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5UFX
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BU of 5ufx by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with OP1074
Descriptor: (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-1-benzopyran-7-ol, Estrogen receptor
Authors:Fanning, S.W, Hodges-Gallagher, L, Myles, D.C, Sun, R, Fowler, C.E, Green, B.D, Harmon, C.L, Greene, G.L, Kushner, P.J.
Deposit date:2017-01-06
Release date:2018-01-10
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.5503 Å)
Cite:Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.
Nat Commun, 9, 2018
5UFW
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BU of 5ufw by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with OP1154
Descriptor: (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-1-benzopyran-7-ol, Estrogen receptor
Authors:Fanning, S.W, Hodges-Gallagher, L, Myles, D.C, Sun, R, Fowler, C.E, Green, B.D, Harmon, C.L, Greene, G.L, Kushner, P.J.
Deposit date:2017-01-06
Release date:2018-01-10
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.583 Å)
Cite:Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.
Nat Commun, 9, 2018
7JHD
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BU of 7jhd by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S in Complex with TTC-352 and GRIP Peptide
Descriptor: 3-(4-fluorophenyl)-2-(4-hydroxyphenoxy)-1-benzothiophene-6-ol, Estrogen receptor, Nuclear receptor coactivator 2
Authors:Fanning, S.W, Abderraman, B, Maximov, P.Y, Jordan, V.C, Greene, G.L.
Deposit date:2020-07-20
Release date:2020-11-25
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.402 Å)
Cite:Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer.
Mol.Cancer Ther., 20, 2021
6C42
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BU of 6c42 by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with OP1156
Descriptor: (2R,3S,4R)-3-(4-hydroxyphenyl)-4-methyl-2-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}-3,4-dihydro-2H-1-benzopyran-7-ol, Estrogen receptor
Authors:Fanning, S.W, Hodges-Gallager, L, Myles, D.C, Sun, R, Fowler, C.E, Green, B.D, Harmon, C.L, Greene, G.L, Kushner, P.J.
Deposit date:2018-01-11
Release date:2018-02-14
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.997 Å)
Cite:Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.
Nat Commun, 9, 2018
5T1Z
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BU of 5t1z by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Ethoxytriphenylethylene and GRIP Peptide
Descriptor: 4,4'-[(1Z)-1-(4-ethoxyphenyl)but-1-ene-1,2-diyl]diphenol, Estrogen receptor, Nuclear receptor coactivator 2
Authors:Fanning, S.W, Rajan, S.S, Maximov, P.Y, Abderrahman, B.H, Surojeet, S, Fernandes, D.J, Fan, P, Curpan, R.F, Greene, G.L, Jordan, V.C.
Deposit date:2016-08-22
Release date:2017-08-30
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (2.102 Å)
Cite:Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer.
Mol. Pharmacol., 94, 2018
5W9D
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BU of 5w9d by Molmil
Estrogen Receptor Alpha Ligand Binding Domain C381S, C417S, C530S Mutant in Complex with Endoxifen
Descriptor: Endoxifen, Estrogen receptor
Authors:Fanning, S.W, Greene, G.L.
Deposit date:2017-06-23
Release date:2017-10-11
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.6464 Å)
Cite:Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer.
Mol. Pharmacol., 94, 2018
6CBZ
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BU of 6cbz by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Estradiol and GRIP Peptide
Descriptor: ESTRADIOL, Estrogen receptor, GLYCEROL, ...
Authors:Fanning, S.W, Greene, G.L.
Deposit date:2018-02-05
Release date:2018-02-28
Last modified:2020-02-26
Method:X-RAY DIFFRACTION (1.65 Å)
Cite:Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer.
Mol. Pharmacol., 94, 2018
6PIT
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BU of 6pit by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with SRC2 Stapled Peptide 41A and Estradiol
Descriptor: ESTRADIOL, Estrogen receptor, Stapled Peptide 41A
Authors:Fanning, S.W, Montgomery, J.E, Greene, G.L, Moellering, R.E.
Deposit date:2019-06-27
Release date:2019-10-16
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.25 Å)
Cite:Versatile Peptide Macrocyclization with Diels-Alder Cycloadditions.
J.Am.Chem.Soc., 141, 2019
6PSJ
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BU of 6psj by Molmil
Bazedoxifene in Complex with Y537S Estrogen Receptor Alpha Ligand Binding Domain
Descriptor: Bazedoxifene, Estrogen receptor
Authors:Fanning, S.W, Greene, G.L.
Deposit date:2019-07-12
Release date:2019-11-20
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
4XI3
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BU of 4xi3 by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with Bazedoxifene
Descriptor: Bazedoxifene, Estrogen receptor
Authors:Fanning, S.W, Mayne, C.G, Toy, W, Carlson, K, Greene, B, Nowak, J, Walter, R, Panchamukhi, S, Tajhorshid, E, Nettles, K.W, Chandarlapaty, S, Katzenellenbogen, J, Greene, G.L.
Deposit date:2015-01-06
Release date:2016-01-13
Last modified:2024-03-06
Method:X-RAY DIFFRACTION (2.491 Å)
Cite:The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.
Elife, 7, 2018
5HYR
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BU of 5hyr by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Stapled Peptide SRC2-SP2 and Estradiol
Descriptor: ESTRADIOL, Estrogen receptor, GLYCEROL, ...
Authors:Fanning, S.W, Speltz, T.E, Mayne, C.G, Tajkhorshid, E, Greene, G.L, Moore, T.W.
Deposit date:2016-02-01
Release date:2016-05-25
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.271 Å)
Cite:Stapled Peptides with gamma-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction.
Angew.Chem.Int.Ed.Engl., 55, 2016
7TE7
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BU of 7te7 by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with RAD1901
Descriptor: (6R)-6-{2-[ethyl({4-[2-(ethylamino)ethyl]phenyl}methyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor
Authors:Joiner, C, Hancock, G, Young, K, Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-01-04
Release date:2022-01-19
Last modified:2023-10-25
Method:X-RAY DIFFRACTION (1.85 Å)
Cite:Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells.
NPJ Breast Cancer, 8, 2022
7UJ7
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BU of 7uj7 by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with RU39411
Descriptor: 11alpha-{4-[2-(dimethylamino)ethoxy]phenyl}estra-1(10),2,4-triene-3,17beta-diol, Estrogen receptor
Authors:Fanning, S.W, Greene, G.L.
Deposit date:2022-03-30
Release date:2022-05-04
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.68 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJO
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BU of 7ujo by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with RU39411
Descriptor: (9beta,11beta,17beta)-11-{4-[2-(dimethylamino)ethoxy]phenyl}estra-1,3,5(10)-triene-3,17-diol, Estrogen receptor, MAGNESIUM ION
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-31
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.449 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJW
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BU of 7ujw by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Possesses Selective Estrogen Receptor Degrader Activities
Descriptor: (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-31
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJ8
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BU of 7uj8 by Molmil
Estrogen Receptor Alpha Ligand Binding Domain Y537S in Complex with 4-Hydroxytamoxifen
Descriptor: 4-HYDROXYTAMOXIFEN, Estrogen receptor
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-30
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (2.385 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJF
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BU of 7ujf by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Methylated Lasofoxifene Derivative with Selective Estrogen Receptor Degrader Properties
Descriptor: (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-30
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.7 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJM
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BU of 7ujm by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Methylated Lasofoxifene Derivative That Increases Receptor Resonance Time in the Nucleus of Breast Cancer Cells
Descriptor: (5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-31
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJY
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BU of 7ujy by Molmil
Estrogen receptor alpha ligand binding domain Y537S mutant in complex with a methylated lasofoxifene derivative that enhances estrogen receptor alpha nuclear resonance time
Descriptor: (5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-31
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.7 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
7UJC
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BU of 7ujc by Molmil
Raloxifene in Complex with Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutation
Descriptor: Estrogen receptor, RALOXIFENE
Authors:Hosfield, D.J, Greene, G.L, Fanning, S.W.
Deposit date:2022-03-30
Release date:2022-06-15
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.78 Å)
Cite:Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Elife, 11, 2022
4Q13
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BU of 4q13 by Molmil
Apo Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant with a glucocorticoid receptor-interacting protein 1 NR box II peptide
Descriptor: Estrogen receptor, Glucocorticoid receptor-interacting protein 1 NR box II peptide
Authors:Fanning, S.W, Panchamukhi, S, Greene, G.L.
Deposit date:2014-04-02
Release date:2015-04-08
Last modified:2024-02-28
Method:X-RAY DIFFRACTION (2.24 Å)
Cite:Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.
Elife, 5, 2016
4PXM
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BU of 4pxm by Molmil
The Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant in Complex with Estradiol and a glucocorticoid receptor-interacting protein 1 NR box II peptide
Descriptor: ESTRADIOL, Estrogen receptor, Nuclear receptor coactivator 2
Authors:Fanning, S.W, Panchamukhi, S, Greene, G.L.
Deposit date:2014-03-24
Release date:2015-04-08
Last modified:2024-02-28
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.
Elife, 5, 2016
4Q50
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BU of 4q50 by Molmil
The Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant in Complex with 4-hydroxytamoxifen
Descriptor: 4-HYDROXYTAMOXIFEN, Estrogen receptor, SULFATE ION
Authors:Fanning, S.W, Greene, G.L.
Deposit date:2014-04-15
Release date:2015-04-15
Last modified:2024-02-28
Method:X-RAY DIFFRACTION (3.07 Å)
Cite:Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.
Elife, 5, 2016
5WGD
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BU of 5wgd by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with Estradiol and SRC2-LP1
Descriptor: (ACE)AILHKLLQDS(NH2), (ACE)HKILHKLLQDS(NH2), ESTRADIOL, ...
Authors:Fanning, S.W, Speltz, T.E, Mayne, C.G, Siddiqui, Z, Greene, G.L, Tajkhorshid, E, Moore, T.W.
Deposit date:2017-07-14
Release date:2018-06-13
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:A "cross-stitched" peptide with improved helicity and proteolytic stability.
Org. Biomol. Chem., 16, 2018
5WGQ
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BU of 5wgq by Molmil
Estrogen Receptor Alpha Ligand Binding Domain in Complex with Estradiol and SRC2-BCP1
Descriptor: ESTRADIOL, Estrogen receptor, SRC2-BCP1
Authors:Fanning, S.W, Speltz, T.E, Mayne, C.G, Siddiqui, Z, Greene, G.L, Tajkhorshid, E, Moore, T.W.
Deposit date:2017-07-14
Release date:2018-06-13
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:A "cross-stitched" peptide with improved helicity and proteolytic stability.
Org. Biomol. Chem., 16, 2018

 

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