5BOU
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5bou by Molmil](/molmil-images/mine/5bou) | |
3OEU
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![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
|
|
3MG6
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![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
|
|
4NNW
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4nnw by Molmil](/molmil-images/mine/4nnw) | yCP in complex with Z-Leu-Leu-Leu-ketoaldehyde | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2R,3S)-1,2-dihydroxy-5-methylhexan-3-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 | 2013-11-19 | 公開日 | 2014-02-12 | 最終更新日 | 2024-03-13 | 実験手法 | X-RAY DIFFRACTION (2.6 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
|
|
8OHZ
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8ohz by Molmil](/molmil-images/mine/8ohz) | Yeast 20S proteasome in complex with a photoswitchable cepafungin derivative (transCep1) | 分子名称: | (2~{S},3~{R})-2-[2-[4-[2-(4-ethylphenyl)hydrazinyl]phenyl]ethanoylamino]-~{N}-[(5~{S},8~{S},10~{S})-5-methyl-10-oxidanyl-2,7-bis(oxidanylidene)-1,6-diazacyclododec-8-yl]-3-oxidanyl-butanamide, CHLORIDE ION, MAGNESIUM ION, ... | 著者 | Morstein, J, Amatuni, A, Schuster, A, Kuttenlochner, W, Ko, T, Groll, M, Adibekian, A, Renata, H, Trauner, D.H. | 登録日 | 2023-03-21 | 公開日 | 2023-12-27 | 最終更新日 | 2024-02-21 | 実験手法 | X-RAY DIFFRACTION (2.65 Å) | 主引用文献 | Optical Control of Proteasomal Protein Degradation with a Photoswitchable Lipopeptide. Angew.Chem.Int.Ed.Engl., 63, 2024
|
|
3SDI
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![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
|
|
3MG0
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![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
|
|
5L5V
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l5v by Molmil](/molmil-images/mine/5l5v) | |
3UN8
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3un8 by Molmil](/molmil-images/mine/3un8) | Yeast 20S proteasome in complex with PR-957 (epoxide) | 分子名称: | 2-(acetylamino)-4,5-anhydro-1,2-dideoxy-4-methyl-1-phenyl-D-xylitol, Proteasome component C1, Proteasome component C11, ... | 著者 | Huber, E, Basler, M, Schwab, R, Heinemeyer, W, Kirk, C, Groettrup, M, Groll, M. | 登録日 | 2011-11-15 | 公開日 | 2012-02-29 | 最終更新日 | 2023-09-13 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Immuno- and constitutive proteasome crystal structures reveal differences in substrate and inhibitor specificity. Cell(Cambridge,Mass.), 148, 2012
|
|
5CZ6
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5cz6 by Molmil](/molmil-images/mine/5cz6) | Yeast 20S proteasome beta5-T1A mutant in complex with Syringolin A, propeptide expressed in trans | 分子名称: | (2S)-2-[[(2S)-1-[[(5S,8S,9E)-2,7-dioxo-5-propan-2-yl-1,6-diazacyclododeca-3,9-dien-8-yl]amino]-3-methyl-1-oxo-butan-2-yl]carbamoylamino]-3-methyl-butanoic acid, CHLORIDE ION, MAGNESIUM ION, ... | 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 (2.7 Å) | 主引用文献 | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome. Nat Commun, 7, 2016
|
|
5L64
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l64 by Molmil](/molmil-images/mine/5l64) | |
6HVY
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6hvy by Molmil](/molmil-images/mine/6hvy) | Yeast 20S proteasome in complex with 5 (7- and 6-membered ring) | 分子名称: | (2~{S})-~{N}-[(2~{S},3~{R})-1-[(1~{S},4~{a}~{S},8~{a}~{R})-1,2,3,4,4~{a},5,6,7,8,8~{a}-decahydronaphthalen-1-yl]-4-methyl-3,4-bis(oxidanyl)pentan-2-yl]-3-(4-methoxyphenyl)-2-[[(2~{S})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, (2~{S})-~{N}-[(2~{S},3~{S},4~{R})-1-[(1~{S},4~{a}~{S},8~{a}~{R})-1,2,3,4,4~{a},5,6,7,8,8~{a}-decahydronaphthalen-1-yl]-4-methyl-3,5-bis(oxidanyl)pentan-2-yl]-3-(4-methoxyphenyl)-2-[[(2~{S})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | 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 (2.7 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
|
|
5L60
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l60 by Molmil](/molmil-images/mine/5l60) | |
5L69
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l69 by Molmil](/molmil-images/mine/5l69) | Yeast 20S proteasome with mouse beta5i (1-138) and mouse 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 (2.7 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
|
|
5L63
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l63 by Molmil](/molmil-images/mine/5l63) | Yeast 20S proteasome with human beta5c (1-138) 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, 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 (2.7 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
|
|
5L5Z
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l5z by Molmil](/molmil-images/mine/5l5z) | |
4X6Z
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4x6z by Molmil](/molmil-images/mine/4x6z) | Yeast 20S proteasome in complex with PR-VI modulator | 分子名称: | (4S)-2-METHYL-2,4-PENTANEDIOL, GLYCEROL, MAGNESIUM ION, ... | 著者 | Rostankowski, R, Witkowska, J, Borek, D, Otwinowski, Z, Jankowska, E. | 登録日 | 2014-12-09 | 公開日 | 2015-12-23 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | Crystal structures revealed the common place of binding of low-molecular
mass activators with the 20S proteasome To Be Published
|
|
5L52
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l52 by Molmil](/molmil-images/mine/5l52) | |
5L5Y
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5l5y by Molmil](/molmil-images/mine/5l5y) | |
5FGA
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5fga by Molmil](/molmil-images/mine/5fga) | |
5FG7
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5fg7 by Molmil](/molmil-images/mine/5fg7) | Yeast 20S proteasome beta2-T1A 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 | 2015-12-20 | 公開日 | 2016-03-23 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | 主引用文献 | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome. Nat Commun, 7, 2016
|
|
5M2B
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5m2b by Molmil](/molmil-images/mine/5m2b) | |
5FHS
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5fhs by Molmil](/molmil-images/mine/5fhs) | |
4QV4
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4qv4 by Molmil](/molmil-images/mine/4qv4) | yCP beta5-M45T 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 (2.7 Å) | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914. Structure, 23, 2015
|
|
3SDK
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![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
|
|