5T1Z
 
 | | 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
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5W9C
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4XI3
 | | 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
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5WGD
 | | 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: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | A "cross-stitched" peptide with improved helicity and proteolytic stability.
Org. Biomol. Chem., 16, 2018
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5WGQ
 | | 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: | 2024-10-30 | | 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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7JHD
 | | 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
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6PIT
 | | 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
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6CBZ
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6PSJ
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5HYR
 | | 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
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7KBS
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6CZN
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Z2OHTPE and a glucocorticoid receptor-interacting protein 1 NR box II peptide | | Descriptor: | 4,4'-[(1R,2R)-1-phenylbutane-1,2-diyl]diphenol, Estrogen receptor, GRIP Peptide | | Authors: | Fanning, S.W, Han, R, Maximov, P, Jordan, V.C, Greene, G.L. | | Deposit date: | 2018-04-09 | | Release date: | 2019-03-20 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Z2OHTPE and a glucocorticoid receptor-interacting protein 1 NR box II peptide
To Be Published
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6D0F
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with 3OHTPE and GRIP Peptide | | Descriptor: | 4,4',4''-[(2R)-butane-1,1,2-triyl]triphenol, Estrogen receptor, GRIP Peptide | | Authors: | Fanning, S.W, Han, R, Maximov, P, Jordan, V.C, Greene, G.L. | | Deposit date: | 2018-04-10 | | Release date: | 2019-04-17 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with 3OHTPE and GRIP Peptide
To Be Published
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6C42
 | | 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
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5W9D
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5UFX
 | | 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
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5UFW
 | | 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
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5DXB
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Stapled Peptide SRC2-P1 and Estradiol | | Descriptor: | CHLORIDE ION, ESTRADIOL, Estrogen receptor, ... | | Authors: | Fanning, S.W, Speltz, T.E, Mayne, C.G, Tajkhorshid, E, Greene, G.L, Moore, T.W. | | Deposit date: | 2015-09-23 | | Release date: | 2016-07-27 | | Last modified: | 2020-02-19 | | Method: | X-RAY DIFFRACTION (2.08 Å) | | Cite: | Stapled Peptides with gamma-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction.
Angew. Chem. Int. Ed. Engl., 55, 2016
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5DXG
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Stapled Peptide SRC2-P5 | | 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: | 2015-09-23 | | Release date: | 2016-07-27 | | Last modified: | 2020-02-19 | | Method: | X-RAY DIFFRACTION (1.86 Å) | | Cite: | Stapled Peptides with gamma-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction.
Angew. Chem. Int. Ed. Engl., 55, 2016
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5DXE
 | | Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with Stapled Peptide SRC2-P4 and Estradiol | | Descriptor: | ESTRADIOL, Estrogen receptor, Nuclear receptor coactivator 2 | | Authors: | Fanning, S.W, Speltz, T.E, Mayne, C.G, Tajkhorshid, E, Greene, G.L, Moore, T.W. | | Deposit date: | 2015-09-23 | | Release date: | 2016-08-03 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Stapled Peptides with gamma-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction.
Angew.Chem.Int.Ed.Engl., 55, 2016
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6V8T
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6VGH
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6V87
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6VPF
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6VJD
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