5NIF
 
 | | Yeast 20S proteasome in complex with Blm-pep activator | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, GLYCEROL, ... | | 著者 | Witkowska, J, Grudnik, P, Golik, P, Dubin, G, Jankowska, E. | | 登録日 | 2017-03-23 | | 公開日 | 2017-08-02 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal structure of a low molecular weight activator Blm-pep with yeast 20S proteasome - insights into the enzyme activation mechanism.
Sci Rep, 7, 2017
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6G8N
 | | Yeast 20S proteasome in complex with Cystargolide B Derivative 2 | | 分子名称: | (2~{S},3~{S})-3-methyl-2-[(1~{R})-2-[[(2~{S})-3-methyl-1-[[(2~{S})-3-methyl-1-oxidanylidene-1-phenylmethoxy-butan-2-yl] amino]-1-oxidanylidene-butan-2-yl]amino]-1-oxidanyl-2-oxidanylidene-ethyl]pentanoic acid, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Groll, M, Tello-Aburto, R. | | 登録日 | 2018-04-09 | | 公開日 | 2018-09-12 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Design, synthesis, and evaluation of cystargolide-based beta-lactones as potent proteasome inhibitors.
Eur J Med Chem, 157, 2018
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6HVW
 | | Yeast 20S proteasome with human beta2i (1-53) in complex with 43 | | 分子名称: | (2~{S})-~{N}-[(2~{S},3~{R})-1-[(4~{a}~{S},8~{a}~{S})-1,2,3,4,4~{a},5,6,7,8,8~{a}-decahydronaphthalen-2-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-(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 (3 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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4NO6
 | | yCP in complex with Z-Leu-Leu-Leu-vinylsulfone | | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(3S)-5-methyl-1-(methylsulfonyl)hexan-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 (3 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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4V7O
 | | Proteasome Activator Complex | | 分子名称: | Proteasome activator BLM10, Proteasome component C1, Proteasome component C11, ... | | 著者 | Hill, C.P, Whitby, F.G. | | 登録日 | 2009-12-22 | | 公開日 | 2014-07-09 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (3.005 Å) | | 主引用文献 | Structure of a Blm10 complex reveals common mechanisms for proteasome binding and gate opening.
Mol.Cell, 37, 2010
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8RHJ
 | | Yeast 20S proteasome in complex with a macrocyclic oxindole epoxyketone (compound 5) | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Macrocyclic oxindole epoxyketone, ... | | 著者 | Goetz, M.G, Godwin, K, Price, R, Dorn, R, Merrill-Steskal, G, Hansen, H, Klemmer, W, Produturi, G, Rocha, M, Palmer, M, Molacek, L, Strater, Z, Groll, M. | | 登録日 | 2023-12-15 | | 公開日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.
Acs Med.Chem.Lett., 15, 2024
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4QV0
 | | yCP beta5-A49T-A50V-double 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 (3.1 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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4INU
 | | Yeast 20S proteasome in complex with the vinyl sulfone LU112 | | 分子名称: | N3Phe-Phe(4-NH2CH2)-Leu-Phe(4-NH2CH2)-methyl vinyl sulfone, bound form, Proteasome component C1, ... | | 著者 | Geurink, P.P, van der Linden, W.A, Mirabella, A.C, Gallastegui, N, de Bruin, G, Blom, A.E.M, Voges, M.J, Mock, E.D, Florea, B.I, van der Marel, G.A, Driessen, C, van der Stelt, M, Groll, M, Overkleeft, H.S, Kisselev, A.F. | | 登録日 | 2013-01-06 | | 公開日 | 2013-01-30 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Incorporation of Non-natural Amino Acids Improves Cell Permeability and Potency of Specific Inhibitors of Proteasome Trypsin-like Sites.
J.Med.Chem., 56, 2013
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6HVS
 | | Yeast 20S proteasome with human beta2i (1-53) in complex with 18 | | 分子名称: | (2~{S})-~{N}-[2-[[(2~{S})-1-[4-(aminomethyl)phenyl]-4-methylsulfonyl-butan-2-yl]amino]-2-oxidanylidene-ethyl]-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 (3.1 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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4JT0
 | | Yeast 20S proteasome in complex with the dimerized linear mimetic of TMC-95A - yCP:4a | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | | 著者 | Desvergne, A, Genin, E, Marechal, X, Gallastegui, N, Dufau, L, Richy, N, Groll, M, Vidal, J, Reboud-Ravaux, M. | | 登録日 | 2013-03-22 | | 公開日 | 2013-05-01 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.
J.Med.Chem., 56, 2013
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3MG4
 | | Structure of yeast 20S proteasome with Compound 1 | | 分子名称: | (2S)-2-amino-N-[(1S)-1-({(1S)-1-[(4-methylbenzyl)carbamoyl]-3-phenylpropyl}carbamoyl)-3-phenylpropyl]-4-phenylbutanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, ... | | 著者 | Sintchak, M.D. | | 登録日 | 2010-04-05 | | 公開日 | 2011-04-27 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3.11 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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3WXR
 | | Yeast 20S proteasome with a mutation of alpha7 subunit | | 分子名称: | Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, ... | | 著者 | Yashiroda, H, Toda, Y, Otsu, S, Takagi, K, Mizushima, T, Murata, S. | | 登録日 | 2014-08-06 | | 公開日 | 2014-10-22 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (3.15 Å) | | 主引用文献 | N-terminal alpha 7 deletion of the proteasome 20S core particle substitutes for yeast PI31 function
Mol.Cell.Biol., 35, 2015
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7LS6
 | | Cryo-EM structure of Pre-15S proteasome core particle assembly intermediate purified from Pre3-1 proteasome mutant (G34D) | | 分子名称: | Proteasome assembly chaperone 2, Proteasome chaperone 1, Proteasome maturation factor UMP1, ... | | 著者 | Schnell, H.M, Walsh Jr, R.M, Rawson, S, Hanna, J.W. | | 登録日 | 2021-02-17 | | 公開日 | 2021-04-14 | | 最終更新日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (3.17 Å) | | 主引用文献 | Structures of chaperone-associated assembly intermediates reveal coordinated mechanisms of proteasome biogenesis.
Nat.Struct.Mol.Biol., 28, 2021
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8RHL
 | | Yeast 20S proteasome in complex with a linear biarylether epoxyketone (compound 15a) | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, Linear biarylether epoxyketone, ... | | 著者 | Goetz, M.G, Godwin, K, Price, R, Dorn, R, Merrill-Steskal, G, Hansen, H, Klemmer, W, Produturi, G, Rocha, M, Palmer, M, Molacek, L, Strater, Z, Groll, M. | | 登録日 | 2023-12-15 | | 公開日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.
Acs Med.Chem.Lett., 15, 2024
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1FNT
 | | CRYSTAL STRUCTURE OF THE 20S PROTEASOME FROM YEAST IN COMPLEX WITH THE PROTEASOME ACTIVATOR PA26 FROM TRYPANOSOME BRUCEI AT 3.2 ANGSTROMS RESOLUTION | | 分子名称: | MAGNESIUM ION, PROTEASOME ACTIVATOR PROTEIN PA26, PROTEASOME COMPONENT C1, ... | | 著者 | Whitby, F.G, Masters, E, Kramer, L, Knowlton, J.R, Yao, Y, Wang, C.C, Hill, C.P. | | 登録日 | 2000-08-23 | | 公開日 | 2001-04-11 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structural basis for the activation of 20S proteasomes by 11S regulators.
Nature, 408, 2000
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1Z7Q
 | | Crystal structure of the 20s proteasome from yeast in complex with the proteasome activator PA26 from Trypanosome brucei at 3.2 angstroms resolution | | 分子名称: | Potential proteasome component C5, Proteasome component C1, Proteasome component C11, ... | | 著者 | Forster, A, Whitby, F.G, Hill, C.P. | | 登録日 | 2005-03-26 | | 公開日 | 2005-08-09 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (3.22 Å) | | 主引用文献 | The 1.9 A structure of a proteasome-11S activator complex and implications for proteasome-PAN/PA700 interactions.
Mol.Cell, 18, 2005
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8BW1
 | | Yeast 20S proteasome in complex with an engineered fellutamide derivative (C14QAL) | | 分子名称: | 3-PYRIDIN-4-YL-2,4-DIHYDRO-INDENO[1,2-.C.]PYRAZOLE, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Bozhueyuek, K.A.J, Praeve, L, Kegler, C, Kaiser, S, Shi, Y, Kuttenlochner, W, Schenk, L, Groll, M, Hochberg, G.K.A, Bode, H.B. | | 登録日 | 2022-12-06 | | 公開日 | 2023-12-20 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | | 主引用文献 | Evolution-inspired engineering of nonribosomal peptide synthetases.
Science, 383, 2024
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3UN4
 | | Yeast 20S proteasome in complex with PR-957 (morpholine) | | 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, 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 (3.4 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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6HV7
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7LSX
 | | Cryo-EM structure of 13S proteasome core particle assembly intermediate purified from Pre3-1 proteasome mutant (G34D) | | 分子名称: | Proteasome assembly chaperone 2, Proteasome chaperone 1, Proteasome maturation factor UMP1, ... | | 著者 | Schnell, H.M, Walsh Jr, R.M, Rawson, S, Hanna, J.W. | | 登録日 | 2021-02-18 | | 公開日 | 2021-04-14 | | 最終更新日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (3.61 Å) | | 主引用文献 | Structures of chaperone-associated assembly intermediates reveal coordinated mechanisms of proteasome biogenesis.
Nat.Struct.Mol.Biol., 28, 2021
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6J2X
 | | Yeast proteasome in resting state (C1-a) | | 分子名称: | 26S PROTEASE REGULATORY SUBUNIT 4 HOMOLOG, 26S PROTEASOME REGULATORY SUBUNIT RPN5, 26S proteasome complex subunit SEM1, ... | | 著者 | Cong, Y. | | 登録日 | 2019-01-03 | | 公開日 | 2019-03-13 | | 最終更新日 | 2019-11-06 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Structural Snapshots of 26S Proteasome Reveal Tetraubiquitin-Induced Conformations.
Mol. Cell, 73, 2019
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6AVO
 | | Cryo-EM structure of human immunoproteasome with a novel noncompetitive inhibitor that selectively inhibits activated lymphocytes | | 分子名称: | N~1~-{2-[([1,1'-biphenyl]-3-carbonyl)amino]ethyl}-N~4~-tert-butyl-N~2~-(3-phenylpropanoyl)-L-aspartamide, Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, ... | | 著者 | Li, H, Santos, R, Bai, L. | | 登録日 | 2017-09-04 | | 公開日 | 2017-12-06 | | 最終更新日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Structure of human immunoproteasome with a reversible and noncompetitive inhibitor that selectively inhibits activated lymphocytes.
Nat Commun, 8, 2017
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6J2Q
 | | Yeast proteasome in Ub-accepted state (C1-b) | | 分子名称: | 26S protease regulatory subunit 4 homolog, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B homolog, ... | | 著者 | Cong, Y. | | 登録日 | 2019-01-02 | | 公開日 | 2019-03-13 | | 最終更新日 | 2019-04-10 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Structural Snapshots of 26S Proteasome Reveal Tetraubiquitin-Induced Conformations.
Mol. Cell, 73, 2019
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5MP9
 | | 26S proteasome in presence of ATP (s1) | | 分子名称: | 26S protease regulatory subunit 4 homolog, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B homolog, ... | | 著者 | Wehmer, M, Rudack, T, Beck, F, Aufderheide, A, Pfeifer, G, Plitzko, J.M, Foerster, F, Schulten, K, Baumeister, W, Sakata, E. | | 登録日 | 2016-12-16 | | 公開日 | 2017-03-08 | | 最終更新日 | 2024-05-15 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Structural insights into the functional cycle of the ATPase module of the 26S proteasome.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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6FVT
 | | 26S proteasome, s1 state | | 分子名称: | 26S proteasome complex subunit SEM1, 26S proteasome regulatory subunit 4 homolog, 26S proteasome regulatory subunit 6A, ... | | 著者 | Eisele, M.R, Reed, R.G, Rudack, T, Schweitzer, A, Beck, F, Nagy, I, Pfeifer, G, Plitzko, J.M, Baumeister, W, Tomko, R.J, Sakata, E. | | 登録日 | 2018-03-05 | | 公開日 | 2018-08-22 | | 最終更新日 | 2024-05-08 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Expanded Coverage of the 26S Proteasome Conformational Landscape Reveals Mechanisms of Peptidase Gating.
Cell Rep, 24, 2018
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