4QZX
 
 | | yCP beta5-C63F mutant in complex with the epoxyketone inhibitor 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 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-29 | | 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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3D29
 | | Proteasome Inhibition by Fellutamide B | | 分子名称: | (3R)-3-HYDROXYDODECANOIC ACID, Fellutamide B, PRE10 isoform 1, ... | | 著者 | Groll, M, Hines, J, Fahnestock, M, Crews, M.C. | | 登録日 | 2008-05-07 | | 公開日 | 2008-06-10 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Proteasome Inhibition by Fellutamide B Induces Nerve Growth Factor Synthesis
Chem.Biol., 15, 2008
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4R3O
 | | Human Constitutive 20S Proteasome | | 分子名称: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | 著者 | Sacchettini, J.C, Harshbarger, W.H. | | 登録日 | 2014-08-16 | | 公開日 | 2015-01-28 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal Structure of the Human 20S Proteasome in Complex with Carfilzomib.
Structure, 23, 2015
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5FGF
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4Y8N
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4Y8Q
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4Y7X
 | | Yeast 20S proteasome in complex with Ac-PAA-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-PPA-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 (2.6 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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4Y8K
 | | Yeast 20S proteasome in complex with H-APLL-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, H-APLL-ep, ... | | 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 (2.6 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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4Y8I
 | | Yeast 20S proteasome in complex with Ac-PLL-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-PLL-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 (2.6 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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6HW3
 | | Yeast 20S proteasome 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, CHLORIDE ION, MAGNESIUM 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 (2.6 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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4Y6A
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4Y8G
 | | Yeast 20S proteasome in complex with N3-APnLL-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 (2.6 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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6HWB
 | | Yeast 20S proteasome in complex with 44b | | 分子名称: | (2~{S})-~{N}-[(2~{S},3~{R})-1-(4-cyclohexylcyclohexyl)-4-methyl-3,4-bis(oxidanyl)pentan-2-yl]-3-(4-methoxyphenyl)-2-[[(2~{S})-2-(2-morpholin-4-ium-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 (2.6 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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5BOU
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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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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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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
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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
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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
 | | 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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5L5V
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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
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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
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5L64
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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
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