5CGG
 
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5D0V
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5CZ9
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4JSU
 | | Yeast 20S proteasome in complex with the dimerized linear mimetic of TMC-95A - yCP:3a | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | | Authors: | Desvergne, A, Genin, E, Marechal, X, Gallastegui, N, Dufau, L, Richy, N, Groll, M, Vidal, J, Reboud-Ravaux, M. | | Deposit date: | 2013-03-22 | | Release date: | 2013-05-01 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | 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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4NO9
 | | yCP in complex with Z-Leu-Leu-Leu-epoxyketone | | Descriptor: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2R,3S,4S)-1,3-dihydroxy-2,6-dimethylheptan-4-yl]-L-leucinamide, N-[(benzyloxy)carbonyl]-L-leucyl-N-{(1R,2S)-1-hydroxy-4-methyl-1-[(2R)-2-methyloxiran-2-yl]pentan-2-yl}-L-leucinamide, ... | | 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: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.9 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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8OI1
 | | Yeast 20S proteasome in complex with a photoswitchable cepafungin derivative (transCep4) | | Descriptor: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | Authors: | Morstein, J, Amatuni, A, Schuster, A, Kuttenlochner, W, Ko, T, Groll, M, Adibekian, A, Renata, H, Trauner, D.H. | | Deposit date: | 2023-03-21 | | Release date: | 2023-12-27 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | Optical Control of Proteasomal Protein Degradation with a Photoswitchable Lipopeptide.
Angew.Chem.Int.Ed.Engl., 63, 2024
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8QZ9
 | | Human 20S proteasome assembly intermediate structure 4 | | Descriptor: | Proteasome assembly chaperone 1, Proteasome assembly chaperone 2, Proteasome maturation protein, ... | | Authors: | Schulman, B.A, Hanna, J.W, Harper, J.W, Adolf, F, Du, J, Rawson, S.D, Walsh Jr, R.M, Goodall, E.A. | | Deposit date: | 2023-10-26 | | Release date: | 2024-02-21 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (2.95 Å) | | Cite: | Visualizing chaperone-mediated multistep assembly of the human 20S proteasome.
Nat.Struct.Mol.Biol., 2024
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7TEO
 | | Cryo-EM structure of the 20S Alpha 3 Deletion proteasome core particle in complex with FUB1 | | Descriptor: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-4, ... | | Authors: | Walsh Jr, R.M, Rawson, S, Schnell, H.M, Hanna, J. | | Deposit date: | 2022-01-05 | | Release date: | 2022-08-10 | | Last modified: | 2024-02-28 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Yeast PI31 inhibits the proteasome by a direct multisite mechanism.
Nat.Struct.Mol.Biol., 29, 2022
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6HV4
 | | Yeast 20S proteasome with human beta2i (1-53) in complex with ONX 0914 | | Descriptor: | (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, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2018-10-10 | | Release date: | 2019-01-30 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (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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8T08
 | | Preholo-Proteasome from Pre1-1 Pre4-1 Double Mutant | | Descriptor: | Proteasome assembly chaperone 2, Proteasome chaperone 1, Proteasome maturation factor UMP1, ... | | Authors: | Walsh Jr, R.M, Rawson, S, Schnell, H, Velez, B, Hanna, J. | | Deposit date: | 2023-05-31 | | Release date: | 2023-09-06 | | Last modified: | 2023-10-25 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structure of the preholoproteasome reveals late steps in proteasome core particle biogenesis.
Nat.Struct.Mol.Biol., 30, 2023
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3E47
 | | Crystal Structure of the Yeast 20S Proteasome in Complex with Homobelactosin C | | Descriptor: | Proteasome component C1, Proteasome component C11, Proteasome component C5, ... | | Authors: | Groll, M, Larionov, O.V, de Meijere, A. | | Deposit date: | 2008-08-10 | | Release date: | 2008-09-02 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Inhibitor-binding mode of homobelactosin C to proteasomes: new insights into class I MHC ligand generation
Proc.Natl.Acad.Sci.Usa, 103, 2006
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6ZP8
 | | Yeast 20S proteasome in complex with glidobactin-like natural product HB335 | | Descriptor: | (2~{S},3~{R})-~{N}-[(5~{S},8~{S},10~{S})-5-methyl-10-oxidanyl-2,7-bis(oxidanylidene)-1,6-diazacyclododec-8-yl]-3-oxidanyl-2-(3-phenylpropanoylamino)butanamide, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Zhao, L, Le Chapelain, C, Brachmann, A.O, Kaiser, M, Groll, M, Bode, H.B. | | Deposit date: | 2020-07-08 | | Release date: | 2021-05-19 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Activation, Structure, Biosynthesis and Bioactivity of Glidobactin-like Proteasome Inhibitors from Photorhabdus laumondii.
Chembiochem, 22, 2021
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4FZG
 | | 20S yeast proteasome in complex with glidobactin | | Descriptor: | Glidobactin, Proteasome component C1, Proteasome component C11, ... | | Authors: | Stein, M, Beck, P, Kaiser, M, Dudler, R, Becker, C.F.W, Groll, M. | | Deposit date: | 2012-07-06 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | One-shot NMR analysis of microbial secretions identifies highly potent proteasome inhibitor.
Proc.Natl.Acad.Sci.USA, 109, 2012
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4QBY
 | | yCP in complex with BOC-ALA-ALA-ALA-CHO | | Descriptor: | BOC-ALA-ALA-ALA-CHO, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | Authors: | Arciniega, M, Beck, P, Lange, O, Groll, M, Huber, R. | | Deposit date: | 2014-05-09 | | Release date: | 2014-06-18 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Differential global structural changes in the core particle of yeast and mouse proteasome induced by ligand binding.
Proc.Natl.Acad.Sci.USA, 111, 2014
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6REY
 | | Human 20S-PA200 Proteasome Complex | | Descriptor: | INOSITOL HEXAKISPHOSPHATE, Proteasome activator complex subunit 4, Proteasome subunit alpha type-1, ... | | Authors: | Toste Rego, A, da Fonseca, P.C.A. | | Deposit date: | 2019-04-12 | | Release date: | 2019-09-04 | | Last modified: | 2024-05-22 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Characterization of Fully Recombinant Human 20S and 20S-PA200 Proteasome Complexes.
Mol.Cell, 76, 2019
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4QZ4
 | | yCP beta5-A49S mutant in complex with the epoxyketone inhibitor ONX 0914 | | 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: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-27 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QV3
 | | yCP beta5-M45V mutant | | Descriptor: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | Authors: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-14 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QW5
 | | yCP beta5-M45A mutant in complex with carfilzomib | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-16 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QZ0
 | | yCP beta5-M45V mutant in complex with the epoxyketone inhibitor ONX 0914 | | 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: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-27 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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1JD2
 | | Crystal Structure of the yeast 20S Proteasome:TMC-95A complex: A non-covalent Proteasome Inhibitor | | Descriptor: | MAGNESIUM ION, PROTEASOME COMPONENT C1, PROTEASOME COMPONENT C11, ... | | Authors: | Groll, M, Koguchi, Y, Huber, R, Kohno, J. | | Deposit date: | 2001-06-12 | | Release date: | 2002-02-13 | | Last modified: | 2017-10-04 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Crystal structure of the 20 S proteasome:TMC-95A complex: a non-covalent proteasome inhibitor.
J.Mol.Biol., 311, 2001
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4QUX
 | | yCP beta5-A49T-mutant | | Descriptor: | MAGNESIUM ION, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | | Authors: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-14 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QVW
 | | yCP beta5-A49S-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: | 2014-07-16 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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8CVT
 | | Human 19S-20S proteasome, state SD2 | | Descriptor: | 26S protease regulatory subunit 10B, 26S protease regulatory subunit 8, 26S proteasome complex subunit SEM1, ... | | Authors: | Zhao, J. | | Deposit date: | 2022-05-18 | | Release date: | 2022-11-02 | | Method: | ELECTRON MICROSCOPY (3 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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4QZ1
 | | yCP beta5-M45T mutant in complex with the epoxyketone inhibitor ONX 0914 | | 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: | Huber, E.M, Heinemeyer, W, Groll, M. | | Deposit date: | 2014-07-27 | | Release date: | 2015-02-04 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4Z1L
 | | Yeast 20S proteasome in complex with belactosin C derivative 3 | | Descriptor: | (2S,3S)-2-{(1R)-2-[(3,5-dimethoxybenzyl)amino]-1-hydroxy-2-oxoethyl}-3-methylpentanoic acid, CHLORIDE ION, MAGNESIUM ION, ... | | Authors: | Huber, E.M, Groll, M. | | Deposit date: | 2015-03-27 | | Release date: | 2015-05-27 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | A Minimal beta-Lactone Fragment for Selective beta 5c or beta 5i Proteasome Inhibitors.
Angew.Chem.Int.Ed.Engl., 54, 2015
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