3NZW
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![BU of 3nzw by Molmil](/molmil-images/mine/3nzw) | Crystal structure of the yeast 20S proteasome in complex with 2b | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Proteasome component C1, Proteasome component C11, ... | 著者 | Groll, M, Gallastegui, N, Marechal, X, Le Ravalec, V, Basse, N, Richy, N, Genin, E, Huber, R, Moroder, M, Vidal, V, Reboud-Ravaux, M. | 登録日 | 2010-07-17 | 公開日 | 2011-02-16 | 最終更新日 | 2023-12-06 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | 20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A. Chemmedchem, 5, 2010
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4R02
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![BU of 4r02 by Molmil](/molmil-images/mine/4r02) | yCP in complex with BSc4999 (alpha-Keto Phenylamide) | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-{(2S,3S)-1-[(2,4-dimethylphenyl)amino]-2-hydroxy-5-methyl-1-oxohexan-3-yl}-L-leucinamide, Probable proteasome subunit alpha type-7, ... | 著者 | Voss, C, Scholz, C, Knorr, S, Beck, P, Stein, M, Zall, A, Kuckelkorn, U, Kloetzel, P.-M, Groll, M, Hamacher, K, Schmidt, B. | 登録日 | 2014-07-29 | 公開日 | 2014-08-13 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | alpha-Keto Phenylamides as P1'-Extended Proteasome Inhibitors. Chemmedchem, 9, 2014
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6H39
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4QV1
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![BU of 4qv1 by Molmil](/molmil-images/mine/4qv1) | yCP beta5-M45A mutant | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | 登録日 | 2014-07-14 | 公開日 | 2015-02-04 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914. Structure, 23, 2015
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4Y8H
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![BU of 4y8h by Molmil](/molmil-images/mine/4y8h) | Yeast 20S proteasome in complex with N3-APAL-ep | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-02-16 | 公開日 | 2015-06-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors. J.Am.Chem.Soc., 137, 2015
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4Y77
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![BU of 4y77 by Molmil](/molmil-images/mine/4y77) | Yeast 20S proteasome in complex with Ac-LAF-ep | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAF-ep, CHLORIDE ION, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-02-13 | 公開日 | 2015-06-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors. J.Am.Chem.Soc., 137, 2015
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4Y7W
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![BU of 4y7w by Molmil](/molmil-images/mine/4y7w) | Yeast 20S proteasome in complex with Ac-LAE-ep | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAE-ep, CHLORIDE ION, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-02-16 | 公開日 | 2015-06-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors. J.Am.Chem.Soc., 137, 2015
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4Y80
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![BU of 4y80 by Molmil](/molmil-images/mine/4y80) | Yeast 20S proteasome in complex with Ac-LAI-ep | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAI-ep, CHLORIDE ION, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-02-16 | 公開日 | 2015-06-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors. J.Am.Chem.Soc., 137, 2015
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4YA5
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4LTC
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![BU of 4ltc by Molmil](/molmil-images/mine/4ltc) | Crystal structure of yeast 20S proteasome in complex with enone carmaphycin analogue 6 | 分子名称: | N-hexanoyl-L-valyl-N~1~-[(4S,5S,6R)-5-hydroxy-2,6-dimethyloctan-4-yl]-N~5~,N~5~-dimethyl-L-glutamamide, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | 著者 | Stein, M, Trivella, D.B.B, Groll, M. | 登録日 | 2013-07-23 | 公開日 | 2014-07-02 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Enzyme inhibition by hydroamination: design and mechanism of a hybrid carmaphycin-syringolin enone proteasome inhibitor. Chem.Biol., 21, 2014
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5CGH
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6HWF
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![BU of 6hwf by Molmil](/molmil-images/mine/6hwf) | Yeast 20S proteasome beta2-G45A mutant in complex with ONX 0914 | 分子名称: | (2~{S})-3-(4-methoxyphenyl)-~{N}-[(2~{S},3~{R})-4-methyl-3,4-bis(oxidanyl)-1-phenyl-pentan-2-yl]-2-[[(2~{S})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2018-10-11 | 公開日 | 2019-01-30 | 最終更新日 | 2024-01-24 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Structure-Based Design of Inhibitors Selective for Human Proteasome beta 2c or beta 2i Subunits. J.Med.Chem., 62, 2019
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4NO1
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![BU of 4no1 by Molmil](/molmil-images/mine/4no1) | yCP in complex with Z-Leu-Leu-Leu-B(OH)2 | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-leucinamide, Probable proteasome subunit alpha type-7, ... | 著者 | Stein, M.L, Cui, H, Beck, P, Dubiella, C, Voss, C, Krueger, A, Schmidt, B, Groll, M. | 登録日 | 2013-11-19 | 公開日 | 2014-02-12 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Systematic Comparison of Peptidic Proteasome Inhibitors Highlights the alpha-Ketoamide Electrophile as an Auspicious Reversible Lead Motif. Angew.Chem.Int.Ed.Engl., 53, 2014
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4RUR
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![BU of 4rur by Molmil](/molmil-images/mine/4rur) | Yeast 20S proteasome in complex with the alkaloid indolo-phakellin (4) | 分子名称: | (2E,3aR,14aS)-9-bromo-2-imino-1,2,3,5,6,14a-hexahydro-4H,8H-imidazo[4',5':5,6]pyrrolo[1',2':4,5]pyrazino[1,2-a]indol-8-one, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | 著者 | Beck, P, Lansdell, T.A, Hewlett, N.M, Tepe, J.J, Groll, M. | 登録日 | 2014-11-21 | 公開日 | 2014-12-10 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Indolo-Phakellins as beta 5-Specific Noncovalent Proteasome Inhibitors. Angew.Chem.Int.Ed.Engl., 54, 2015
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5CZA
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![BU of 5cza by Molmil](/molmil-images/mine/5cza) | Yeast 20S proteasome beta5-D166N mutant | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-07-31 | 公開日 | 2016-03-23 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome. Nat Commun, 7, 2016
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4NNN
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![BU of 4nnn by Molmil](/molmil-images/mine/4nnn) | yCP in complex with MG132 | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-hydroxy-4-methylpentan-2-yl]-L-leucinamide, Probable proteasome subunit alpha type-7, ... | 著者 | Stein, M.L, Cui, H, Beck, P, Dubiella, C, Voss, C, Krueger, A, Schmidt, B, Groll, M. | 登録日 | 2013-11-18 | 公開日 | 2014-02-12 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | 主引用文献 | Systematic Comparison of Peptidic Proteasome Inhibitors Highlights the alpha-Ketoamide Electrophile as an Auspicious Reversible Lead Motif. Angew.Chem.Int.Ed.Engl., 53, 2014
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5D0S
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4EU2
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![BU of 4eu2 by Molmil](/molmil-images/mine/4eu2) | Crystal structure of 20s proteasome with novel inhibitor K-7174 | 分子名称: | 1,4-bis[(4E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl]-1,4-diazepane, Proteasome component C1, Proteasome component C11, ... | 著者 | Kikuchi, J, Shibayama, N, Yamada, S, Wada, T, Nobuyoshi, M, Izumi, T, Akutsu, M, Kano, Y, Ohki, M, Sugiyama, K, Park, S.-Y, Furukawa, Y. | 登録日 | 2012-04-25 | 公開日 | 2013-05-01 | 最終更新日 | 2024-03-20 | 実験手法 | X-RAY DIFFRACTION (2.509 Å) | 主引用文献 | Homopiperazine derivatives as a novel class of proteasome inhibitors with a unique mode of proteasome binding. Plos One, 8, 2013
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4QVY
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![BU of 4qvy by Molmil](/molmil-images/mine/4qvy) | yCP beta5-A49T-mutant in complex with bortezomib | 分子名称: | CHLORIDE ION, MAGNESIUM ION, N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, ... | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | 登録日 | 2014-07-16 | 公開日 | 2015-02-04 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.51 Å) | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914. Structure, 23, 2015
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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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5L5H
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5L6B
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![BU of 5l6b by Molmil](/molmil-images/mine/5l6b) | Yeast 20S proteasome with mouse beta5i (1-138) and mouse beta6 (97-111; 118-133) in complex with ONX 0914 | 分子名称: | 1,2,4-trideoxy-4-methyl-2-{[N-(morpholin-4-ylacetyl)-L-alanyl-O-methyl-L-tyrosyl]amino}-1-phenyl-D-xylitol, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | 著者 | Groll, M, Huber, E.M. | 登録日 | 2016-05-28 | 公開日 | 2016-11-09 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i. EMBO J., 35, 2016
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5D0T
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![BU of 5d0t by Molmil](/molmil-images/mine/5d0t) | |
5L5U
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![BU of 5l5u by Molmil](/molmil-images/mine/5l5u) | Yeast 20S proteasome with human beta5i (1-138; V31M) and human beta6 (97-111; 118-133) in complex with epoxyketone inhibitor 17 | 分子名称: | 1,2,4-trideoxy-4-methyl-2-{[N-(morpholin-4-ylacetyl)-L-alanyl-O-methyl-L-tyrosyl]amino}-1-phenyl-D-xylitol, CHLORIDE ION, MAGNESIUM ION, ... | 著者 | Groll, M, Huber, E.M. | 登録日 | 2016-05-28 | 公開日 | 2016-11-09 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i. EMBO J., 35, 2016
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5D0X
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