PDBsum entry 3erd

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protein ligands metals Protein-protein interface(s) links
Nuclear receptor PDB id
Jmol PyMol
Protein chains
246 a.a. *
12 a.a. *
12 a.a. *
DES ×2
ACY ×2
Waters ×147
* Residue conservation analysis
PDB id:
Name: Nuclear receptor
Title: Human estrogen receptor alpha ligand-binding domain in complex with diethylstilbestrol and a glucocorticoid receptor interacting protein 1 nr box ii peptide
Structure: Protein (estrogen receptor alpha). Chain: a, b. Fragment: ligand-binding domain. Synonym: oestrogen receptor, er lbd. Engineered: yes. Protein (glucocorticoid receptor interacting protein 1). Chain: c, d. Fragment: nuclear receptor box ii.
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: estrogen receptor alpha. Expressed in: escherichia coli. Expression_system_taxid: 562.
Biol. unit: Homo-Dimer (from PDB file)
2.03Å     R-factor:   0.196     R-free:   0.248
Authors: A.K.Shiau,D.Barstad,P.M.Loria,L.Cheng,P.J.Kushner,D.A.Agard, G.L.Greene
Key ref:
A.K.Shiau et al. (1998). The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell, 95, 927-937. PubMed id: 9875847 DOI: 10.1016/S0092-8674(00)81717-1
31-Mar-99     Release date:   08-Apr-99    
Supersedes: 2erd
Go to PROCHECK summary

Protein chains
Pfam   ArchSchema ?
P03372  (ESR1_HUMAN) -  Estrogen receptor
595 a.a.
246 a.a.
Protein chain
Pfam   ArchSchema ?
Q15596  (NCOA2_HUMAN) -  Nuclear receptor coactivator 2
1464 a.a.
12 a.a.
Protein chain
Pfam   ArchSchema ?
Q15596  (NCOA2_HUMAN) -  Nuclear receptor coactivator 2
1464 a.a.
12 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Gene Ontology (GO) functional annotation 
  GO annot!
  Cellular component     nucleus   1 term 
  Biological process     steroid hormone mediated signaling pathway   2 terms 
  Biochemical function     DNA binding     2 terms  


DOI no: 10.1016/S0092-8674(00)81717-1 Cell 95:927-937 (1998)
PubMed id: 9875847  
The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen.
A.K.Shiau, D.Barstad, P.M.Loria, L.Cheng, P.J.Kushner, D.A.Agard, G.L.Greene.
Ligand-dependent activation of transcription by nuclear receptors (NRs) is mediated by interactions with coactivators. Receptor agonists promote coactivator binding, and antagonists block coactivator binding. Here we report the crystal structure of the human estrogen receptor alpha (hER alpha) ligand-binding domain (LBD) bound to both the agonist diethylstilbestrol (DES) and a peptide derived from the NR box II region of the coactivator GRIP1 and the crystal structure of the hER alpha LBD bound to the selective antagonist 4-hydroxytamoxifen (OHT). In the DES-LBD-peptide complex, the peptide binds as a short alpha helix to a hydrophobic groove on the surface of the LBD. In the OHT-LBD complex, helix 12 occludes the coactivator recognition groove by mimicking the interactions of the NR box peptide with the LBD. These structures reveal the two distinct mechanisms by which structural features of OHT promote this "autoinhibitory" helix 12 conformation.
  Selected figure(s)  
Figure 1.
Figure 1. Views of the Electron Density of the DES-ERα LBD-GRIP1 NR Box II Peptide Complex and of the OHT-ERα LBD Complex(A) A view of a 2F[o]−F[c] electron density map of the DES-LBD-peptide complex calculated at 2.03 Å resolution and contoured at 1.0 σ showing the GRIP1 NR box II interaction with the LBD. The peptide was omitted from the model prior to map calculation. Ile-689 from the peptide and two of the three receptor residues with which it interacts (Glu-542 and Leu-539) are labeled. Asp-538 has been omitted for clarity. The hydrogen bonds between the γ-carboxylate of Glu-542 and the amides of residues 689 and 690 of the peptide are depicted as dashed orange bonds.(B) A view of a 2F[o]−F[c] electron density map of the OHT-LBD complex calculated at 1.90 Å resolution and contoured at 1.0 σ showing the N-terminal region of helix 12. The dashed orange bonds depict the water-mediated hydrogen bond network between the imidazole ring of His-377, the γ-carboxylate of Glu-380, and the amide of Tyr-537. The three labeled residues (Glu-380, Leu-536, and Tyr-537) interact with each other through van der Waals contacts and/or hydrogen bonds.
Figure 4.
Figure 4. DES Interactions with the LBD (A) and OHT Interactions with the LBD (B)Residues that interact with the ligands are drawn at approximately their true positions. The residues that form van der Waals contacts with ligand are depicted as labeled arcs with radial spokes that point towards the ligand atoms with which they interact. The residues that hydrogen bond to ligand are shown in ball-and-stick representation. Hydrogen bonds are represented as dashed cyan lines; the distance of each bond is given. The ligand rings and the individual ligand atoms are labeled.
  The above figures are reprinted by permission from Cell Press: Cell (1998, 95, 927-937) copyright 1998.  
  Figures were selected by an automated process.  

Literature references that cite this PDB file's key reference

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PDB code: 3kwy
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PDB codes: 2qxs 2qzo 3os8 3os9 3osa
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PDB codes: 3a2h 3a2i 3a2j
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PDB codes: 3oll 3ols
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Quantification of the vitamin D receptor-coregulator interaction.
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Probing the flexibility of large conformational changes in protein structures through local perturbations.
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New selective estrogen and androgen receptor modulators.
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Estrogen Regulation of MicroRNA Expression.
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Development of a second-generation antiandrogen for treatment of advanced prostate cancer.
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Multiple binding modes between HNF4alpha and the LXXLL motifs of PGC-1alpha lead to full activation.
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PDB code: 3fs1
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An effective docking strategy for virtual screening based on multi-objective optimization algorithm.
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KLF4 suppresses estrogen-dependent breast cancer growth by inhibiting the transcriptional activity of ERalpha.
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A progesterone receptor co-activator (JDP2) mediates activity through interaction with residues in the carboxyl-terminal extension of the DNA binding domain.
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Structure of the AML1-ETO eTAFH domain-HEB peptide complex and its contribution to AML1-ETO activity.
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PDB code: 2knh
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Estrogen directly activates AID transcription and function.
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Anti-androgens and androgen-depleting therapies in prostate cancer: new agents for an established target.
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Breast cancer, estrogen receptor and ligands.
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Human prolactin gene promoter regulation by estrogen: convergence with tumor necrosis factor-alpha signaling.
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Biological functions and clinical implications of oestrogen receptors alfa and beta in epithelial tissues.
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The HER4/4ICD estrogen receptor coactivator and BH3-only protein is an effector of tamoxifen-induced apoptosis.
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18363513 C.Möller, J.Hoffmann, T.A.Kirkland, and W.Schwede (2008).
Investigational developments for the treatment of progesterone-dependent diseases.
  Expert Opin Investig Drugs, 17, 469-479.  
18175308 C.Schalon, J.S.Surgand, E.Kellenberger, and D.Rognan (2008).
A simple and fuzzy method to align and compare druggable ligand-binding sites.
  Proteins, 71, 1755-1778.  
18794234 D.Di Lorenzo, G.Rando, P.Ciana, and A.Maggi (2008).
Molecular imaging, an innovative methodology for whole-body profiling of endocrine disrupter action.
  Toxicol Sci, 106, 304-311.  
18363044 D.F.Skafar, and C.Zhao (2008).
The multifunctional estrogen receptor-alpha F domain.
  Endocrine, 33, 1-8.  
18367407 D.J.Britton, G.K.Scott, B.Schilling, C.Atsriku, J.M.Held, B.W.Gibson, C.C.Benz, and M.A.Baldwin (2008).
A novel serine phosphorylation site detected in the N-terminal domain of estrogen receptor isolated from human breast cancer cells.
  J Am Soc Mass Spectrom, 19, 729-740.  
19015525 E.P.Sablin, A.Woods, I.N.Krylova, P.Hwang, H.A.Ingraham, and R.J.Fletterick (2008).
The structure of corepressor Dax-1 bound to its target nuclear receptor LRH-1.
  Proc Natl Acad Sci U S A, 105, 18390-18395.
PDB code: 3f5c
19022902 E.Powell, and W.Xu (2008).
Intermolecular interactions identify ligand-selective activity of estrogen receptor alpha/beta dimers.
  Proc Natl Acad Sci U S A, 105, 19012-19017.  
18462183 F.Journé, J.J.Body, G.Leclercq, and G.Laurent (2008).
Hormone therapy for breast cancer, with an emphasis on the pure antiestrogen fulvestrant: mode of action, antitumor efficacy and effects on bone health.
  Expert Opin Drug Saf, 7, 241-258.  
19119325 J.Nilmeier, and M.Jacobson (2008).
Multiscale Monte Carlo Sampling of Protein Sidechains: Application to Binding Pocket Flexibility.
  J Chem Theory Comput, 4, 835-846.  
  18484708 J.R.Gunther, T.W.Moore, M.L.Collins, and J.A.Katzenellenbogen (2008).
Amphipathic benzenes are designed inhibitors of the estrogen receptor alpha/steroid receptor coactivator interaction.
  ACS Chem Biol, 3, 282-286.  
  18839960 J.Singh, M.Salcius, S.W.Liu, B.L.Staker, R.Mishra, J.Thurmond, G.Michaud, D.R.Mattoon, J.Printen, J.Christensen, J.M.Bjornsson, B.A.Pollok, M.Kiledjian, L.Stewart, J.Jarecki, and M.E.Gurney (2008).
DcpS as a therapeutic target for spinal muscular atrophy.
  ACS Chem Biol, 3, 711-722.
PDB codes: 3bl7 3bl9 3bla
18710950 K.R.Badri, Y.Zhou, U.Dhru, S.Aramgam, and L.Schuger (2008).
Effects of the SANT domain of tension-induced/inhibited proteins (TIPs), novel partners of the histone acetyltransferase p300, on p300 activity and TIP-6-induced adipogenesis.
  Mol Cell Biol, 28, 6358-6372.  
18769464 K.W.Nettles (2008).
Insights into PPARgamma from structures with endogenous and covalently bound ligands.
  Nat Struct Mol Biol, 15, 893-895.  
18344977 K.W.Nettles, J.B.Bruning, G.Gil, J.Nowak, S.K.Sharma, J.B.Hahm, K.Kulp, R.B.Hochberg, H.Zhou, J.A.Katzenellenbogen, B.S.Katzenellenbogen, Y.Kim, A.Joachmiak, and G.L.Greene (2008).
NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.
  Nat Chem Biol, 4, 241-247.
PDB codes: 2b23 2qa6 2qa8 2qab 2qgt 2qgw 2qh6 2qr9 2qse 2qxm
18462184 L.Gennari, D.Merlotti, V.D.Paola, and R.Nuti (2008).
Raloxifene in breast cancer prevention.
  Expert Opin Drug Saf, 7, 259-270.  
19102007 M.A.Thorat, D.Turbin, A.Morimiya, S.Leung, Q.Zhang, M.H.Jeng, D.G.Huntsman, H.Nakshatri, and S.Badve (2008).
Amplified in breast cancer 1 expression in breast cancer.
  Histopathology, 53, 634-641.  
18852122 M.C.Hodgson, H.C.Shen, A.N.Hollenberg, and S.P.Balk (2008).
Structural basis for nuclear receptor corepressor recruitment by antagonist-liganded androgen receptor.
  Mol Cancer Ther, 7, 3187-3194.  
18655705 M.Paris, K.Pettersson, M.Schubert, S.Bertrand, I.Pongratz, H.Escriva, and V.Laudet (2008).
An amphioxus orthologue of the estrogen receptor that does not bind estradiol: insights into estrogen receptor evolution.
  BMC Evol Biol, 8, 219.  
17904370 N.Yoshimoto, Y.Inaba, S.Yamada, M.Makishima, M.Shimizu, and K.Yamamoto (2008).
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
  Bioorg Med Chem, 16, 457-473.  
19079612 R.Narayanan, M.L.Mohler, C.E.Bohl, D.D.Miller, and J.T.Dalton (2008).
Selective androgen receptor modulators in preclinical and clinical development.
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18372406 R.S.Thomas, N.Sarwar, F.Phoenix, R.C.Coombes, and S.Ali (2008).
Phosphorylation at serines 104 and 106 by Erk1/2 MAPK is important for estrogen receptor-alpha activity.
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18179891 R.W.Collin, E.Kalay, M.Tariq, T.Peters, B.van der Zwaag, H.Venselaar, J.Oostrik, K.Lee, Z.M.Ahmed, R.Caylan, Y.Li, H.A.Spierenburg, E.Eyupoglu, A.Heister, S.Riazuddin, E.Bahat, M.Ansar, S.Arslan, B.Wollnik, H.G.Brunner, C.W.Cremers, A.Karaguzel, W.Ahmad, F.P.Cremers, G.Vriend, T.B.Friedman, S.Riazuddin, S.M.Leal, and H.Kremer (2008).
Mutations of ESRRB encoding estrogen-related receptor beta cause autosomal-recessive nonsyndromic hearing impairment DFNB35.
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17949766 R.W.Hsieh, S.S.Rajan, S.K.Sharma, and G.L.Greene (2008).
Molecular characterization of a B-ring unsaturated estrogen: implications for conjugated equine estrogen components of premarin.
  Steroids, 73, 59-68.
PDB code: 2b1z
18391212 S.M.Soisson, G.Parthasarathy, A.D.Adams, S.Sahoo, A.Sitlani, C.Sparrow, J.Cui, and J.W.Becker (2008).
Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation.
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PDB code: 3bej
18347588 S.Mader (2008).
Fast-tracking steroid receptor crystallization.
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18951949 S.Sheng, D.H.Barnett, and B.S.Katzenellenbogen (2008).
Differential estradiol and selective estrogen receptor modulator (SERM) regulation of Keratin 13 gene expression and its underlying mechanism in breast cancer cells.
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18798693 S.W.Kruse, K.Suino-Powell, X.E.Zhou, J.E.Kretschman, R.Reynolds, C.Vonrhein, Y.Xu, L.Wang, S.Y.Tsai, M.J.Tsai, and H.E.Xu (2008).
Identification of COUP-TFII orphan nuclear receptor as a retinoic acid-activated receptor.
  PLoS Biol, 6, e227.
PDB code: 3cjw
18474858 S.Y.Dai, M.J.Chalmers, J.Bruning, K.S.Bramlett, H.E.Osborne, C.Montrose-Rafizadeh, R.J.Barr, Y.Wang, M.Wang, T.P.Burris, J.A.Dodge, and P.R.Griffin (2008).
Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method.
  Proc Natl Acad Sci U S A, 105, 7171-7176.
PDB codes: 2r6w 2r6y
18330543 T.Harada, K.Yamagishi, T.Nakano, K.Kitaura, and H.Tokiwa (2008).
Ab initio fragment molecular orbital study of ligand binding to human progesterone receptor ligand-binding domain.
  Naunyn Schmiedebergs Arch Pharmacol, 377, 607-615.  
18068350 V.C.Jordan (2008).
Tamoxifen: catalyst for the change to targeted therapy.
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  18097104 V.Cura, M.Gangloff, S.Eiler, D.Moras, and M.Ruff (2008).
Cleaved thioredoxin fusion protein enables the crystallization of poorly soluble ERalpha in complex with synthetic ligands.
  Acta Crystallogr Sect F Struct Biol Cryst Commun, 64, 54-57.  
18578507 Y.G.Tao, Y.Xu, H.E.Xu, and S.S.Simons (2008).
Mutations of glucocorticoid receptor differentially affect AF2 domain activity in a steroid-selective manner to alter the potency and efficacy of gene induction and repression.
  Biochemistry, 47, 7648-7662.  
18167132 Y.Nagahara, I.Shiina, K.Nakata, A.Sasaki, T.Miyamoto, and M.Ikekita (2008).
Induction of mitochondria-involved apoptosis in estrogen receptor-negative cells by a novel tamoxifen derivative, ridaifen-B.
  Cancer Sci, 99, 608-614.  
18350282 Y.Umezawa (2008).
Detecting mitochondrial RNA and other cellular events in living cells.
  Anal Bioanal Chem, 391, 1591-1598.  
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Can a single model explain both breast cancer and prostate cancer?
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17521611 A.Zhang, C.W.Li, and J.D.Chen (2007).
Characterization of transcriptional regulatory domains of ankyrin repeat cofactor-1.
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17286281 A.Zhang, C.W.Li, S.C.Tsai, and J.D.Chen (2007).
Subcellular localization of ankyrin repeats cofactor-1 regulates its corepressor activity.
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17886255 B.J.Cheskis, J.G.Greger, S.Nagpal, and L.P.Freedman (2007).
Signaling by estrogens.
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17400923 C.Bovet, A.Wortmann, S.Eiler, F.Granger, M.Ruff, B.Gerrits, D.Moras, and R.Zenobi (2007).
Estrogen receptor-ligand complexes measured by chip-based nanoelectrospray mass spectrometry: an approach for the screening of endocrine disruptors.
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17555576 C.J.Fong, L.D.Burgoon, K.J.Williams, A.L.Forgacs, and T.R.Zacharewski (2007).
Comparative temporal and dose-dependent morphological and transcriptional uterine effects elicited by tamoxifen and ethynylestradiol in immature, ovariectomized mice.
  BMC Genomics, 8, 151.  
17983255 C.K.Baumann, and M.Castiglione-Gertsch (2007).
Estrogen receptor modulators and down regulators: optimal use in postmenopausal women with breast cancer.
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17933688 C.Kremoser, M.Albers, T.P.Burris, U.Deuschle, and M.Koegl (2007).
Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators.
  Drug Discov Today, 12, 860-869.  
17368178 C.M.Bula, J.E.Bishop, and A.W.Norman (2007).
Conservative mutageneic perturbations of amino acids connecting helix 12 in the 1alpha,25(OH)2-D3 receptor (VDR) to the ligand cause significant transactivational effects.
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17392432 C.M.Eakin, M.J.Maccoss, G.L.Finney, and R.E.Klevit (2007).
Estrogen receptor alpha is a putative substrate for the BRCA1 ubiquitin ligase.
  Proc Natl Acad Sci U S A, 104, 5794-5799.  
17631495 D.Kressler, M.B.Hock, and A.Kralli (2007).
Coactivators PGC-1beta and SRC-1 interact functionally to promote the agonist activity of the selective estrogen receptor modulator tamoxifen.
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17137423 D.L.Bain, A.F.Heneghan, K.D.Connaghan-Jones, and M.T.Miura (2007).
Nuclear receptor structure: implications for function.
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17992292 E.A.Hillard, P.Pigeon, A.Vessières, C.Amatore, and G.Jaouen (2007).
The influence of phenolic hydroxy substitution on the electron transfer and anti-cancer properties of compounds based on the 2-ferrocenyl-1-phenyl-but-1-ene motif.
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17475621 E.L.Reineke, H.Liu, M.Lam, Y.Liu, and H.Y.Kao (2007).
Aberrant association of promyelocytic leukemia protein-retinoic acid receptor-alpha with coactivators contributes to its ability to regulate gene expression.
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17223708 E.Wright, J.Vincent, and E.J.Fernandez (2007).
Thermodynamic characterization of the interaction between CAR-RXR and SRC-1 peptide by isothermal titration calorimetry.
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17456742 F.F.Vajdos, L.R.Hoth, K.F.Geoghegan, S.P.Simons, P.K.LeMotte, D.E.Danley, M.J.Ammirati, and J.Pandit (2007).
The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene.
  Protein Sci, 16, 897-905.
PDB code: 2ouz
17584613 H.B.Zhou, K.W.Nettles, J.B.Bruning, Y.Kim, A.Joachimiak, S.Sharma, K.E.Carlson, F.Stossi, B.S.Katzenellenbogen, G.L.Greene, and J.A.Katzenellenbogen (2007).
Elemental isomerism: a boron-nitrogen surrogate for a carbon-carbon double bond increases the chemical diversity of estrogen receptor ligands.
  Chem Biol, 14, 659-669.
PDB code: 2q6j
17455211 H.J.Li, Z.K.Haque, A.Chen, and M.Mendelsohn (2007).
RIF-1, a novel nuclear receptor corepressor that associates with the nuclear matrix.
  J Cell Biochem, 102, 1021-1035.  
17937915 J.B.Bruning, M.J.Chalmers, S.Prasad, S.A.Busby, T.M.Kamenecka, Y.He, K.W.Nettles, and P.R.Griffin (2007).
Partial agonists activate PPARgamma using a helix 12 independent mechanism.
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PDB codes: 2q59 2q5p 2q5s 2q61 2q6r 2q6s
17556356 J.Kallen, R.Lattmann, R.Beerli, A.Blechschmidt, M.J.Blommers, M.Geiser, J.Ottl, J.M.Schlaeppi, A.Strauss, and B.Fournier (2007).
Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism.
  J Biol Chem, 282, 23231-23239.
PDB code: 2pjl
17264933 J.M.Davis, L.K.Tsou, and A.D.Hamilton (2007).
Synthetic non-peptide mimetics of alpha-helices.
  Chem Soc Rev, 36, 326-334.  
17223545 J.W.Pike, M.B.Meyer, M.Watanuki, S.Kim, L.A.Zella, J.A.Fretz, M.Yamazaki, and N.K.Shevde (2007).
Perspectives on mechanisms of gene regulation by 1,25-dihydroxyvitamin D3 and its receptor.
  J Steroid Biochem Mol Biol, 103, 389-395.  
17721435 K.A.Green, and J.S.Carroll (2007).
Oestrogen-receptor-mediated transcription and the influence of co-factors and chromatin state.
  Nat Rev Cancer, 7, 713-722.  
17436259 K.Stierand, and M.Rarey (2007).
From Modeling to Medicinal Chemistry: Automatic Generation of Two-Dimensional Complex Diagrams.
  ChemMedChem, 2, 853-860.  
17468738 K.W.Nettles, J.B.Bruning, G.Gil, E.E.O'Neill, J.Nowak, Y.Guo, A.Hughs, Y.Kim, E.R.DeSombre, R.Dilis, R.N.Hanson, A.Joachimiak, and G.L.Greene (2007).
Structural plasticity in the oestrogen receptor ligand-binding domain.
  EMBO Rep, 8, 563-568.
PDB code: 2p15
17254542 L.A.Zella, C.Y.Chang, D.P.McDonnell, and J.Wesley Pike (2007).
The vitamin D receptor interacts preferentially with DRIP205-like LxxLL motifs.
  Arch Biochem Biophys, 460, 206-212.  
17503894 L.Gennari, D.Merlotti, F.Valleggi, G.Martini, and R.Nuti (2007).
Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development.
  Drugs Aging, 24, 361-379.  
17387660 M.Awais, M.Sato, and Y.Umezawa (2007).
Imaging of selective nuclear receptor modulator-induced conformational changes in the nuclear receptor to allow interaction with coactivator and corepressor proteins in living cells.
  Chembiochem, 8, 737-743.  
17115070 M.Ning, C.Zhou, J.Weng, S.Zhang, D.Chen, C.Yang, H.Wang, J.Ren, L.Zhou, C.Jin, and M.W.Wang (2007).
Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134).
  Br J Pharmacol, 150, 19-28.  
17768726 M.W.Büttner, C.Burschka, J.O.Daiss, D.Ivanova, N.Rochel, S.Kammerer, C.Peluso-Iltis, A.Bindler, C.Gaudon, P.Germain, D.Moras, H.Gronemeyer, and R.Tacke (2007).
Silicon analogues of the retinoid agonists TTNPB and 3-methyl-TTNPB, disila-TTNPB and disila-3-methyl-TTNPB: chemistry and biology.
  Chembiochem, 8, 1688-1699.  
17283072 N.Heldring, T.Pawson, D.McDonnell, E.Treuter, J.A.Gustafsson, and A.C.Pike (2007).
Structural insights into corepressor recognition by antagonist-bound estrogen receptors.
  J Biol Chem, 282, 10449-10455.
PDB codes: 2jf9 2jfa
18007036 N.Jouravel, E.Sablin, L.A.Arnold, R.K.Guy, and R.J.Fletterick (2007).
Interaction between the androgen receptor and a segment of its corepressor SHP.
  Acta Crystallogr D Biol Crystallogr, 63, 1198-1200.
PDB code: 2z4j
17908797 Q.Li, M.J.Chu, and J.Xu (2007).
Tissue- and nuclear receptor-specific function of the C-terminal LXXLL motif of coactivator NCoA6/AIB3 in mice.
  Mol Cell Biol, 27, 8073-8086.  
17565270 S.Kato, M.S.Kim, K.Yamaoka, and R.Fujiki (2007).
Mechanisms of transcriptional repression by 1,25(OH)2 vitamin D.
  Curr Opin Nephrol Hypertens, 16, 297-304.  
17827713 S.Suzuki, S.Nishida, K.Ohno, and T.Santa (2007).
Modulation of coactivator recruitment by cooperative ligand binding to human Estrogen receptor alpha and beta.
  Biol Pharm Bull, 30, 1641-1647.  
17135255 S.Wang, C.Zhang, S.K.Nordeen, and D.J.Shapiro (2007).
In vitro fluorescence anisotropy analysis of the interaction of full-length SRC1a with estrogen receptors alpha and beta supports an active displacement model for coregulator utilization.
  J Biol Chem, 282, 2765-2775.  
17948058 T.Saitoh, M.Igura, T.Obita, T.Ose, R.Kojima, K.Maenaka, T.Endo, and D.Kohda (2007).
Tom20 recognizes mitochondrial presequences through dynamic equilibrium among multiple bound states.
  EMBO J, 26, 4777-4787.
PDB codes: 2v1s 2v1t
17186017 V.C.Jordan (2007).
Chemoprevention of breast cancer with selective oestrogen-receptor modulators.
  Nat Rev Cancer, 7, 46-53.  
17765940 V.C.Jordan (2007).
New insights into the metabolism of tamoxifen and its role in the treatment and prevention of breast cancer.
  Steroids, 72, 829-842.  
17300979 V.Nahoum, and W.Bourguet (2007).
Androgen and estrogen receptors: potential of crystallography in the fight against cancer.
  Int J Biochem Cell Biol, 39, 1280-1287.  
17606915 W.H.Bisson, A.V.Cheltsov, N.Bruey-Sedano, B.Lin, J.Chen, N.Goldberger, L.T.May, A.Christopoulos, J.T.Dalton, P.M.Sexton, X.K.Zhang, and R.Abagyan (2007).
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
  Proc Natl Acad Sci U S A, 104, 11927-11932.  
17384075 W.Y.Peh, E.Reimhult, H.F.Teh, J.S.Thomsen, and X.Su (2007).
Understanding ligand binding effects on the conformation of estrogen receptor alpha-DNA complexes: a combinational quartz crystal microbalance with dissipation and surface plasmon resonance study.
  Biophys J, 92, 4415-4423.  
17627277 W.Zwart, A.Griekspoor, V.Berno, K.Lakeman, K.Jalink, M.Mancini, J.Neefjes, and R.Michalides (2007).
PKA-induced resistance to tamoxifen is associated with an altered orientation of ERalpha towards co-activator SRC-1.
  EMBO J, 26, 3534-3544.  
17284330 Y.E.Timsit, and M.Negishi (2007).
CAR and PXR: the xenobiotic-sensing receptors.
  Steroids, 72, 231-246.  
17215127 Y.Xue, E.Chao, W.J.Zuercher, T.M.Willson, J.L.Collins, and M.R.Redinbo (2007).
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
  Bioorg Med Chem, 15, 2156-2166.
PDB code: 2o9i
16483936 A.Cvoro, C.Tzagarakis-Foster, D.Tatomer, S.Paruthiyil, M.S.Fox, and D.C.Leitman (2006).
Distinct roles of unliganded and liganded estrogen receptors in transcriptional repression.
  Mol Cell, 21, 555-564.  
16930291 A.Vedani, M.Dobler, and M.A.Lill (2006).
The challenge of predicting drug toxicity in silico.
  Basic Clin Pharmacol Toxicol, 99, 195-208.  
16402138 A.Vessières, S.Top, W.Beck, E.Hillard, and G.Jaouen (2006).
Metal complex SERMs (selective oestrogen receptor modulators). The influence of different metal units on breast cancer cell antiproliferative effects.
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16511587 C.K.Glass (2006).
Going nuclear in metabolic and cardiovascular disease.
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16493426 C.K.Glass, and S.Ogawa (2006).
Combinatorial roles of nuclear receptors in inflammation and immunity.
  Nat Rev Immunol, 6, 44-55.  
16514628 C.Scafoglio, C.Ambrosino, L.Cicatiello, L.Altucci, M.Ardovino, P.Bontempo, N.Medici, A.M.Molinari, A.Nebbioso, A.Facchiano, R.A.Calogero, R.Elkon, N.Menini, R.Ponzone, N.Biglia, P.Sismondi, M.De Bortoli, and A.Weisz (2006).
Comparative gene expression profiling reveals partially overlapping but distinct genomic actions of different antiestrogens in human breast cancer cells.
  J Cell Biochem, 98, 1163-1184.  
16261397 D.J.Britton, I.R.Hutcheson, J.M.Knowlden, D.Barrow, M.Giles, R.A.McClelland, J.M.Gee, and R.I.Nicholson (2006).
Bidirectional cross talk between ERalpha and EGFR signalling pathways regulates tamoxifen-resistant growth.
  Breast Cancer Res Treat, 96, 131-146.  
16778215 D.Sharma, N.K.Saxena, N.E.Davidson, and P.M.Vertino (2006).
Restoration of tamoxifen sensitivity in estrogen receptor-negative breast cancer cells: tamoxifen-bound reactivated ER recruits distinctive corepressor complexes.
  Cancer Res, 66, 6370-6378.  
17068076 D.Zhou, J.J.Ye, Y.Li, K.Lui, and S.Chen (2006).
The molecular basis of the interaction between the proline-rich SH3-binding motif of PNRC and estrogen receptor alpha.
  Nucleic Acids Res, 34, 5974-5986.  
16892391 E.Hillard, A.Vessières, F.Le Bideau, D.Plazuk, D.Spera, M.Huché, and G.Jaouen (2006).
A series of unconjugated ferrocenyl phenols: prospects as anticancer agents.
  ChemMedChem, 1, 551-559.  
16608856 F.Stossi, V.S.Likhite, J.A.Katzenellenbogen, and B.S.Katzenellenbogen (2006).
Estrogen-occupied estrogen receptor represses cyclin G2 gene expression and recruits a repressor complex at the cyclin G2 promoter.
  J Biol Chem, 281, 16272-16278.  
16645950 H.Neubauer, S.E.Clare, R.Kurek, T.Fehm, D.Wallwiener, K.Sotlar, A.Nordheim, W.Wozny, G.P.Schwall, S.Poznanović, C.Sastri, C.Hunzinger, W.Stegmann, A.Schrattenholz, and M.A.Cahill (2006).
Breast cancer proteomics by laser capture microdissection, sample pooling, 54-cm IPG IEF, and differential iodine radioisotope detection.
  Electrophoresis, 27, 1840-1852.  
16541309 H.S.Seo, D.G.DeNardo, Y.Jacquot, I.Laïos, D.S.Vidal, C.R.Zambrana, G.Leclercq, and P.H.Brown (2006).
Stimulatory effect of genistein and apigenin on the growth of breast cancer cells correlates with their ability to activate ER alpha.
  Breast Cancer Res Treat, 99, 121-134.  
16537187 J.B.Hargis, and S.T.Nakajima (2006).
Resumption of menses with initiation of letrozole after five years of amenorrhea on tamoxifen: caution needed when using tamoxifen followed by aromatase inhibitors.
  Cancer Invest, 24, 174-177.  
16328721 J.K.Hess-Wilson, J.Boldison, K.E.Weaver, and K.E.Knudsen (2006).
Xenoestrogen action in breast cancer: impact on ER-dependent transcription and mitogenesis.
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17085477 J.Lopez-Garcia, M.Periyasamy, R.S.Thomas, M.Christian, M.Leao, P.Jat, K.B.Kindle, D.M.Heery, M.G.Parker, L.Buluwela, T.Kamalati, and S.Ali (2006).
ZNF366 is an estrogen receptor corepressor that acts through CtBP and histone deacetylases.
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16892386 J.T.Moore, J.L.Collins, and K.H.Pearce (2006).
The nuclear receptor superfamily and drug discovery.
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16539836 J.Yan, S.Y.Tsai, and M.J.Tsai (2006).
SRC-3/AIB1: transcriptional coactivator in oncogenesis.
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16565070 K.L.Damm, and H.A.Carlson (2006).
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17157789 L.H.Wang, X.Y.Yang, X.Zhang, P.An, H.J.Kim, J.Huang, R.Clarke, C.K.Osborne, J.K.Inman, E.Appella, and W.L.Farrar (2006).
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PDB codes: 2gp7 2gpo 2gpp 2gpu 2gpv
16555356 M.Awais, M.Sato, X.Lee, and Y.Umezawa (2006).
A fluorescent indicator to visualize activities of the androgen receptor ligands in single living cells.
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16532451 M.Y.Mizutani, Y.Takamatsu, T.Ichinose, K.Nakamura, and A.Itai (2006).
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18850210 N.M.Saarinen, C.Bingham, S.Lorenzetti, A.Mortensen, S.Mäkelä, P.Penttinen, I.K.Sørensen, L.M.Valsta, F.Virgili, G.Vollmer, A.Wärri, and O.Zierau (2006).
Tools to evaluate estrogenic potency of dietary phytoestrogens:A consensus paper from the EU Thematic Network "Phytohealth" (QLKI-2002-2453).
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16871612 N.Saito, and A.Kittaka (2006).
Highly potent vitamin D receptor antagonists: design, synthesis, and biological evaluation.
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16892382 N.Vicker, H.R.Lawrence, G.M.Allan, C.Bubert, A.Smith, H.J.Tutill, A.Purohit, J.M.Day, M.F.Mahon, M.J.Reed, and B.V.Potter (2006).
Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.
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16683264 N.W.Allen, and N.L.Thompson (2006).
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16469706 P.Zhu, S.H.Baek, E.M.Bourk, K.A.Ohgi, I.Garcia-Bassets, H.Sanjo, S.Akira, P.F.Kotol, C.K.Glass, M.G.Rosenfeld, and D.W.Rose (2006).
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An intramolecular folding sensor for imaging estrogen receptor-ligand interactions.
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PDB codes: 1zky 2b1v 2fai
16492776 S.H.Baek, K.A.Ohgi, C.A.Nelson, D.Welsbie, C.Chen, C.L.Sawyers, D.W.Rose, and M.G.Rosenfeld (2006).
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells.
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16978016 T.S.Dowers, Z.H.Qin, G.R.Thatcher, and J.L.Bolton (2006).
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16453361 U.Schatzschneider, and N.Metzler-Nolte (2006).
New principles in medicinal organometallic chemistry.
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16962311 V.Neduva, and R.B.Russell (2006).
Peptides mediating interaction networks: new leads at last.
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16427018 X.Wei, H.Xu, and D.Kufe (2006).
MUC1 oncoprotein stabilizes and activates estrogen receptor alpha.
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16938840 Y.K.Leung, P.Mak, S.Hassan, and S.M.Ho (2006).
Estrogen receptor (ER)-beta isoforms: a key to understanding ER-beta signaling.
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PDB codes: 2f8x 2f8y
16633364 Y.Shang (2006).
Molecular mechanisms of oestrogen and SERMs in endometrial carcinogenesis.
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16940184 Y.Tateishi, R.Sonoo, Y.Sekiya, N.Sunahara, M.Kawano, M.Wayama, R.Hirota, Y.Kawabe, A.Murayama, S.Kato, K.Kimura, and J.Yanagisawa (2006).
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A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta.
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PDB code: 2fsz
16892383 Z.Q.Wang, N.Weber, Y.J.Lou, and P.Proksch (2006).
Prenylflavonoids as nonsteroidal phytoestrogens and related structure-activity relationships.
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The Estradiol-Dihydrotestosterone model of prostate cancer.
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Potent inhibitors of LXXLL-based protein-protein interactions.
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15964825 B.D.Paul, L.Fu, D.R.Buchholz, and Y.B.Shi (2005).
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15767587 C.Oostenbrink, and W.F.van Gunsteren (2005).
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15860367 C.Y.Chang, and D.P.McDonnell (2005).
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15563469 E.Estébanez-Perpiñá, J.M.Moore, E.Mar, E.Delgado-Rodrigues, P.Nguyen, J.D.Baxter, B.M.Buehrer, P.Webb, R.J.Fletterick, and R.K.Guy (2005).
The molecular mechanisms of coactivator utilization in ligand-dependent transactivation by the androgen receptor.
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PDB codes: 1t5z 1t63 1t65 1xj7
15728727 E.H.Kong, N.Heldring, J.A.Gustafsson, E.Treuter, R.E.Hubbard, and A.C.Pike (2005).
Delineation of a unique protein-protein interaction site on the surface of the estrogen receptor.
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PDB code: 2bj4
15542861 F.A.Klein, R.A.Atkinson, N.Potier, D.Moras, and J.Cavarelli (2005).
Biochemical and NMR mapping of the interface between CREB-binding protein and ligand binding domains of nuclear receptor: beyond the LXXLL motif.
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Biochemical applications of mass spectrometry in pharmaceutical drug discovery.
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Molecular dynamics simulations reveal multiple pathways of ligand dissociation from thyroid hormone receptors.
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T:G mismatch-specific thymine-DNA glycosylase (TDG) as a coregulator of transcription interacts with SRC1 family members through a novel tyrosine repeat motif.
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Molecular modelling of the androgen receptor axis: rational basis for androgen receptor intervention in androgen-independent prostate cancer.
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16168139 R.Schiff, and C.K.Osborne (2005).
Endocrinology and hormone therapy in breast cancer: new insight into estrogen receptor-alpha function and its implication for endocrine therapy resistance in breast cancer.
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Advanced concepts in estrogen receptor biology and breast cancer endocrine resistance: implicated role of growth factor signaling and estrogen receptor coregulators.
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Function of nuclear sex hormone receptors in gene regulation.
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15647825 S.Kim, N.K.Shevde, and J.W.Pike (2005).
1,25-Dihydroxyvitamin D3 stimulates cyclic vitamin D receptor/retinoid X receptor DNA-binding, co-activator recruitment, and histone acetylation in intact osteoblasts.
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15957004 V.Perissi, and M.G.Rosenfeld (2005).
Controlling nuclear receptors: the circular logic of cofactor cycles.
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Structural and biochemical mechanisms for the specificity of hormone binding and coactivator assembly by mineralocorticoid receptor.
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PDB code: 2a3i
14617632 A.J.Krieg, S.A.Krieg, B.S.Ahn, and D.J.Shapiro (2004).
Interplay between estrogen response element sequence and ligands controls in vivo binding of estrogen receptor to regulated genes.
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15049842 A.K.Galande, K.S.Bramlett, T.P.Burris, J.L.Wittliff, and A.F.Spatola (2004).
Thioether side chain cyclization for helical peptide formation: inhibitors of estrogen receptor-coactivator interactions.
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A new series of estrogen receptor modulators: effect of alkyl substituents on receptor-binding affinity.
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Directed evolution of ligand dependence: small-molecule-activated protein splicing.
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15184363 A.Zhang, P.L.Yeung, C.W.Li, S.C.Tsai, G.K.Dinh, X.Wu, H.Li, and J.D.Chen (2004).
Identification of a novel family of ankyrin repeats containing cofactors for p160 nuclear receptor coactivators.
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15519887 B.E.Black, and B.M.Paschal (2004).
Intranuclear organization and function of the androgen receptor.
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15107424 B.He, S.Bai, A.T.Hnat, R.I.Kalman, J.T.Minges, C.Patterson, and E.M.Wilson (2004).
An androgen receptor NH2-terminal conserved motif interacts with the COOH terminus of the Hsp70-interacting protein (CHIP).
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Thyroxine-thyroid hormone receptor interactions.
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PDB codes: 1xzx 1y0x
15036253 C.J.Gruber, D.M.Gruber, I.M.Gruber, F.Wieser, and J.C.Huber (2004).
Anatomy of the estrogen response element.
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14992717 C.K.Glass, D.P.McDonnell, and E.Jensen (2004).
The jensen symposium; a tribute to a pioneer in the field of nuclear receptor biology.
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14696186 C.Oostenbrink, and W.F.van Gunsteren (2004).
Free energies of binding of polychlorinated biphenyls to the estrogen receptor from a single simulation.
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Recognition and accommodation at the androgen receptor coactivator binding interface.
  PLoS Biol, 2, E274.
PDB codes: 1t73 1t74 1t76 1t79 1t7f 1t7m 1t7r 1t7t
15469931 E.Morais-de-Sá, P.J.Pereira, M.J.Saraiva, and A.M.Damas (2004).
The crystal structure of transthyretin in complex with diethylstilbestrol: a promising template for the design of amyloid inhibitors.
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PDB codes: 1tt6 1tz8
15576033 E.S.Manas, Z.B.Xu, R.J.Unwalla, and W.S.Somers (2004).
Understanding the selectivity of genistein for human estrogen receptor-beta using X-ray crystallography and computational methods.
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PDB codes: 1x7j 1x7r
15246430 G.Benoit, M.Malewicz, and T.Perlmann (2004).
Digging deep into the pockets of orphan nuclear receptors: insights from structural studies.
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15282735 G.D.Cappon, M.Horimoto, and M.E.Hurtt (2004).
Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in male rats.
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15161930 H.Greschik, R.Flaig, J.P.Renaud, and D.Moras (2004).
Structural basis for the deactivation of the estrogen-related receptor gamma by diethylstilbestrol or 4-hydroxytamoxifen and determinants of selectivity.
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PDB codes: 1s9p 1s9q 1tfc 1vjb
15190886 H.L.Jessop, R.F.Suswillo, S.C.Rawlinson, G.Zaman, K.Lee, V.Das-Gupta, A.A.Pitsillides, and L.E.Lanyon (2004).
Osteoblast-like cells from estrogen receptor alpha knockout mice have deficient responses to mechanical strain.
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15310754 H.Liu, C.K.Shaw, E.L.Reineke, Y.Liu, and H.Y.Kao (2004).
Retinoid X receptor alpha (RXRalpha) helix 12 plays an inhibitory role in the recruitment of the p160 co-activators by unliganded RXRalpha/retinoic acid receptor alpha heterodimers.
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15270657 J.Eng-Wong, and J.A.Zujewski (2004).
Raloxifene and its role in breast cancer prevention.
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15166356 J.L.Turgeon, D.P.McDonnell, K.A.Martin, and P.M.Wise (2004).
Hormone therapy: physiological complexity belies therapeutic simplicity.
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Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer.
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15450240 K.H.Pearce, M.A.Iannone, C.A.Simmons, and J.G.Gray (2004).
Discovery of novel nuclear receptor modulating ligands: an integral role for peptide interaction profiling.
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15610733 K.Suino, L.Peng, R.Reynolds, Y.Li, J.Y.Cha, J.J.Repa, S.A.Kliewer, and H.E.Xu (2004).
The nuclear xenobiotic receptor CAR: structural determinants of constitutive activation and heterodimerization.
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PDB code: 1xls
15215582 K.Takeyama, S.Ito, S.Sawatsubashi, Y.Shirode, A.Yamamoto, E.Suzuki, A.Maki, K.Yamagata, Y.Zhao, A.Kouzmenko, T.Tabata, and S.Kato (2004).
A novel genetic system for analysis of co-activators for the N-terminal transactivation function domain of the human androgen receptor.
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14967140 K.W.Nettles, J.Sun, J.T.Radek, S.Sheng, A.L.Rodriguez, J.A.Katzenellenbogen, B.S.Katzenellenbogen, and G.L.Greene (2004).
Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors.
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15500393 L.Picariello, F.Tonelli, and M.L.Brandi (2004).
Selective oestrogen receptor modulators in desmoid tumours.
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14699072 M.Kian Tee, I.Rogatsky, C.Tzagarakis-Foster, A.Cvoro, J.An, R.J.Christy, K.R.Yamamoto, and D.C.Leitman (2004).
Estradiol and selective estrogen receptor modulators differentially regulate target genes with estrogen receptors alpha and beta.
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14977406 M.L.Privalsky (2004).
The role of corepressors in transcriptional regulation by nuclear hormone receptors.
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15123269 N.Fokialakis, G.Lambrinidis, D.J.Mitsiou, N.Aligiannis, S.Mitakou, A.L.Skaltsounis, H.Pratsinis, E.Mikros, and M.N.Alexis (2004).
A new class of phytoestrogens; evaluation of the estrogenic activity of deoxybenzoins.
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Identification of tamoxifen-induced coregulator interaction surfaces within the ligand-binding domain of estrogen receptors.
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Recovering the true targets of specific ligands by virtual screening of the protein data bank.
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15207254 N.Platet, A.M.Cathiard, M.Gleizes, and M.Garcia (2004).
Estrogens and their receptors in breast cancer progression: a dual role in cancer proliferation and invasion.
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15193262 R.Michalides, A.Griekspoor, A.Balkenende, D.Verwoerd, L.Janssen, K.Jalink, A.Floore, A.Velds, L.van't Veer, and J.Neefjes (2004).
Tamoxifen resistance by a conformational arrest of the estrogen receptor alpha after PKA activation in breast cancer.
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15049832 R.S.Savkur, and T.P.Burris (2004).
The coactivator LXXLL nuclear receptor recognition motif.
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In vivo potentiation of human oestrogen receptor alpha by Cdk7-mediated phosphorylation.
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Packing, specificity, and mutability at the binding interface between the p160 coactivator and CREB-binding protein.
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15340084 S.Malik, M.Guermah, C.X.Yuan, W.Wu, S.Yamamura, and R.G.Roeder (2004).
Structural and functional organization of TRAP220, the TRAP/mediator subunit that is targeted by nuclear receptors.
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14711828 S.S.Taneja, S.Ha, N.K.Swenson, I.P.Torra, S.Rome, P.D.Walden, H.Y.Huang, E.Shapiro, M.J.Garabedian, and S.K.Logan (2004).
ART-27, an androgen receptor coactivator regulated in prostate development and cancer.
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The biological role of estrogen receptors alpha and beta in cancer.
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Selective estrogen-receptor modulators (SERMs) in the cyclopentadienylrhenium tricarbonyl series: synthesis and biological behaviour.
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Ligand-selective inhibition of the interaction of steroid receptor coactivators and estrogen receptor isoforms.
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15050912 V.C.Jordan (2004).
Selective estrogen receptor modulation: concept and consequences in cancer.
  Cancer Cell, 5, 207-213.  
15289619 W.Shao, E.K.Keeton, D.P.McDonnell, and M.Brown (2004).
Coactivator AIB1 links estrogen receptor transcriptional activity and stability.
  Proc Natl Acad Sci U S A, 101, 11599-11604.  
14680484 W.Shao, and M.Brown (2004).
Advances in estrogen receptor biology: prospects for improvements in targeted breast cancer therapy.
  Breast Cancer Res, 6, 39-52.  
15105832 Y.Brelivet, S.Kammerer, N.Rochel, O.Poch, and D.Moras (2004).
Signature of the oligomeric behaviour of nuclear receptors at the sequence and structural level.
  EMBO Rep, 5, 423-429.  
15031286 Y.Liu, B.O.Kim, C.Kao, C.Jung, J.T.Dalton, and J.J.He (2004).
Tip110, the human immunodeficiency virus type 1 (HIV-1) Tat-interacting protein of 110 kDa as a negative regulator of androgen receptor (AR) transcriptional activation.
  J Biol Chem, 279, 21766-21773.  
15174161 Y.Shi, and J.T.Koh (2004).
Light-activated transcription and repression by using photocaged SERMs.
  Chembiochem, 5, 788-796.  
15538384 Y.Tateishi, Y.Kawabe, T.Chiba, S.Murata, K.Ichikawa, A.Murayama, K.Tanaka, T.Baba, S.Kato, and J.Yanagisawa (2004).
Ligand-dependent switching of ubiquitin-proteasome pathways for estrogen receptor.
  EMBO J, 23, 4813-4823.  
13679575 A.M.Leduc, J.O.Trent, J.L.Wittliff, K.S.Bramlett, S.L.Briggs, N.Y.Chirgadze, Y.Wang, T.P.Burris, and A.F.Spatola (2003).
Helix-stabilized cyclic peptides as selective inhibitors of steroid receptor-coactivator interactions.
  Proc Natl Acad Sci U S A, 100, 11273-11278.
PDB code: 1pcg
12536206 B.C.Kallenberger, J.D.Love, V.K.Chatterjee, and J.W.Schwabe (2003).
A dynamic mechanism of nuclear receptor activation and its perturbation in a human disease.
  Nat Struct Biol, 10, 136-140.  
12732728 B.D.Nguyen, K.L.Abbott, K.Potempa, M.S.Kobor, J.Archambault, J.Greenblatt, P.Legault, and J.G.Omichinski (2003).
NMR structure of a complex containing the TFIIF subunit RAP74 and the RNA polymerase II carboxyl-terminal domain phosphatase FCP1.
  Proc Natl Acad Sci U S A, 100, 5688-5693.
PDB code: 1onv
12665583 B.Farboud, H.Hauksdottir, Y.Wu, and M.L.Privalsky (2003).
Isotype-restricted corepressor recruitment: a constitutively closed helix 12 conformation in retinoic acid receptors beta and gamma interferes with corepressor recruitment and prevents transcriptional repression.
  Mol Cell Biol, 23, 2844-2858.  
12612084 B.He, and E.M.Wilson (2003).
Electrostatic modulation in steroid receptor recruitment of LXXLL and FXXLF motifs.
  Mol Cell Biol, 23, 2135-2150.  
12540843 B.J.Cheskis, N.J.McKenna, C.W.Wong, J.Wong, B.Komm, C.R.Lyttle, and B.W.O'Malley (2003).
Hierarchical affinities and a bipartite interaction model for estrogen receptor isoforms and full-length steroid receptor coactivator (SRC/p160) family members.
  J Biol Chem, 278, 13271-13277.  
12618500 C.K.Osborne, V.Bardou, T.A.Hopp, G.C.Chamness, S.G.Hilsenbeck, S.A.Fuqua, J.Wong, D.C.Allred, G.M.Clark, and R.Schiff (2003).
Role of the estrogen receptor coactivator AIB1 (SRC-3) and HER-2/neu in tamoxifen resistance in breast cancer.
  J Natl Cancer Inst, 95, 353-361.  
12840015 C.Zhang, D.R.Dowd, A.Staal, C.Gu, J.B.Lian, A.J.van Wijnen, G.S.Stein, and P.N.MacDonald (2003).
Nuclear coactivator-62 kDa/Ski-interacting protein is a nuclear matrix-associated coactivator that may couple vitamin D receptor-mediated transcription and RNA splicing.
  J Biol Chem, 278, 35325-35336.  
12736255 C.Zhao, A.Koide, J.Abrams, S.Deighton-Collins, A.Martinez, J.A.Schwartz, S.Koide, and D.F.Skafar (2003).
Mutation of Leu-536 in human estrogen receptor-alpha alters the coupling between ligand binding, transcription activation, and receptor conformation.
  J Biol Chem, 278, 27278-27286.  
12874288 D.Chen, M.J.Lucey, F.Phoenix, J.Lopez-Garcia, S.M.Hart, R.Losson, L.Buluwela, R.C.Coombes, P.Chambon, P.Schär, and S.Ali (2003).
T:G mismatch-specific thymine-DNA glycosylase potentiates transcription of estrogen-regulated genes through direct interaction with estrogen receptor alpha.
  J Biol Chem, 278, 38586-38592.  
12491500 E.Diamanti-Kandarakis, G.P.Sykiotis, and A.G.Papavassiliou (2003).
Selective modulation of postmenopausal women: cutting the Gordian knot of hormone replacement therapy with breast carcinoma.
  Cancer, 97, 12-20.  
  16604176 E.H.Xu, and M.H.Lambert (2003).
Structural insights into regulation of nuclear receptors by ligands.
  Nucl Recept Signal, 1, e004.  
12820970 E.P.Sablin, I.N.Krylova, R.J.Fletterick, and H.A.Ingraham (2003).
Structural basis for ligand-independent activation of the orphan nuclear receptor LRH-1.
  Mol Cell, 11, 1575-1585.
PDB code: 1pk5
12725419 G.Hudelist, K.Czerwenka, E.Kubista, E.Marton, K.Pischinger, and C.F.Singer (2003).
Expression of sex steroid receptors and their co-factors in normal and malignant breast tissue: AIB1 is a carcinoma-specific co-activator.
  Breast Cancer Res Treat, 78, 193-204.  
12909775 G.L.Starova, M.S.Egorov, E.S.Vasiljeva, and A.G.Shavva (2003).
  Acta Crystallogr C, 59, o451-o453.  
12796488 H.Yamamoto, N.K.Shevde, A.Warrier, L.A.Plum, H.F.DeLuca, and J.W.Pike (2003).
2-Methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 potently stimulates gene-specific DNA binding of the vitamin D receptor in osteoblasts.
  J Biol Chem, 278, 31756-31765.  
12520523 J.W.Pike, P.Pathrose, O.Barmina, C.Y.Chang, D.P.McDonnell, H.Yamamoto, and N.K.Shevde (2003).
Synthetic LXXLL peptide antagonize 1,25-dihydroxyvitamin D3-dependent transcription.
  J Cell Biochem, 88, 252-258.  
12809604 K.D.Baker, L.M.Shewchuk, T.Kozlova, M.Makishima, A.Hassell, B.Wisely, J.A.Caravella, M.H.Lambert, J.L.Reinking, H.Krause, C.S.Thummel, T.M.Willson, and D.J.Mangelsdorf (2003).
The Drosophila orphan nuclear receptor DHR38 mediates an atypical ecdysteroid signaling pathway.
  Cell, 113, 731-742.
PDB code: 1pdu
12579585 K.Nam, P.Marshall, R.M.Wolf, and W.Cornell (2003).
Simulation of the different biological activities of diethylstilbestrol (DES) on estrogen receptor alpha and estrogen-related receptor gamma.
  Biopolymers, 68, 130-138.  
12588987 L.N.Song, R.Herrell, S.Byers, S.Shah, E.M.Wilson, and E.P.Gelmann (2003).
Beta-catenin binds to the activation function 2 region of the androgen receptor and modulates the effects of the N-terminal domain and TIF2 on ligand-dependent transcription.
  Mol Cell Biol, 23, 1674-1687.  
12576474 L.Wu, Y.Wu, B.Gathings, M.Wan, X.Li, W.Grizzle, Z.Liu, C.Lu, Z.Mao, and X.Cao (2003).
Smad4 as a transcription corepressor for estrogen receptor alpha.
  J Biol Chem, 278, 15192-15200.  
12819202 M.Färnegårdh, T.Bonn, S.Sun, J.Ljunggren, H.Ahola, A.Wilhelmsson, J.A.Gustafsson, and M.Carlquist (2003).
The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands.
  J Biol Chem, 278, 38821-38828.
PDB codes: 1pq6 1pq9 1pqc
12715898 M.Hentschke, C.Schulze, U.Süsens, and U.Borgmeyer (2003).
Characterization of calmodulin binding to the orphan nuclear receptor Errgamma.
  Biol Chem, 384, 473-482.  
12777627 M.Schapira, B.M.Raaka, S.Das, L.Fan, M.Totrov, Z.Zhou, S.R.Wilson, R.Abagyan, and H.H.Samuels (2003).
Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking.
  Proc Natl Acad Sci U S A, 100, 7354-7359.  
12808380 M.W.Draper, and W.W.Chin (2003).
Molecular and clinical evidence for the unique nature of individual selective estrogen receptor modulators.
  Clin Obstet Gynecol, 46, 265-297.  
12711630 M.Yoon, H.Lee, S.Jeong, J.J.Kim, C.J.Nicol, K.W.Nam, M.Kim, B.G.Cho, and G.T.Oh (2003).
Peroxisome proliferator-activated receptor alpha is involved in the regulation of lipid metabolism by ginseng.
  Br J Pharmacol, 138, 1295-1302.  
12794859 N.Foy, E.Stéphan, A.Vessières, E.Salomon, J.M.Heldt, M.Huché, and G.Jaouen (2003).
Synthesis, receptor binding, molecular modeling, and proliferative assays of a series of 17alpha-arylestradiols.
  Chembiochem, 4, 494-503.  
  12904255 P.Webb, C.Valentine, P.Nguyen, R.H.Price, A.Marimuthu, B.L.West, J.D.Baxter, and P.J.Kushner (2003).
ERbeta Binds N-CoR in the Presence of Estrogens via an LXXLL-like Motif in the N-CoR C-terminus.
  Nucl Recept, 1, 4.  
12482846 P.Webb, P.Nguyen, and P.J.Kushner (2003).
Differential SERM effects on corepressor binding dictate ERalpha activity in vivo.
  J Biol Chem, 278, 6912-6920.  
12917445 S.Benko, J.D.Love, M.Beládi, J.W.Schwabe, and L.Nagy (2003).
Molecular determinants of the balance between co-repressor and co-activator recruitment to the retinoic acid receptor.
  J Biol Chem, 278, 43797-43806.  
14673100 S.Borngraeber, M.J.Budny, G.Chiellini, S.T.Cunha-Lima, M.Togashi, P.Webb, J.D.Baxter, T.S.Scanlan, and R.J.Fletterick (2003).
Ligand selectivity by seeking hydrophobicity in thyroid hormone receptor.
  Proc Natl Acad Sci U S A, 100, 15358-15363.
PDB code: 1q4x
12838268 S.J.Teague (2003).
Implications of protein flexibility for drug discovery.
  Nat Rev Drug Discov, 2, 527-541.  
12547836 S.O.Mueller, J.M.Hall, D.L.Swope, L.C.Pedersen, and K.S.Korach (2003).
Molecular determinants of the stereoselectivity of agonist activity of estrogen receptors (ER) alpha and beta.
  J Biol Chem, 278, 12255-12262.  
12520525 S.Peleg, A.Ismail, M.R.Uskokovic, and Z.Avnur (2003).
Evidence for tissue- and cell-type selective activation of the vitamin D receptor by Ro-26-9228, a noncalcemic analog of vitamin D3.
  J Cell Biochem, 88, 267-273.  
12964159 S.S.Muddana, and B.R.Peterson (2003).
Fluorescent cellular sensors of steroid receptor ligands.
  Chembiochem, 4, 848-855.  
12945660 S.Suzuki, K.Ohno, T.Santa, and K.Imai (2003).
Study on interactions of endocrine disruptors with estrogen receptor-beta using fluorescence polarization.
  Anal Sci, 19, 1103-1108.  
12496244 S.T.Pearce, H.Liu, and V.C.Jordan (2003).
Modulation of estrogen receptor alpha function and stability by tamoxifen and a critical amino acid (Asp-538) in helix 12.
  J Biol Chem, 278, 7630-7638.  
12424754 S.Yamada, M.Shimizu, and K.Yamamoto (2003).
Structure-function relationships of vitamin D including ligand recognition by the vitamin D receptor.
  Med Res Rev, 23, 89.  
12738788 T.Fujita, Y.Kobayashi, O.Wada, Y.Tateishi, L.Kitada, Y.Yamamoto, H.Takashima, A.Murayama, T.Yano, T.Baba, S.Kato, Y.Kawabe, and J.Yanagisawa (2003).
Full activation of estrogen receptor alpha activation function-1 induces proliferation of breast cancer cells.
  J Biol Chem, 278, 26704-26714.  
12767224 T.Ostberg, M.Jacobsson, A.Attersand, A.Mata de Urquiza, and L.Jendeberg (2003).
A triple mutant of the Drosophila ERR confers ligand-induced suppression of activity.
  Biochemistry, 42, 6427-6435.  
12482977 T.Suzuki, M.Kasahara, H.Yoshioka, K.Morohashi, and K.Umesono (2003).
LXXLL-related motifs in Dax-1 have target specificity for the orphan nuclear receptors Ad4BP/SF-1 and LRH-1.
  Mol Cell Biol, 23, 238-249.  
12556447 V.H.Coulthard, S.Matsuda, and D.M.Heery (2003).
An extended LXXLL motif sequence determines the nuclear receptor binding specificity of TRAP220.
  J Biol Chem, 278, 10942-10951.  
12842037 Y.Li, M.H.Lambert, and H.E.Xu (2003).
Activation of nuclear receptors: a perspective from structural genomics.
  Structure, 11, 741-746.  
12502716 Y.Wu, W.W.Chin, Y.Wang, and T.P.Burris (2003).
Ligand and coactivator identity determines the requirement of the charge clamp for coactivation of the peroxisome proliferator-activated receptor gamma.
  J Biol Chem, 278, 8637-8644.  
11953755 A.K.Shiau, D.Barstad, J.T.Radek, M.J.Meyers, K.W.Nettles, B.S.Katzenellenbogen, J.A.Katzenellenbogen, D.A.Agard, and G.L.Greene (2002).
Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.
  Nat Struct Biol, 9, 359-364.
PDB codes: 1l2i 1l2j
11818562 A.Koide, S.Abbatiello, L.Rothgery, and S.Koide (2002).
Probing protein conformational changes in living cells by using designer binding proteins: application to the estrogen receptor.
  Proc Natl Acad Sci U S A, 99, 1253-1258.
PDB code: 2ocf
12215540 A.N.Moraitis, V.Giguère, and C.C.Thompson (2002).
Novel mechanism of nuclear receptor corepressor interaction dictated by activation function 2 helix determinants.
  Mol Cell Biol, 22, 6831-6841.  
11963993 A.Ohno, M.Shimizu, and S.Yamada (2002).
Fluorinated vitamin D analogs to probe the conformation of vitamin D in its receptor complex: 19F-NMR studies and biological activity.
  Chem Pharm Bull (Tokyo), 50, 475-483.  
12177783 A.S.Levenson, I.L.Kliakhandler, K.M.Svoboda, K.M.Pease, S.A.Kaiser, J.E.Ward, and V.C.Jordan (2002).
Molecular classification of selective oestrogen receptor modulators on the basis of gene expression profiles of breast cancer cells expressing oestrogen receptor alpha.
  Br J Cancer, 87, 449-456.  
11937504 A.Wärnmark, E.Treuter, J.A.Gustafsson, R.E.Hubbard, A.M.Brzozowski, and A.C.Pike (2002).
Interaction of transcriptional intermediary factor 2 nuclear receptor box peptides with the coactivator binding site of estrogen receptor alpha.
  J Biol Chem, 277, 21862-21868.
PDB codes: 1gwq 1gwr
12000757 B.He, L.W.Lee, J.T.Minges, and E.M.Wilson (2002).
Dependence of selective gene activation on the androgen receptor NH2- and COOH-terminal interaction.
  J Biol Chem, 277, 25631-25639.  
11897660 B.Lefebvre, K.Ozato, and P.Lefebvre (2002).
Phosphorylation of histone H3 is functionally linked to retinoic acid receptor beta promoter activation.
  EMBO Rep, 3, 335-340.  
11923515 B.S.Katzenellenbogen, and J.A.Katzenellenbogen (2002).
Biomedicine. Defining the "S" in SERMs.
  Science, 295, 2380-2381.  
12138189 D.Li, T.Li, F.Wang, H.Tian, and H.H.Samuels (2002).
Functional evidence for retinoid X receptor (RXR) as a nonsilent partner in the thyroid hormone receptor/RXR heterodimer.
  Mol Cell Biol, 22, 5782-5792.  
  12004085 D.S.Goodsell (2002).
The molecular perspective: tamoxifen and the estrogen receptor.
  Stem Cells, 20, 267-268.  
11884406 E.A.Rozhkova, N.Fujimoto, I.Sagami, S.N.Daff, and T.Shimizu (2002).
Interactions between the isolated oxygenase and reductase domains of neuronal nitric-oxide synthase: assessing the role of calmodulin.
  J Biol Chem, 277, 16888-16894.  
11864604 H.Greschik, J.M.Wurtz, S.Sanglier, W.Bourguet, A.van Dorsselaer, D.Moras, and J.P.Renaud (2002).
Structural and functional evidence for ligand-independent transcriptional activation by the estrogen-related receptor 3.
  Mol Cell, 9, 303-313.
PDB code: 1kv6
  11781162 H.Hong, W.Tong, H.Fang, L.Shi, Q.Xie, J.Wu, R.Perkins, J.D.Walker, W.Branham, and D.M.Sheehan (2002).
Prediction of estrogen receptor binding for 58,000 chemicals using an integrated system of a tree-based model with structural alerts.
  Environ Health Perspect, 110, 29-36.  
11751902 H.Liu, W.C.Park, D.J.Bentrem, K.P.McKian, A.d.e. .L.Reyes, J.A.Loweth, J.M.Schafer, J.W.Zapf, and V.C.Jordan (2002).
Structure-function relationships of the raloxifene-estrogen receptor-alpha complex for regulating transforming growth factor-alpha expression in breast cancer cells.
  J Biol Chem, 277, 9189-9198.  
12101224 I.Dussault, M.Lin, K.Hollister, M.Fan, J.Termini, M.A.Sherman, and B.M.Forman (2002).
A structural model of the constitutive androstane receptor defines novel interactions that mediate ligand-independent activity.
  Mol Cell Biol, 22, 5270-5280.  
12481024 I.Rogatsky, H.F.Luecke, D.C.Leitman, and K.R.Yamamoto (2002).
Alternate surfaces of transcriptional coregulator GRIP1 function in different glucocorticoid receptor activation and repression contexts.
  Proc Natl Acad Sci U S A, 99, 16701-16706.  
11823467 J.A.Schwartz, L.Zhong, S.Deighton-Collins, C.Zhao, and D.F.Skafar (2002).
Mutations targeted to a predicted helix in the extreme carboxyl-terminal region of the human estrogen receptor-alpha alter its response to estradiol and 4-hydroxytamoxifen.
  J Biol Chem, 277, 13202-13209.  
11972046 J.C.Ghosh, X.Yang, A.Zhang, M.H.Lambert, H.Li, H.E.Xu, and J.D.Chen (2002).
Interactions that determine the assembly of a retinoid X receptor/corepressor complex.
  Proc Natl Acad Sci U S A, 99, 5842-5847.  
12198482 J.C.Young, and F.U.Hartl (2002).
Chaperones and transcriptional regulation by nuclear receptors.
  Nat Struct Biol, 9, 640-642.  
11782480 J.D.Love, J.T.Gooch, S.Benko, C.Li, L.Nagy, V.K.Chatterjee, R.M.Evans, and J.W.Schwabe (2002).
The structural basis for the specificity of retinoid-X receptor-selective agonists: new insights into the role of helix H12.
  J Biol Chem, 277, 11385-11391.
PDB code: 1h9u
11824555 K.Morito, T.Aomori, T.Hirose, J.Kinjo, J.Hasegawa, S.Ogawa, S.Inoue, M.Muramatsu, and Y.Masamune (2002).
Interaction of phytoestrogens with estrogen receptors alpha and beta (II).
  Biol Pharm Bull, 25, 48-52.  
12444966 K.Steketee, C.A.Berrevoets, H.J.Dubbink, P.Doesburg, R.Hersmus, A.O.Brinkmann, and J.Trapman (2002).
Amino acids 3-13 and amino acids in and flanking the 23FxxLF27 motif modulate the interaction between the N-terminal and ligand-binding domain of the androgen receptor.
  Eur J Biochem, 269, 5780-5791.  
12115546 K.Steketee, L.Timmerman, A.C.Ziel-van der Made, P.Doesburg, A.O.Brinkmann, and J.Trapman (2002).
Broadened ligand responsiveness of androgen receptor mutants obtained by random amino acid substitution of H874 and mutation hot spot T877 in prostate cancer.
  Int J Cancer, 100, 309-317.  
12372281 K.Takeyama, S.Ito, A.Yamamoto, H.Tanimoto, T.Furutani, H.Kanuka, M.Miura, T.Tabata, and S.Kato (2002).
Androgen-dependent neurodegeneration by polyglutamine-expanded human androgen receptor in Drosophila.
  Neuron, 35, 855-864.  
12394261 L.A.Hammond, G.Brown, R.G.Keedwell, J.Durham, and R.A.Chandraratna (2002).
The prospects of retinoids in the treatment of prostate cancer.
  Anticancer Drugs, 13, 781-790.  
12123286 L.L.Hart, and J.R.Davie (2002).
The estrogen receptor: more than the average transcription factor.
  Biochem Cell Biol, 80, 335-341.  
12237083 M.A.Ortiz, Y.Bayon, F.J.Lopez-Hernandez, and F.J.Piedrafita (2002).
Retinoids in combination therapies for the treatment of cancer: mechanisms and perspectives.
  Drug Resist Updat, 5, 162-175.  
11849367 M.A.Shupnik (2002).
Oestrogen receptors, receptor variants and oestrogen actions in the hypothalamic-pituitary axis.
  J Neuroendocrinol, 14, 85-94.  
12486878 M.Fu, C.Wang, J.Wang, B.T.Zafonte, M.P.Lisanti, and R.G.Pestell (2002).
Acetylation in hormone signaling and the cell cycle.
  Cytokine Growth Factor Rev, 13, 259-276.  
12180985 M.Hentschke, U.Süsens, and U.Borgmeyer (2002).
Domains of ERRgamma that mediate homodimerization and interaction with factors stimulating DNA binding.
  Eur J Biochem, 269, 4086-4097.  
12004807 M.Nichols, and K.S.McCarty (2002).
Functional mutations of estrogen receptor protein: assay for detection.
  Breast Cancer Res Treat, 72, 61-68.  
11909518 N.J.McKenna, and B.W.O'Malley (2002).
Combinatorial control of gene expression by nuclear receptors and coregulators.
  Cell, 108, 465-474.  
11839696 P.Ciana, E.Vegeto, M.Beato, P.Chambon, J.A.Gustafsson, M.Parker, W.Wahli, and A.Maggi (2002).
Looking at nuclear receptors from the heights of Erice. Workshop on nuclear receptor structure and function.
  EMBO Rep, 3, 125-129.  
12469913 P.Pathrose, O.Barmina, C.Y.Chang, D.P.McDonnell, N.K.Shevde, and J.W.Pike (2002).
Inhibition of 1,25-dihydroxyvitamin D3-dependent transcription by synthetic LXXLL peptide antagonists that target the activation domains of the vitamin D and retinoid X receptors.
  J Bone Miner Res, 17, 2196-2205.  
12218053 Q.Wang, D.Sharma, Y.Ren, and J.D.Fondell (2002).
A coregulatory role for the TRAP-mediator complex in androgen receptor-mediated gene expression.
  J Biol Chem, 277, 42852-42858.  
12077320 R.L.Rich, L.R.Hoth, K.F.Geoghegan, T.A.Brown, P.K.LeMotte, S.P.Simons, P.Hensley, and D.G.Myszka (2002).
Kinetic analysis of estrogen receptor/ligand interactions.
  Proc Natl Acad Sci U S A, 99, 8562-8567.  
12453411 R.Métivier, A.Stark, G.Flouriot, M.R.Hübner, H.Brand, G.Penot, D.Manu, S.Denger, G.Reid, M.Kos, R.B.Russell, O.Kah, F.Pakdel, and F.Gannon (2002).
A dynamic structural model for estrogen receptor-alpha activation by ligands, emphasizing the role of interactions between distant A and E domains.
  Mol Cell, 10, 1019-1032.  
12067682 R.M.O'Regan, and V.C.Jordan (2002).
The evolution of tamoxifen therapy in breast cancer: selective oestrogen-receptor modulators and downregulators.
  Lancet Oncol, 3, 207-214.  
12635173 S.Ali, and R.C.Coombes (2002).
Endocrine-responsive breast cancer and strategies for combating resistance.
  Nat Rev Cancer, 2, 101-112.  
12142447 S.H.McLaughlin, and S.E.Jackson (2002).
Folding and stability of the ligand-binding domain of the glucocorticoid receptor.
  Protein Sci, 11, 1926-1936.  
  12634121 S.H.Safe, L.Pallaroni, K.Yoon, K.Gaido, S.Ross, and D.McDonnell (2002).
Problems for risk assessment of endocrine-active estrogenic compounds.
  Environ Health Perspect, 110, 925-929.  
12145311 S.Kaul, P.J.Murphy, J.Chen, L.Brown, W.B.Pratt, and S.S.Simons (2002).
Mutations at positions 547-553 of rat glucocorticoid receptors reveal that hsp90 binding requires the presence, but not defined composition, of a seven-amino acid sequence at the amino terminus of the ligand binding domain.
  J Biol Chem, 277, 36223-36232.  
  12122114 S.Nanni, M.Narducci, L.Della Pietra, F.Moretti, A.Grasselli, P.De Carli, A.Sacchi, A.Pontecorvi, and A.Farsetti (2002).
Signaling through estrogen receptors modulates telomerase activity in human prostate cancer.
  J Clin Invest, 110, 219-227.  
  15455059 S.Sasorith, I.M.Billas, T.Iwema, D.Moras, and J.M.Wurtz (2002).
Structure-based analysis of the ultraspiracle protein and docking studies of putative ligands.
  J Insect Sci, 2, 25.  
12360281 T.J.Powles (2002).
Anti-oestrogenic prevention of breast cancer--the make or break point.
  Nat Rev Cancer, 2, 787-794.  
12208951 T.Kino, A.Gragerov, O.Slobodskaya, M.Tsopanomichalou, G.P.Chrousos, and G.N.Pavlakis (2002).
Human immunodeficiency virus type 1 (HIV-1) accessory protein Vpr induces transcription of the HIV-1 and glucocorticoid-responsive promoters by binding directly to p300/CBP coactivators.
  J Virol, 76, 9724-9734.  
  12381545 T.Kino, A.Vottero, E.Charmandari, and G.P.Chrousos (2002).
Familial/sporadic glucocorticoid resistance syndrome and hypertension.
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12185669 V.Giguère (2002).
To ERR in the estrogen pathway.
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11971969 W.Shao, S.Halachmi, and M.Brown (2002).
ERAP140, a conserved tissue-specific nuclear receptor coactivator.
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12111992 X.Gu (2002).
Helix 12 in the human estrogen receptor (hER) is essential for the hER function by overcoming nucleosome repression in yeast.
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12093804 Y.C.Hu, C.R.Shyr, W.Che, X.M.Mu, E.Kim, and C.Chang (2002).
Suppression of estrogen receptor-mediated transcription and cell growth by interaction with TR2 orphan receptor.
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11923541 Y.Shang, and M.Brown (2002).
Molecular determinants for the tissue specificity of SERMs.
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12473098 Y.Xu, F.Fang, Y.Chu, D.Jones, and G.Jones (2002).
Activation of transcription through the ligand-binding pocket of the orphan nuclear receptor ultraspiracle.
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11250199 A.C.Pike, A.M.Brzozowski, J.Walton, R.E.Hubbard, A.G.Thorsell, Y.L.Li, J.A.Gustafsson, and M.Carlquist (2001).
Structural insights into the mode of action of a pure antiestrogen.
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PDB code: 1hj1
11340063 A.C.Steinmetz, J.P.Renaud, and D.Moras (2001).
Binding of ligands and activation of transcription by nuclear receptors.
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11564893 A.K.Teo, H.K.Oh, R.B.Ali, and B.F.Li (2001).
The modified human DNA repair enzyme O(6)-methylguanine-DNA methyltransferase is a negative regulator of estrogen receptor-mediated transcription upon alkylation DNA damage.
  Mol Cell Biol, 21, 7105-7114.  
11157757 C.J.Schwartz, H.M.Sampson, D.Hlousek, A.Percival-Smith, J.W.Copeland, A.J.Simmonds, and H.M.Krause (2001).
FTZ-Factor1 and Fushi tarazu interact via conserved nuclear receptor and coactivator motifs.
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11452016 C.M.Klinge (2001).
Estrogen receptor interaction with estrogen response elements.
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11689423 C.Stehlin, J.M.Wurtz, A.Steinmetz, E.Greiner, R.Schüle, D.Moras, and J.P.Renaud (2001).
X-ray structure of the orphan nuclear receptor RORbeta ligand-binding domain in the active conformation.
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PDB code: 1k4w
11389589 C.W.Wong, B.Komm, and B.J.Cheskis (2001).
Structure-function evaluation of ER alpha and beta interplay with SRC family coactivators. ER selective ligands.
  Biochemistry, 40, 6756-6765.  
11432835 D.E.Clark, C.E.Poteet-Smith, J.A.Smith, and D.A.Lannigan (2001).
Rsk2 allosterically activates estrogen receptor alpha by docking to the hormone-binding domain.
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11791116 D.J.Bentrem, R.M.O'Regan, and V.C.Jordan (2001).
New strategies for the treatment of breast cancer.
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11438648 D.L.Osburn, G.Shao, H.M.Seidel, and I.G.Schulman (2001).
Ligand-dependent degradation of retinoid X receptors does not require transcriptional activity or coactivator interactions.
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11390668 D.L.Stenoien, A.C.Nye, M.G.Mancini, K.Patel, M.Dutertre, B.W.O'Malley, C.L.Smith, A.S.Belmont, and M.A.Mancini (2001).
Ligand-mediated assembly and real-time cellular dynamics of estrogen receptor alpha-coactivator complexes in living cells.
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11768608 D.O.Azorsa, H.E.Cunliffe, and P.S.Meltzer (2001).
Association of steroid receptor coactivator AIB1 with estrogen receptor-alpha in breast cancer cells.
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11113208 F.Sauvé, L.D.McBroom, J.Gallant, A.N.Moraitis, F.Labrie, and V.Giguère (2001).
CIA, a novel estrogen receptor coactivator with a bifunctional nuclear receptor interacting determinant.
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11171988 G.M.Clayton, S.Y.Peak-Chew, R.M.Evans, and J.W.Schwabe (2001).
The structure of the ultraspiracle ligand-binding domain reveals a nuclear receptor locked in an inactive conformation.
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PDB code: 1hg4
11737619 H.W.Schnaper, A.C.Poncelet, and T.Hayashida (2001).
Talking at cross purposes: molecular interactions downstream from TGF-beta.
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11390665 H.Y.Mak, and M.G.Parker (2001).
Use of suppressor mutants to probe the function of estrogen receptor-p160 coactivator interactions.
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11339974 J.G.Emery, E.H.Ohlstein, and M.Jaye (2001).
Therapeutic modulation of transcription factor activity.
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11297193 J.Russo, Y.F.Hu, Q.Tahin, D.Mihaila, C.Slater, M.H.Lareef, and I.H.Russo (2001).
Carcinogenicity of estrogens in human breast epithelial cells.
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11320241 J.S.Sack, K.F.Kish, C.Wang, R.M.Attar, S.E.Kiefer, Y.An, G.Y.Wu, J.E.Scheffler, M.E.Salvati, S.R.Krystek, R.Weinmann, and H.M.Einspahr (2001).
Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.
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PDB codes: 1i37 1i38
11397643 K.C.Lee, and W.Lee Kraus (2001).
Nuclear receptors, coactivators and chromatin: new approaches, new insights.
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11181953 K.Pettersson, and J.A.Gustafsson (2001).
Role of estrogen receptor beta in estrogen action.
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11500849 M.A.Iannone, T.G.Consler, K.H.Pearce, J.B.Stimmel, D.J.Parks, and J.G.Gray (2001).
Multiplexed molecular interactions of nuclear receptors using fluorescent microspheres.
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11551916 M.B.Kumar, P.Ramadoss, R.K.Reen, J.P.Vanden Heuvel, and G.H.Perdew (2001).
The Q-rich subdomain of the human Ah receptor transactivation domain is required for dioxin-mediated transcriptional activity.
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11250900 M.Watanabe, J.Yanagisawa, H.Kitagawa, K.Takeyama, S.Ogawa, Y.Arao, M.Suzawa, Y.Kobayashi, T.Yano, H.Yoshikawa, Y.Masuhiro, and S.Kato (2001).
A subfamily of RNA-binding DEAD-box proteins acts as an estrogen receptor alpha coactivator through the N-terminal activation domain (AF-1) with an RNA coactivator, SRA.
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11689448 M.Y.Kim, S.J.Hsiao, and W.L.Kraus (2001).
A role for coactivators and histone acetylation in estrogen receptor alpha-mediated transcription initiation.
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11509661 N.Vo, C.Fjeld, and R.H.Goodman (2001).
Acetylation of nuclear hormone receptor-interacting protein RIP140 regulates binding of the transcriptional corepressor CtBP.
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11447273 P.Coward, D.Lee, M.V.Hull, and J.M.Lehmann (2001).
4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor gamma.
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11315340 R.Gust, V.Lubczyk, K.Schmidt, and U.Shihada (2001).
Synthesis, conformational studies, and investigations on the estrogen receptor binding of [R/S-1-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]platinum(II) complexes.
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11392537 R.Tedesco, M.K.Youngman, S.R.Wilson, and J.A.Katzenellenbogen (2001).
Synthesis and evaluation of hexahydrochrysene and tetrahydrobenzofluorene ligands for the estrogen receptor.
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11180760 S.Kato (2001).
Estrogen receptor-mediated cross-talk with growth factor signaling pathways.
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Nuclear-receptor interactions on DNA-response elements.
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11197334 S.R.Stauffer, Y.Huang, C.J.Coletta, R.Tedesco, and J.A.Katzenellenbogen (2001).
Estrogen pyrazoles: defining the pyrazole core structure and the orientation of substituents in the ligand binding pocket of the estrogen receptor.
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11197335 S.R.Stauffer, Y.R.Huang, Z.D.Aron, C.J.Coletta, J.Sun, B.S.Katzenellenbogen, and J.A.Katzenellenbogen (2001).
Triarylpyrazoles with basic side chains: development of pyrazole-based estrogen receptor antagonists.
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11592991 T.Suzuki, H.Kawasaki, R.T.Yu, H.Ueda, and K.Umesono (2001).
Segmentation gene product Fushi tarazu is an LXXLL motif-dependent coactivator for orphan receptor FTZ-F1.
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11600716 T.Tsuji, M.Onimaru, and H.Yanagawa (2001).
Random multi-recombinant PCR for the construction of combinatorial protein libraries.
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11607933 U.Egner, N.Heinrich, M.Ruff, M.Gangloff, A.Mueller-Fahrnow, and J.M.Wurtz (2001).
Different ligands-different receptor conformations: modeling of the hER alpha LBD in complex with agonists and antagonists.
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11170455 X.Be, Y.Hong, J.Wei, E.J.Androphy, J.J.Chen, and J.D.Baleja (2001).
Solution structure determination and mutational analysis of the papillomavirus E6 interacting peptide of E6AP.
  Biochemistry, 40, 1293-1299.
PDB code: 1eqx
11238912 X.Hu, Y.Li, and M.A.Lazar (2001).
Determinants of CoRNR-dependent repression complex assembly on nuclear hormone receptors.
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11585838 X.Yuan, M.L.Lu, T.Li, and S.P.Balk (2001).
SRY interacts with and negatively regulates androgen receptor transcriptional activity.
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11553641 Y.Yamamoto, O.Wada, M.Suzawa, Y.Yogiashi, T.Yano, S.Kato, and J.Yanagisawa (2001).
The tamoxifen-responsive estrogen receptor alpha mutant D351Y shows reduced tamoxifen-dependent interaction with corepressor complexes.
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10747799 A.S.Budhu, and N.Noy (2000).
On the role of the carboxyl-terminal helix of RXR in the interactions of the receptor with ligand.
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10703925 A.Verstuyf, L.Verlinden, E.van Etten, L.Shi, Y.Wu, C.D'Halleweyn, D.Van Haver, G.D.Zhu, Y.J.Chen, X.Zhou, M.R.Haussler, P.De Clercq, M.Vandewalle, H.Van Baelen, C.Mathieu, and R.Bouillon (2000).
Biological activity of CD-ring modified 1alpha,25-dihydroxyvitamin D analogues: C-ring and five-membered D-ring analogues.
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The p23 molecular chaperones act at a late step in intracellular receptor action to differentially affect ligand efficacies.
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10681591 C.Leo, H.Li, and J.D.Chen (2000).
Differential mechanisms of nuclear receptor regulation by receptor-associated coactivator 3.
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Activation of estrogen receptor alpha by S118 phosphorylation involves a ligand-dependent interaction with TFIIH and participation of CDK7.
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10736263 D.F.Smith (2000).
Chaperones in progesterone receptor complexes.
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10911988 D.M.Lonard, Z.Nawaz, C.L.Smith, and B.W.O'Malley (2000).
The 26S proteasome is required for estrogen receptor-alpha and coactivator turnover and for efficient estrogen receptor-alpha transactivation.
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11032772 E.V.Hestermann, J.J.Stegeman, and M.E.Hahn (2000).
Relative contributions of affinity and intrinsic efficacy to aryl hydrocarbon receptor ligand potency.
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10681503 F.Caira, P.Antonson, M.Pelto-Huikko, E.Treuter, and J.A.Gustafsson (2000).
Cloning and characterization of RAP250, a novel nuclear receptor coactivator.
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11094064 F.Ledo, A.M.Carrión, W.A.Link, B.Mellström, and J.R.Naranjo (2000).
DREAM-alphaCREM interaction via leucine-charged domains derepresses downstream regulatory element-dependent transcription.
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10788463 Haan, S.Chusacultanachai, C.Mao, B.S.Katzenellenbogen, and D.J.Shapiro (2000).
Estrogen receptor-KRAB chimeras are potent ligand-dependent repressors of estrogen-regulated gene expression.
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10757780 I.Tzameli, P.Pissios, E.G.Schuetz, and D.D.Moore (2000).
The xenobiotic compound 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene is an agonist ligand for the nuclear receptor CAR.
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10913186 J.A.Iñiguez-Lluhí, and D.Pearce (2000).
A common motif within the negative regulatory regions of multiple factors inhibits their transcriptional synergy.
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10653634 J.E.Riby, C.Feng, Y.C.Chang, C.M.Schaldach, G.L.Firestone, and L.F.Bjeldanes (2000).
The major cyclic trimeric product of indole-3-carbinol is a strong agonist of the estrogen receptor signaling pathway.
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10866661 J.Font de Mora, and M.Brown (2000).
AIB1 is a conduit for kinase-mediated growth factor signaling to the estrogen receptor.
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10760302 J.Llopis, S.Westin, M.Ricote, Z.Wang, C.Y.Cho, R.Kurokawa, T.M.Mullen, D.W.Rose, M.G.Rosenfeld, R.Y.Tsien, C.K.Glass, and J.Wang (2000).
Ligand-dependent interactions of coactivators steroid receptor coactivator-1 and peroxisome proliferator-activated receptor binding protein with nuclear hormone receptors can be imaged in live cells and are required for transcription.
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A new model for 20-hydroxyecdysone and dibenzoylhydrazine binding: a homology modeling and docking approach.
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10845098 J.Zhang, and M.A.Lazar (2000).
The mechanism of action of thyroid hormones.
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10677485 K.Yamamoto, H.Masuno, M.Choi, K.Nakashima, T.Taga, H.Ooizumi, K.Umesono, W.Sicinska, J.VanHooke, H.F.DeLuca, and S.Yamada (2000).
Three-dimensional modeling of and ligand docking to vitamin D receptor ligand binding domain.
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10648597 L.Johansson, A.Båvner, J.S.Thomsen, M.Färnegårdh, J.A.Gustafsson, and E.Treuter (2000).
The orphan nuclear receptor SHP utilizes conserved LXXLL-related motifs for interactions with ligand-activated estrogen receptors.
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11005855 M.B.Hawkins, J.W.Thornton, D.Crews, J.K.Skipper, A.Dotte, and P.Thomas (2000).
Identification of a third distinct estrogen receptor and reclassification of estrogen receptors in teleosts.
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11094341 M.Herdick, A.Steinmeyer, and C.Carlberg (2000).
Carboxylic ester antagonists of 1alpha,25-dihydroxyvitamin D(3) show cell-specific actions.
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10848596 M.Li, G.Pascual, and C.K.Glass (2000).
Peroxisome proliferator-activated receptor gamma-dependent repression of the inducible nitric oxide synthase gene.
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11250728 M.Ruff, M.Gangloff, J.M.Wurtz, and D.Moras (2000).
Estrogen receptor transcription and transactivation: Structure-function relationship in DNA- and ligand-binding domains of estrogen receptors.
  Breast Cancer Res, 2, 353-359.  
10655475 M.Schapira, B.M.Raaka, H.H.Samuels, and R.Abagyan (2000).
Rational discovery of novel nuclear hormone receptor antagonists.
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10869427 N.K.Shevde, A.C.Bendixen, K.M.Dienger, and J.W.Pike (2000).
Estrogens suppress RANK ligand-induced osteoclast differentiation via a stromal cell independent mechanism involving c-Jun repression.
  Proc Natl Acad Sci U S A, 97, 7829-7834.  
11015194 N.Swamy, W.Xu, N.Paz, J.C.Hsieh, M.R.Haussler, G.J.Maalouf, S.C.Mohr, and R.Ray (2000).
Molecular modeling, affinity labeling, and site-directed mutagenesis define the key points of interaction between the ligand-binding domain of the vitamin D nuclear receptor and 1 alpha,25-dihydroxyvitamin D3.
  Biochemistry, 39, 12162-12171.  
10835357 P.F.Egea, A.Mitschler, N.Rochel, M.Ruff, P.Chambon, and D.Moras (2000).
Crystal structure of the human RXRalpha ligand-binding domain bound to its natural ligand: 9-cis retinoic acid.
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PDB code: 1fby
10983973 P.Pissios, I.Tzameli, P.Kushner, and D.D.Moore (2000).
Dynamic stabilization of nuclear receptor ligand binding domains by hormone or corepressor binding.
  Mol Cell, 6, 245-253.  
10984507 R.L.Luciano, and A.C.Wilson (2000).
N-terminal transcriptional activation domain of LZIP comprises two LxxLL motifs and the host cell factor-1 binding motif.
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10882139 R.T.Gampe, V.G.Montana, M.H.Lambert, A.B.Miller, R.K.Bledsoe, M.V.Milburn, S.A.Kliewer, T.M.Willson, and H.E.Xu (2000).
Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.
  Mol Cell, 5, 545-555.
PDB codes: 1fm6 1fm9
10970886 R.T.Gampe, V.G.Montana, M.H.Lambert, G.B.Wisely, M.V.Milburn, and H.E.Xu (2000).
Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix.
  Genes Dev, 14, 2229-2241.
PDB codes: 1g1u 1g5y
10809746 S.Chen, J.Cui, K.Nakamura, R.C.Ribeiro, B.L.West, and D.G.Gardner (2000).
Coactivator-vitamin D receptor interactions mediate inhibition of the atrial natriuretic peptide promoter.
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10947845 S.Kato, Y.Masuhiro, M.Watanabe, Y.Kobayashi, K.I.Takeyama, H.Endoh, and J.Yanagisawa (2000).
Molecular mechanism of a cross-talk between oestrogen and growth factor signalling pathways.
  Genes Cells, 5, 593-601.  
10890575 V.L.Baker, D.Leitman, and R.B.Jaffe (2000).
Selective estrogen receptor modulators in reproductive medicine and biology.
  Obstet Gynecol Surv, 55, S21-S47.  
11050318 W.Bourguet, P.Germain, and H.Gronemeyer (2000).
Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications.
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10882070 W.Bourguet, V.Vivat, J.M.Wurtz, P.Chambon, H.Gronemeyer, and D.Moras (2000).
Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains.
  Mol Cell, 5, 289-298.
PDB code: 1dkf
10594021 Y.K.Lee, H.Dell, D.H.Dowhan, M.Hadzopoulou-Cladaras, and D.D.Moore (2000).
The orphan nuclear receptor SHP inhibits hepatocyte nuclear factor 4 and retinoid X receptor transactivation: two mechanisms for repression.
  Mol Cell Biol, 20, 187-195.  
10891484 Y.Ren, E.Behre, Z.Ren, J.Zhang, Q.Wang, and J.D.Fondell (2000).
Specific structural motifs determine TRAP220 interactions with nuclear hormone receptors.
  Mol Cell Biol, 20, 5433-5446.  
10469641 A.C.Pike, A.M.Brzozowski, R.E.Hubbard, T.Bonn, A.G.Thorsell, O.Engström, J.Ljunggren, J.A.Gustafsson, and M.Carlquist (1999).
Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist.
  EMBO J, 18, 4608-4618.
PDB codes: 1qkm 1qkn