4QLQ
 
 | | yCP in complex with tripeptidic epoxyketone inhibitor 8 | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N-(morpholin-4-ylacetyl)-L-alanyl-N-[(2S,4R)-1-cyclohexyl-5-hydroxy-4-methyl-3-oxopentan-2-yl]-O-methyl-L-tyrosinamide, ... | | 著者 | De Bruin, G, Huber, E, Xin, B, Van Rooden, E, Al-Ayed, K, Kim, K, Kisselev, A, Driessen, C, Van der Marel, G, Groll, M, Overkleeft, H. | | 登録日 | 2014-06-13 | | 公開日 | 2014-07-23 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structure-based design of beta 1i or beta 5i specific inhibitors of human immunoproteasomes
J.Med.Chem., 57, 2014
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4R18
 | | Ligand-induced Lys33-Thr1 crosslinking at subunit beta5 of the yeast 20S proteasome | | 分子名称: | ALPHA-AMINOBUTYRIC ACID, MAGNESIUM ION, PROTEASOME SUBUNIT ALPHA TYPE-1, ... | | 著者 | Dubiella, C, Cui, H, Gersch, M, Brouwer, A.J, Sieber, S.A, Krueger, A, Liskamp, R, Groll, M. | | 登録日 | 2014-08-04 | | 公開日 | 2014-10-15 | | 最終更新日 | 2023-12-06 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Selective inhibition of the immunoproteasome by ligand-induced crosslinking of the active site.
Angew.Chem.Int.Ed.Engl., 53, 2014
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4Y7Y
 | | Yeast 20S proteasome in complex with Ac-LAA-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAA-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 (2.4 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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4Y8L
 | | Yeast 20S proteasome in complex with Ac-APLL-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-APLL-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 (2.4 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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4Y70
 | | Yeast 20S proteasome in complex with Ac-LAV-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAV-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 (2.4 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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8T0M
 | | Proteasome 20S core particle from Pre1-1 Pre4-1 Double mutant | | 分子名称: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | 著者 | Walsh Jr, R.M, Rawson, S, Schnell, H, Velez, B, Hanna, J. | | 登録日 | 2023-06-01 | | 公開日 | 2023-09-06 | | 最終更新日 | 2023-10-25 | | 実験手法 | ELECTRON MICROSCOPY (2.4 Å) | | 主引用文献 | Structure of the preholoproteasome reveals late steps in proteasome core particle biogenesis.
Nat.Struct.Mol.Biol., 30, 2023
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5L5A
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5LF0
 | | Human 20S proteasome complex with Epoxomicin at 2.4 Angstrom | | 分子名称: | CHLORIDE ION, EPOXOMICIN (peptide inhibitor), MAGNESIUM ION, ... | | 著者 | Schrader, J, Henneberg, F, Mata, R, Tittmann, K, Schneider, T.R, Stark, H, Bourenkov, G, Chari, A. | | 登録日 | 2016-06-30 | | 公開日 | 2016-08-17 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.41 Å) | | 主引用文献 | The inhibition mechanism of human 20S proteasomes enables next-generation inhibitor design.
Science, 353, 2016
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3GPT
 | | Crystal structure of the yeast 20S proteasome in complex with Salinosporamide derivatives: slow substrate ligand | | 分子名称: | (2R,3S,4R)-2-[(S)-(1S)-cyclohex-2-en-1-yl(hydroxy)methyl]-4-(2-fluoroethyl)-3-hydroxy-3-methyl-5-oxopyrrolidine-2-carbaldehyde, Proteasome component C1, Proteasome component C11, ... | | 著者 | Groll, M, Macherla, V.R, Manam, R.R, Arthur, K.A.M, Potts, C.B. | | 登録日 | 2009-03-23 | | 公開日 | 2009-09-15 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.41 Å) | | 主引用文献 | Snapshots of the fluorosalinosporamide/20S complex offer mechanistic insights for fine tuning proteasome inhibition
J.Med.Chem., 52, 2009
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7B12
 | | HUMAN IMMUNOPROTEASOME 20S PARTICLE IN COMPLEX WITH [2-(3-ethylphenyl)-1-[(2S)-3-phenyl-2-[(pyrazin-2-yl)formamido]propanamido]ethyl]boronic acid | | 分子名称: | ((R)-2-(3-ethylphenyl)-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)ethyl)boronic acid, Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, ... | | 著者 | Musil, D, Klein, M, Crosignani, S. | | 登録日 | 2020-11-23 | | 公開日 | 2021-12-01 | | 最終更新日 | 2023-06-14 | | 実験手法 | X-RAY DIFFRACTION (2.43 Å) | | 主引用文献 | Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 ( beta 5i).
J.Med.Chem., 64, 2021
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4G4S
 | | Structure of Proteasome-Pba1-Pba2 Complex | | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide, Proteasome assembly chaperone 2, ... | | 著者 | Kish-Trier, E, Robinson, H, Stadtmueller, B.M, Hill, C.P. | | 登録日 | 2012-07-16 | | 公開日 | 2012-09-05 | | 最終更新日 | 2013-04-10 | | 実験手法 | X-RAY DIFFRACTION (2.49 Å) | | 主引用文献 | Structure of a Proteasome Pba1-Pba2 Complex: IMPLICATIONS FOR PROTEASOME ASSEMBLY, ACTIVATION, AND BIOLOGICAL FUNCTION.
J.Biol.Chem., 287, 2012
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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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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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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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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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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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5CGH
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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
 | | 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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5D0S
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4YA5
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6H39
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5CZ7
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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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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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