4Y8S
 
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4Y8R
 | | Yeast 20S proteasome beta2-H116D mutant | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2015-02-16 | | Release date: | 2015-06-17 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors.
J.Am.Chem.Soc., 137, 2015
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4YA9
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4YA7
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4Y74
 | | Yeast 20S proteasome in complex with Ac-LAL-ep | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAL-ep, CHLORIDE ION, ... | | Authors: | Groll, M, Huber, E.M. | | Deposit date: | 2015-02-13 | | Release date: | 2015-06-17 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors.
J.Am.Chem.Soc., 137, 2015
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4Y84
 | | Yeast 20S proteasome in complex with N3-A(4,4-F2P)nLL-ep | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2015-02-16 | | Release date: | 2015-06-17 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors.
J.Am.Chem.Soc., 137, 2015
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5CZ6
 | | Yeast 20S proteasome beta5-T1A mutant in complex with Syringolin A, propeptide expressed in trans | | Descriptor: | (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, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2015-07-31 | | Release date: | 2016-03-23 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome.
Nat Commun, 7, 2016
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3NZX
 | | Crystal structure of the yeast 20S proteasome in complex with ligand 2c | | Descriptor: | Proteasome component C1, Proteasome component C11, Proteasome component C5, ... | | Authors: | Groll, M, Gallastegui, N, Marechal, X, Le Ravalec, V, Basse, N, Richy, N, Genin, E, Huber, R, Moroder, M, Vidal, V, Reboud-Ravaux, M. | | Deposit date: | 2010-07-17 | | Release date: | 2011-02-16 | | Last modified: | 2023-12-06 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A.
Chemmedchem, 5, 2010
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5L5V
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4NO8
 | | yCP in complex with Z-Leu-Leu-Leu-ketoamide | | Descriptor: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S,3S)-2-hydroxy-5-methyl-1-oxo-1-(phenylamino)hexan-3-yl]-L-leucinamide, Probable proteasome subunit alpha type-7, ... | | Authors: | Stein, M.L, Cui, H, Beck, P, Dubiella, C, Voss, C, Krueger, A, Schmidt, B, Groll, M. | | Deposit date: | 2013-11-19 | | Release date: | 2014-02-12 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 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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6G7F
 | | Yeast 20S proteasome in complex with Cystargolide B | | Descriptor: | CHLORIDE ION, Cystargolide B- bound form, MAGNESIUM ION, ... | | Authors: | Groll, M, Tello-Aburto, R. | | Deposit date: | 2018-04-05 | | Release date: | 2018-09-12 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Design, synthesis, and evaluation of cystargolide-based beta-lactones as potent proteasome inhibitors.
Eur J Med Chem, 157, 2018
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5FGG
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5L64
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3UN8
 | | Yeast 20S proteasome in complex with PR-957 (epoxide) | | Descriptor: | 2-(acetylamino)-4,5-anhydro-1,2-dideoxy-4-methyl-1-phenyl-D-xylitol, Proteasome component C1, Proteasome component C11, ... | | Authors: | Huber, E, Basler, M, Schwab, R, Heinemeyer, W, Kirk, C, Groettrup, M, Groll, M. | | Deposit date: | 2011-11-15 | | Release date: | 2012-02-29 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Immuno- and constitutive proteasome crystal structures reveal differences in substrate and inhibitor specificity.
Cell(Cambridge,Mass.), 148, 2012
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8CVR
 | | Human 20S proteasome with MG-132 | | Descriptor: | N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide, Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, ... | | Authors: | Zhao, J. | | Deposit date: | 2022-05-18 | | Release date: | 2022-11-02 | | Last modified: | 2024-06-12 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Structural insights into the human PA28-20S proteasome enabled by efficient tagging and purification of endogenous proteins.
Proc.Natl.Acad.Sci.USA, 119, 2022
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6G8M
 | | Yeast 20S proteasome in complex with Cystargolide B Derivative 1 | | Descriptor: | (2~{S},3~{R})-4-[[(2~{S})-3-methyl-1-[[(2~{S})-3-methyl-1-oxidanylidene-1-phenylmethoxy-butan-2-yl]amino]-1-oxidanylidene-butan-2-yl]amino]-3-oxidanyl-4-oxidanylidene-2-propan-2-yl-butanoic acid, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Groll, M, Tello-Aburto, R. | | Deposit date: | 2018-04-09 | | Release date: | 2018-09-12 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Design, synthesis, and evaluation of cystargolide-based beta-lactones as potent proteasome inhibitors.
Eur J Med Chem, 157, 2018
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5L63
 | | Yeast 20S proteasome with human beta5c (1-138) and human beta6 (97-111; 118-133) in complex with epoxyketone inhibitor 17 | | Descriptor: | 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, ... | | Authors: | Groll, M, Huber, E.M. | | Deposit date: | 2016-05-28 | | Release date: | 2016-11-09 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i.
EMBO J., 35, 2016
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5L5Z
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5L60
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5L69
 | | Yeast 20S proteasome with mouse beta5i (1-138) and mouse beta6 (97-111; 118-133) in complex with epoxyketone inhibitor 16 | | Descriptor: | (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, ... | | Authors: | Groll, M, Huber, E.M. | | Deposit date: | 2016-05-28 | | Release date: | 2016-11-09 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i.
EMBO J., 35, 2016
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5FGA
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5FG7
 | | Yeast 20S proteasome beta2-T1A mutant | | Descriptor: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2015-12-20 | | Release date: | 2016-03-23 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome.
Nat Commun, 7, 2016
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5FHS
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5L52
 | | Yeast 20S proteasome in complex with epoxyketone inhibitor 14 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Groll, M, Huber, E.M. | | Deposit date: | 2016-05-27 | | Release date: | 2016-11-09 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i.
EMBO J., 35, 2016
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4INR
 | | Yeast 20S proteasome in complex with the vinyl sulfone LU102 | | Descriptor: | N3Phe-Leu-Leu-Phe(4-NH2CH2)-methyl vinyl sulfone, bound form, Proteasome component C1, ... | | Authors: | 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. | | Deposit date: | 2013-01-06 | | Release date: | 2013-01-30 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 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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