3SHJ
 
 | | Proteasome in complex with hydroxyurea derivative HU10 | | Descriptor: | 1-hydroxy-1-[(2R)-4-{3-[(3S,5S,7S)-tricyclo[3.3.1.1~3,7~]dec-1-yloxy]phenyl}but-3-yn-2-yl]urea, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Proteasome component C1, ... | | Authors: | Gallastegui, N, Beck, P, Arciniega, M, Hillebrand, S, Huber, R, Groll, M. | | Deposit date: | 2011-06-16 | | Release date: | 2011-12-07 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Hydroxyureas as noncovalent proteasome inhibitors.
Angew.Chem.Int.Ed.Engl., 51, 2012
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4LQI
 | | Yeast 20S Proteasome in complex with Vibralactone | | Descriptor: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | Authors: | List, A, Zeiler, E, Gallastegui, N, Rusch, M, Hedberg, C, Sieber, S.A, Groll, M. | | Deposit date: | 2013-07-18 | | Release date: | 2013-12-25 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Omuralide and Vibralactone: Differences in the Proteasome-beta-Lactone-gamma-Lactam Binding Scaffold Alter Target Preferences.
Angew.Chem.Int.Ed.Engl., 53, 2014
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3NZW
 | | Crystal structure of the yeast 20S proteasome in complex with 2b | | 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: | 2010-07-17 | | Release date: | 2011-02-16 | | Last modified: | 2023-12-06 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | 20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A.
Chemmedchem, 5, 2010
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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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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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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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4JSQ
 | | Yeast 20S proteasome in complex with the dimerized linear mimetic of TMC-95A - yCP:4e | | 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 (2.8 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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4JT0
 | | Yeast 20S proteasome in complex with the dimerized linear mimetic of TMC-95A - yCP:4a | | 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 (3.1 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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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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4INT
 | | Yeast 20S proteasome in complex with the vinyl sulfone LU122 | | Descriptor: | HMB-Val-Ser-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 (2.9 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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4INU
 | | Yeast 20S proteasome in complex with the vinyl sulfone LU112 | | Descriptor: | N3Phe-Phe(4-NH2CH2)-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 (3.1 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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