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5JJM
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CRYSTAL STRUCTURE OF HOMODIMERIC ANDROGEN RECEPTOR LIGAND-BINDING DOMAIN BOUND TO DHT AND LXXLL PEPTIDE
Descriptor:Androgen receptor, Unknown peptide, uba3-derived peptide, ...
Authors:Estebanez-Perpina, E., Fuentes-Prior, P.
Deposit date:2016-04-24
Release date:2017-03-15
Method:X-RAY DIFFRACTION (2.15 Å)
Cite:Structure of the homodimeric androgen receptor ligand-binding domain.
Nat Commun, 8, 2017
4LQI
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YEAST 20S PROTEASOME IN COMPLEX WITH VIBRALACTONE
Descriptor:Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, Proteasome subunit alpha type-4, ...
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:2014-01-22
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
4JT0
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YEAST 20S PROTEASOME IN COMPLEX WITH THE DIMERIZED LINEAR MIMETIC OF TMC-95A - YCP:4A
Descriptor:Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, Proteasome subunit alpha type-4, ...
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:2013-06-05
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., 2013
4JSU
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YEAST 20S PROTEASOME IN COMPLEX WITH THE DIMERIZED LINEAR MIMETIC OF TMC-95A - YCP:3A
Descriptor:Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, Proteasome subunit alpha type-4, ...
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:2014-04-23
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
4JSQ
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YEAST 20S PROTEASOME IN COMPLEX WITH THE DIMERIZED LINEAR MIMETIC OF TMC-95A - YCP:4E
Descriptor:Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, Proteasome subunit alpha type-4, ...
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:2014-04-23
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
4INU
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YEAST 20S PROTEASOME IN COMPLEX WITH THE VINYL SULFONE LU112
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2013-02-27
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
4INT
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YEAST 20S PROTEASOME IN COMPLEX WITH THE VINYL SULFONE LU122
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2013-02-27
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
4INR
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YEAST 20S PROTEASOME IN COMPLEX WITH THE VINYL SULFONE LU102
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2013-02-27
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
3SHJ
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PROTEASOME IN COMPLEX WITH HYDROXYUREA DERIVATIVE HU10
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2012-01-18
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Hydroxyureas as noncovalent proteasome inhibitors.
Angew.Chem.Int.Ed.Engl., 51, 2012
3OKJ
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ALPHA-KETO-ALDEHYDE BINDING MECHANISM REVEALS A NOVEL LEAD STRUCTURE MOTIF FOR PROTEASOME INHIBITION
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
Authors:Groll, M., Poynor, M., Gallastegui, P., Stein, M., Schmidt, B., Kloetzel, P.M., Huber, R.
Deposit date:2010-08-25
Release date:2011-06-08
Last modified:2018-01-24
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Elucidation of the alpha-keto-aldehyde binding mechanism: a lead structure motif for proteasome inhibition
Angew.Chem.Int.Ed.Engl., 50, 2011
3NZX
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CRYSTAL STRUCTURE OF THE YEAST 20S PROTEASOME IN COMPLEX WITH LIGAND 2C
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2012-12-12
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
3NZW
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CRYSTAL STRUCTURE OF THE YEAST 20S PROTEASOME IN COMPLEX WITH 2B
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2012-12-12
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
3NZJ
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CRYSTAL STRUCTURE OF YEAST 20S PROTEASOME IN COMPLEX WITH LIGAND 2A
Descriptor:Proteasome component Y7, Proteasome component Y13, Proteasome component PRE6, ...
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:2012-12-12
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