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1R5K
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HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH GW5638
Descriptor:Estrogen receptor, (2E)-3-{4-[(1E)-1,2-DIPHENYLBUT-1-ENYL]PHENYL}ACRYLIC ACID
Authors:Wu, Y.-L., Yang, X., Ren, Z., McDonnell, D.P., Norris, J.D., Willson, T.M., Greene, G.L.
Deposit date:2003-10-10
Release date:2004-11-23
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Structural basis for an unexpected mode of SERM-mediated ER antagonism.
Mol.Cell, 18, 2005
1YUC
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HUMAN NUCLEAR RECEPTOR LIVER RECEPTOR HOMOLOGUE-1, LRH-1, BOUND TO PHOSPHOLIPID AND A FRAGMENT OF HUMAN SHP
Descriptor:Orphan nuclear receptor NR5A2, Nuclear receptor 0B2, L-ALPHA-PHOSPHATIDYL-BETA-OLEOYL-GAMMA-PALMITOYL-PHOSPHATIDYLETHANOLAMINE, ...
Authors:Ortlund, E.A., Yoonkwang, L., Solomon, I.H., Hager, J.M., Safi, R., Choi, Y., Guan, Z., Tripathy, A., Raetz, C.R.H., McDonnell, D.P., Moore, D.D., Redinbo, M.R.
Deposit date:2005-02-13
Release date:2005-03-01
Last modified:2018-01-31
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Modulation of human nuclear receptor LRH-1 activity by phospholipids and SHP
Nat.Struct.Mol.Biol., 12, 2005
2A66
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HUMAN LIVER RECEPTOR HOMOLOGUE DNA-BINDING DOMAIN (HLRH-1 DBD) IN COMPLEX WITH DSDNA FROM THE HCYP7A1 PROMOTER
Descriptor:5'-D(*GP*TP*TP*CP*AP*AP*GP*GP*CP*CP*AP*G)-3', 5'-D(*CP*TP*GP*GP*CP*CP*TP*TP*GP*AP*AP*C)-3', Orphan nuclear receptor NR5A2, ...
Authors:Solomon, I.H., Hager, J.M., Safi, R., McDonnell, D.P., Redinbo, M.R., Ortlund, E.A.
Deposit date:2005-07-01
Release date:2005-12-06
Last modified:2017-10-11
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Crystal Structure of the Human LRH-1 DBD-DNA Complex Reveals Ftz-F1 Domain Positioning is Required for Receptor Activity.
J.Mol.Biol., 354, 2005
2EWP
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CRYSTAL STRUCTURE OF ESTROGEN RELATED RECEPTOR-3 (ERR-GAMMA) LIGAND BINDING DOMAIND WITH TAMOXIFEN ANALOG GSK5182
Descriptor:Estrogen-related receptor gamma, (Z)-4-(1-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-HYDROXY-2-PHENYLPENT-1-ENYL)PHENOL
Authors:Nolte, R.T.
Deposit date:2005-11-04
Release date:2006-05-09
Last modified:2017-10-18
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Bioorg.Med.Chem.Lett., 16, 2006
5T92
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ESTROGEN RECEPTOR ALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH (2E)-3-{4-[(1R)-2-(4-FLUOROPHENYL)-6-HYDROXY-1-METHY L-1,2,3,4- TETRAHYDROISOQUINOLIN-1-YL]PHENYL}PROP-2-ENOIC ACID
Descriptor:Estrogen receptor, (2E)-3-{4-[(1R)-2-(4-fluorophenyl)-6-hydroxy-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl]phenyl}prop-2-enoic acid
Authors:Kirby, C., Baird, J.
Deposit date:2016-09-09
Release date:2017-03-29
Last modified:2017-04-26
Method:X-RAY DIFFRACTION (2.22 Å)
Cite:Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ER alpha + Breast Cancer.
J. Med. Chem., 60, 2017
5T97
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ESTROGEN RECEPTOR ALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH (2E)-3-(4-{(1R)-6-HYDROXY-1-METHYL-2-[4-(PROPAN-2 -YL)PHENYL]-1,2,3,4- TETRAHYDROISOQUINOLIN-1-YL}PHENYL)PROP-2-ENOIC ACID
Descriptor:Estrogen receptor, (2E)-3-(4-{(1R)-6-hydroxy-1-methyl-2-[4-(propan-2-yl)phenyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}phenyl)prop-2-enoic acid
Authors:Kirby, C.A., Baird, J.
Deposit date:2016-09-09
Release date:2017-03-29
Last modified:2017-04-26
Method:X-RAY DIFFRACTION (3 Å)
Cite:Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ER alpha + Breast Cancer.
J. Med. Chem., 60, 2017
6B0F
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ESTROGEN RECEPTOR ALPHA LIGAND BINDING DOMAIN IN COMPLEX WITH LSZ102
Descriptor:Estrogen receptor, (2E)-3-[4-({2-[2-(1,1-difluoroethyl)-4-fluorophenyl]-6-hydroxy-1-benzothiophen-3-yl}oxy)phenyl]prop-2-enoic acid, GLYCEROL
Authors:Kirby, C.A., Baird, J.
Deposit date:2017-09-14
Release date:2018-04-04
Last modified:2018-04-25
Method:X-RAY DIFFRACTION (2.86 Å)
Cite:Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
J. Med. Chem., 61, 2018