1-[(4-methylbenzyl)amino]-1-oxo-4-phenylbutan-2-yl}-N~2~-[(5-methyl-1,2-oxazol-3-yl)carbonyl]-L-aspartamide, ... | 著者 | Sintchak, M.D. | 登録日 | 2011-06-09 | 公開日 | 2012-06-13 | 最終更新日 | 2023-09-13 | 実験手法 | X-RAY DIFFRACTION (2.65 Å) | 主引用文献 | Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome. Bioorg.Med.Chem.Lett., 20, 2010
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3MG0
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![BU of 3mg0 by Molmil](/molmil-images/mine/3mg0) | Structure of yeast 20S proteasome with bortezomib | 分子名称: | N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, Proteasome component C1, Proteasome component C11, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-04-05 | 公開日 | 2011-05-18 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.68 Å) | 主引用文献 | Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. Biochem.J., 430, 2010
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3OEU
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![BU of 3oeu by Molmil](/molmil-images/mine/3oeu) | Structure of yeast 20S open-gate proteasome with Compound 24 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N-{(2S)-1-[(2-chlorobenzyl)amino]-1-oxo-4-phenylbutan-2-yl}-N~2~-[3-(2-methylphenyl)propanoyl]-L-threoninamide, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-08-13 | 公開日 | 2011-07-20 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome. Bioorg.Med.Chem.Lett., 20, 2010
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3MG4
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![BU of 3mg4 by Molmil](/molmil-images/mine/3mg4) | Structure of yeast 20S proteasome with Compound 1 | 分子名称: | (2S)-2-amino-N-[(1S)-1-({(1S)-1-[(4-methylbenzyl)carbamoyl]-3-phenylpropyl}carbamoyl)-3-phenylpropyl]-4-phenylbutanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-04-05 | 公開日 | 2011-04-27 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (3.11 Å) | 主引用文献 | Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. Biochem.J., 430, 2010
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3MG8
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![BU of 3mg8 by Molmil](/molmil-images/mine/3mg8) | Structure of yeast 20S open-gate proteasome with Compound 16 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N-(2,2-dimethylpropyl)-N~2~-[1H-indol-3-yl(oxo)acetyl]-L-asparaginyl-N-(2-methylbenzyl)-3-pyridin-4-yl-L-alaninamide, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-04-05 | 公開日 | 2011-05-18 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.59 Å) | 主引用文献 | Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. Biochem.J., 430, 2010
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3OEV
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![BU of 3oev by Molmil](/molmil-images/mine/3oev) | Structure of yeast 20S open-gate proteasome with Compound 25 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-(benzyloxy)-N-[(2S,3R)-3-hydroxy-1-{[(2S)-1-{[(3-methylthiophen-2-yl)methyl]amino}-1-oxo-4-phenylbutan-2-yl]amino}-1-oxobutan-2-yl]benzamide, MAGNESIUM ION, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-08-13 | 公開日 | 2011-07-20 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | 主引用文献 | Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome. Bioorg.Med.Chem.Lett., 20, 2010
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3MG6
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![BU of 3mg6 by Molmil](/molmil-images/mine/3mg6) | Structure of yeast 20S open-gate proteasome with Compound 6 | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N~2~-{[(1S)-6-methoxy-3-oxo-2,3-dihydro-1H-inden-1-yl]acetyl}-N-{(1S)-1-[(4-methylbenzyl)carbamoyl]-3-phenylpropyl}-L-threoninamide, ... | 著者 | Sintchak, M.D. | 登録日 | 2010-04-05 | 公開日 | 2011-05-18 | 最終更新日 | 2023-09-06 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. Biochem.J., 430, 2010
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