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
 | | 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
 | | 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
 | | 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
 | | 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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6HTR
 | | Yeast 20S proteasome with human beta2c (S171G) in complex with 13 | | 分子名称: | (2~{S})-~{N}-[(2~{S})-1-[[(2~{S})-1-[4-(aminomethyl)phenyl]-4-methylsulfonyl-butan-2-yl]amino]-3-oxidanyl-1-oxidanylidene-propan-2-yl]-2-[[(2~{S})-2-azido-3-phenyl-propanoyl]amino]-4-methyl-pentanamide, MAGNESIUM ION, PROTEASOME SUBUNIT ALPHA TYPE-1, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2018-10-04 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.6 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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5D0T
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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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4Q1S
 | | Yeast 20S proteasome in Complex with Kendomycin | | 分子名称: | (5R,6R,7S,8R,9R,12S,13E,16S,18S,19R,20aR)-4,7,19-trihydroxy-2,6,8,12,14,16,18-heptamethyl-6,7,8,9,10,11,12,15,16,17,18,19,20,20a-tetradecahydro-1,19:5,9-diepoxybenzo[18]annulen-3(5H)-one, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | | 著者 | Beck, P, Heinemeyer, W, Spaeth, A, Elnakady, Y, Mueller, R, Groll, M. | | 登録日 | 2014-04-04 | | 公開日 | 2014-07-30 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Interactions of the natural product kendomycin and the 20S proteasome.
J.Mol.Biol., 426, 2014
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5L6C
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5L67
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5L5S
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5L5O
 | | Yeast 20S proteasome with human beta5i (1-138) and human beta6 (97-111; 118-133) in complex with epoxyketone inhibitor 16 | | 分子名称: | (2~{S})-3-(1~{H}-indol-3-yl)-~{N}-[(2~{S},3~{S},4~{R})-4-methyl-3,5-bis(oxidanyl)-1-phenyl-pentan-2-yl]-2-[[(2~{R})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, 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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6RGQ
 | | Human 20S Proteasome | | 分子名称: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | 著者 | Toste Rego, A, da Fonseca, P.C.A. | | 登録日 | 2019-04-17 | | 公開日 | 2019-09-04 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (2.6 Å) | | 主引用文献 | Characterization of Fully Recombinant Human 20S and 20S-PA200 Proteasome Complexes.
Mol.Cell, 76, 2019
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5FGE
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5FG9
 | | Yeast 20S proteasome beta2-T(-2)V mutant | | 分子名称: | MAGNESIUM ION, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2015-12-20 | | 公開日 | 2016-03-23 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.6 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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4QVQ
 | | yCP beta5-M45I 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 | 2014-07-15 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.6 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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4QWI
 | | yCP beta5-A49S-mutant in complex with carfilzomib | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | 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 (2.6 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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4QWL
 | | yCP beta5-A50V mutant in complex with carfilzomib | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | 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 (2.6 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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4QV7
 | | yCP beta5-A50V 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 (2.6 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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4QWG
 | | yCP beta5-A49V mutant in complex with carfilzomib | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | 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 (2.6 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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4QV9
 | | yCP beta5-C63F 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 (2.6 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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