1RYP
 
 | | CRYSTAL STRUCTURE OF THE 20S PROTEASOME FROM YEAST AT 2.4 ANGSTROMS RESOLUTION | | Descriptor: | 20S PROTEASOME, MAGNESIUM ION | | Authors: | Groll, M, Ditzel, L, Loewe, J, Stock, D, Bochtler, M, Bartunik, H.D, Huber, R. | | Deposit date: | 1997-02-26 | | Release date: | 1998-04-15 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structure of 20S proteasome from yeast at 2.4 A resolution.
Nature, 386, 1997
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4R17
 | | Ligand-induced aziridine-formation at subunit beta5 of the yeast 20S proteasome | | Descriptor: | (2S,3S)-3-methylaziridine-2-carboxylic acid, MAGNESIUM ION, Proteasome subunit alpha type-1, ... | | Authors: | Dubiella, C, Cui, H, Gersch, M, Brouwer, A.J, Sieber, S.A, Krueger, A, Liskamp, R, Groll, M. | | Deposit date: | 2014-08-04 | | Release date: | 2014-10-15 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Selective inhibition of the immunoproteasome by ligand-induced crosslinking of the active site.
Angew.Chem.Int.Ed.Engl., 53, 2014
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8U7U
 | | Proteasome 20S Core Particle from Beta 3 D205 deletion | | Descriptor: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | Authors: | Walsh Jr, R.M, Rawson, S, Velez, B, Blickling, M, Razi, A, Hanna, J. | | Deposit date: | 2023-09-15 | | Release date: | 2024-04-17 | | Last modified: | 2024-04-24 | | Method: | ELECTRON MICROSCOPY (2.16 Å) | | Cite: | Mechanism of autocatalytic activation during proteasome assembly.
Nat.Struct.Mol.Biol., 2024
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1G65
 | | Crystal structure of epoxomicin:20s proteasome reveals a molecular basis for selectivity of alpha,beta-epoxyketone proteasome inhibitors | | Descriptor: | EPOXOMICIN (peptide inhibitor), MAGNESIUM ION, Proteasome component C1, ... | | Authors: | Groll, M, Kim, K.B, Kairies, N, Huber, R, Crews, C. | | Deposit date: | 2000-11-03 | | Release date: | 2000-11-27 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | Crystal Structure of Epoxomicin:20S Proteasome reveals a molecular basis for selectivity of alpha,beta-Epoxyketone Proteasome Inhibitors
J.Am.Chem.Soc., 122, 2000
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7AWE
 | | HUMAN IMMUNOPROTEASOME 20S PARTICLE IN COMPLEX WITH [(1R)-2-(1-benzofuran-3-yl)-1-{[(1S,2R,4R)-7-oxabicyclo[2.2.1]heptan-2-yl]formamido}ethyl]boronic acid | | Descriptor: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | Authors: | Musil, D, Klein, M. | | Deposit date: | 2020-11-06 | | Release date: | 2021-06-09 | | Last modified: | 2021-08-11 | | Method: | X-RAY DIFFRACTION (2.288 Å) | | Cite: | M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 ( beta 5i) Delivering Efficacy in Multiple Myeloma Models.
Mol.Cancer Ther., 20, 2021
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4QVP
 | | yCP beta5-M45T mutant in complex with bortezomib | | Descriptor: | CHLORIDE ION, MAGNESIUM ION, N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, ... | | Authors: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-15 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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6HWE
 | | Yeast 20S proteasome beta2-G45A mutant in complex with carfilzomib | | Descriptor: | (2~{S})-~{N}-[(2~{S})-1-[[(3~{R},4~{S})-2,6-dimethyl-2,3-bis(oxidanyl)heptan-4-yl]amino]-1-oxidanylidene-3-phenyl-propan-2-yl]-4-methyl-2-[[(2~{S})-2-(2-morpholin-4-ylethanoylamino)-4-phenyl-butanoyl]amino]pentanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2018-10-11 | | Release date: | 2019-01-30 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structure-Based Design of Inhibitors Selective for Human Proteasome beta 2c or beta 2i Subunits.
J.Med.Chem., 62, 2019
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5CZ4
 | | Yeast 20S proteasome at 2.3 A resolution | | Descriptor: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | 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 (2.3 Å) | | Cite: | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome.
Nat Commun, 7, 2016
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8T0M
 | | Proteasome 20S core particle from Pre1-1 Pre4-1 Double mutant | | Descriptor: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | Authors: | Walsh Jr, R.M, Rawson, S, Schnell, H, Velez, B, Hanna, J. | | Deposit date: | 2023-06-01 | | Release date: | 2023-09-06 | | Last modified: | 2023-10-25 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Structure of the preholoproteasome reveals late steps in proteasome core particle biogenesis.
Nat.Struct.Mol.Biol., 30, 2023
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5L5A
 | | Yeast 20S proteasome with human beta5i (1-138; R57T) | | Descriptor: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | 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 (2.4 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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3NZJ
 | | Crystal structure of yeast 20S proteasome in complex with ligand 2a | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Proteasome component C1, Proteasome component C11, ... | | 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: | 2010-07-16 | | Release date: | 2011-02-16 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | 20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A.
Chemmedchem, 5, 2010
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4R18
 | | Ligand-induced Lys33-Thr1 crosslinking at subunit beta5 of the yeast 20S proteasome | | Descriptor: | ALPHA-AMINOBUTYRIC ACID, MAGNESIUM ION, PROTEASOME SUBUNIT ALPHA TYPE-1, ... | | Authors: | Dubiella, C, Cui, H, Gersch, M, Brouwer, A.J, Sieber, S.A, Krueger, A, Liskamp, R, Groll, M. | | Deposit date: | 2014-08-04 | | Release date: | 2014-10-15 | | Last modified: | 2023-12-06 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Selective inhibition of the immunoproteasome by ligand-induced crosslinking of the active site.
Angew.Chem.Int.Ed.Engl., 53, 2014
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4QLQ
 | | yCP in complex with tripeptidic epoxyketone inhibitor 8 | | Descriptor: | 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, ... | | Authors: | 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. | | Deposit date: | 2014-06-13 | | Release date: | 2014-07-23 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structure-based design of beta 1i or beta 5i specific inhibitors of human immunoproteasomes
J.Med.Chem., 57, 2014
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4Y7Y
 | | Yeast 20S proteasome in complex with Ac-LAA-ep | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAA-ep, CHLORIDE 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 (2.4 Å) | | Cite: | 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 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-APLL-ep, CHLORIDE 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 (2.4 Å) | | Cite: | 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 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAV-ep, CHLORIDE ION, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2015-02-13 | | Release date: | 2015-06-17 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors.
J.Am.Chem.Soc., 137, 2015
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1G0U
 | | A GATED CHANNEL INTO THE PROTEASOME CORE PARTICLE | | Descriptor: | MAGNESIUM ION, PROTEASOME COMPONENT C1, PROTEASOME COMPONENT C11, ... | | Authors: | Groll, M, Bajorek, M, Kohler, A, Moroder, L, Rubin, D.M, Huber, R, Glickman, M.H, Finley, D. | | Deposit date: | 2000-10-09 | | Release date: | 2000-11-06 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | A gated channel into the proteasome core particle.
Nat.Struct.Biol., 7, 2000
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3GPT
 | | Crystal structure of the yeast 20S proteasome in complex with Salinosporamide derivatives: slow substrate ligand | | Descriptor: | (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, ... | | Authors: | Groll, M, Macherla, V.R, Manam, R.R, Arthur, K.A.M, Potts, C.B. | | Deposit date: | 2009-03-23 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.41 Å) | | Cite: | 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 | | Descriptor: | ((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, ... | | Authors: | Musil, D, Klein, M, Crosignani, S. | | Deposit date: | 2020-11-23 | | Release date: | 2021-12-01 | | Last modified: | 2023-06-14 | | Method: | X-RAY DIFFRACTION (2.43 Å) | | Cite: | 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 | | Descriptor: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide, Proteasome assembly chaperone 2, ... | | Authors: | Kish-Trier, E, Robinson, H, Stadtmueller, B.M, Hill, C.P. | | Deposit date: | 2012-07-16 | | Release date: | 2012-09-05 | | Last modified: | 2013-04-10 | | Method: | X-RAY DIFFRACTION (2.49 Å) | | Cite: | Structure of a Proteasome Pba1-Pba2 Complex: IMPLICATIONS FOR PROTEASOME ASSEMBLY, ACTIVATION, AND BIOLOGICAL FUNCTION.
J.Biol.Chem., 287, 2012
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3GPW
 | | Crystal structure of the yeast 20S proteasome in complex with Salinosporamide derivatives: irreversible inhibitor ligand | | Descriptor: | (3AR,6R,6AS)-6-((S)-((S)-CYCLOHEX-2-ENYL)(HYDROXY)METHYL)-6A-METHYL-4-OXO-HEXAHYDRO-2H-FURO[3,2-C]PYRROLE-6-CARBALDEHYDE, Proteasome component C1, Proteasome component C11, ... | | Authors: | Groll, M, Macherla, V.R, Manam, R.R, Arthur, K.A.M, Potts, C.B. | | Deposit date: | 2009-03-23 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Snapshots of the fluorosalinosporamide/20S complex offer mechanistic insights for fine tuning proteasome inhibition
J.Med.Chem., 52, 2009
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5CZ7
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5L5F
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3HYE
 | | Crystal structure of 20S proteasome in complex with hydroxylated salinosporamide | | Descriptor: | (2R,3S,4R)-2-[(S)-(1S)-cyclohex-2-en-1-yl(hydroxy)methyl]-3-hydroxy-4-(2-hydroxyethyl)-3-methyl-5-oxopyrrolidine-2-carbaldehyde, Proteasome component C1, Proteasome component C11, ... | | Authors: | Groll, M, Arthur, K.A.M, Macherla, V.R, Manam, R.R, Potts, B.C. | | Deposit date: | 2009-06-22 | | Release date: | 2009-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Snapshots of the fluorosalinosporamide/20S complex offer mechanistic insights for fine tuning proteasome inhibition
J.Med.Chem., 52, 2009
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5LAI
 | | Ligand-induced aziridine-formation at the yeast proteasomal subunit beta5 by sulfonate esters | | Descriptor: | (2S,3S)-3-methylaziridine-2-carboxylic acid, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | Authors: | Groll, M, Dubiella, C, Cui, H. | | Deposit date: | 2016-06-14 | | Release date: | 2017-04-26 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Tunable Probes with Direct Fluorescence Signals for the Constitutive and Immunoproteasome.
Angew. Chem. Int. Ed. Engl., 55, 2016
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