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3V49
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STRUCTURE OF AR LBD WITH ACTIVATOR PEPTIDE AND SARM INHIBITOR 1
Descriptor:Androgen receptor, activator peptide, 4-[(4R)-4-(4-hydroxyphenyl)-3,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile, ...
Authors:Nique, F., Hebbe, S., Peixoto, C., Annoot, D., Lefrancois, J.-M., Duval, E., Michoux, L., Triballeau, N., Lemoullec, J.-M., Mollat, P., Thauvin, M., Prange, T., Minet, D., Clement-Lacroix, P., Robin-Jagerschmidt, C., Fleury, D., Guedin, D., Deprez, P.
Deposit date:2011-12-14
Release date:2012-09-05
Last modified:2018-01-24
Method:X-RAY DIFFRACTION (1.7 Å)
Cite:Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
3V4A
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STRUCTURE OF AR LBD WITH ACTIVATOR PEPTIDE AND SARM INHIBITOR 2
Descriptor:Androgen receptor, (5R)-3-(3,4-dichlorophenyl)-5-(4-hydroxyphenyl)-1,5-dimethyl-2-thioxoimidazolidin-4-one, SULFATE ION
Authors:Nique, F., Hebbe, S., Peixoto, C., Annoot, D., Lefrancois, J.-M., Duval, E., Michoux, L., Triballeau, N., Lemoullec, J.M., Mollat, P., Thauvin, M., Prange, T., Minet, D., Clement-Lacroix, P., Robin-Jagerschmidt, C., Fleury, D., Guedin, D., Deprez, P.
Deposit date:2011-12-14
Release date:2012-09-05
Last modified:2018-01-24
Method:X-RAY DIFFRACTION (1.95 Å)
Cite:Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
1E3G
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HUMAN ANDROGEN RECEPTOR LIGAND BINDING IN COMPLEX WITH THE LIGAND METRIBOLONE (R1881)
Descriptor:ANDROGEN RECEPTOR, (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE
Authors:Matias, P.M., Donner, P., Coelho, R., Thomaz, M., Peixoto, C., Macedo, S., Otto, N., Joschko, S., Scholz, P., Wegg, A., Basler, S., Schafer, M., Ruff, M., Egner, U., Carrondo, M.A.
Deposit date:2000-06-14
Release date:2001-06-14
Last modified:2018-02-28
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.
J. Biol. Chem., 275, 2000
1E3K
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HUMAN PROGESTERON RECEPTOR LIGAND BINDING DOMAIN IN COMPLEX WITH THE LIGAND METRIBOLONE (R1881)
Descriptor:PROGESTERONE RECEPTOR, (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE
Authors:Matias, P.M., Donner, P., Coelho, R., Thomaz, M., Peixoto, C., Macedo, S., Otto, N., Joschko, S., Scholz, P., Wegg, A., Basler, S., Schafer, M., Egner, U., Carrondo, M.A.
Deposit date:2000-06-19
Release date:2001-06-14
Last modified:2018-02-28
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.
J. Biol. Chem., 275, 2000
2J5W
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CERULOPLASMIN REVISITED: STRUCTURAL AND FUNCTIONAL ROLES OF VARIOUS METAL CATION BINDING SITES
Descriptor:CERULOPLASMIN, CALCIUM ION, SODIUM ION, ...
Authors:Bento, I., Peixoto, C., Zaitsev, V.N., Lindley, P.F.
Deposit date:2006-09-19
Release date:2007-02-06
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Ceruloplasmin Revisited: Structural and Functional Roles of Various Metal Cation-Binding Sites.
Acta Crystallogr.,Sect.D, 63, 2007
5M7M
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NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES WITH POTENT AUTOTAXIN/ENPP2 INHIBITOR ACTIVITY
Descriptor:Ectonucleotide pyrophosphatase/phosphodiesterase family member 2, N-ACETYL-D-GLUCOSAMINE, BETA-D-MANNOSE, ...
Authors:Wolhkoning, A., Fleury, D., Leonard, P., Triballeau, N., Mollat, P., Vercheval, L.
Deposit date:2016-10-28
Release date:2017-08-30
Last modified:2018-01-31
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
J. Med. Chem., 60, 2017
5MHP
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NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES WITH POTENT AUTOTAXIN/ENPP2 INHIBITOR ACTIVITY
Descriptor:Ectonucleotide pyrophosphatase/phosphodiesterase family member 2, N-ACETYL-D-GLUCOSAMINE, BETA-D-MANNOSE, ...
Authors:Fleury, D., Mueller, I., Lamers, M., Triballeau, N., Mollat, P., Vercheval, L.
Deposit date:2016-11-25
Release date:2017-08-30
Last modified:2018-01-24
Method:X-RAY DIFFRACTION (2.43 Å)
Cite:Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis.
J. Med. Chem., 60, 2017