PDBsum entry 1err

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Nuclear receptor PDB id
Protein chains
225 a.a. *
223 a.a. *
RAL ×2
Waters ×100
* Residue conservation analysis
PDB id:
Name: Nuclear receptor
Title: Human estrogen receptor ligand-binding domain in complex wit raloxifene
Structure: Estrogen receptor. Chain: a, b. Fragment: ligand-binding domain. Synonym: estrogen receptor, er-lbd, er-alpha. Engineered: yes. Other_details: ligand-binding domain (domain e - residues 3 complex with the selective antagonist raloxifene
Source: Homo sapiens. Human. Organism_taxid: 9606. Strain: jm109. Variant: c1857. Gene: er alpha. Expressed in: escherichia coli. Expression_system_taxid: 562. Expression_system_variant: c1857.
Biol. unit: Dimer (from PDB file)
2.60Å     R-factor:   0.219     R-free:   0.299
Authors: A.M.Brzozowski,A.C.W.Pike
Key ref:
A.M.Brzozowski et al. (1997). Molecular basis of agonism and antagonism in the oestrogen receptor. Nature, 389, 753-758. PubMed id: 9338790 DOI: 10.1038/39645
08-Sep-97     Release date:   16-Sep-98    
Go to PROCHECK summary

Protein chain
Pfam   ArchSchema ?
P03372  (ESR1_HUMAN) -  Estrogen receptor
595 a.a.
225 a.a.*
Protein chain
Pfam   ArchSchema ?
P03372  (ESR1_HUMAN) -  Estrogen receptor
595 a.a.
223 a.a.*
Key:    PfamA domain  Secondary structure  CATH domain
* PDB and UniProt seqs differ at 2 residue positions (black crosses)

 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     3 terms  


DOI no: 10.1038/39645 Nature 389:753-758 (1997)
PubMed id: 9338790  
Molecular basis of agonism and antagonism in the oestrogen receptor.
A.M.Brzozowski, A.C.Pike, Z.Dauter, R.E.Hubbard, T.Bonn, O.Engström, L.Ohman, G.L.Greene, J.A.Gustafsson, M.Carlquist.
Oestrogens are involved in the growth, development and homeostasis of a number of tissues. The physiological effects of these steroids are mediated by a ligand-inducible nuclear transcription factor, the oestrogen receptor (ER). Hormone binding to the ligand-binding domain (LBD) of the ER initiates a series of molecular events culminating in the activation or repression of target genes. Transcriptional regulation arises from the direct interaction of the ER with components of the cellular transcription machinery. Here we report the crystal structures of the LBD of ER in complex with the endogenous oestrogen, 17beta-oestradiol, and the selective antagonist raloxifene, at resolutions of 3.1 and 2.6 A, respectively. The structures provide a molecular basis for the distinctive pharmacophore of the ER and its catholic binding properties. Agonist and antagonist bind at the same site within the core of the LBD but demonstrate different binding modes. In addition, each class of ligand induces a distinct conformation in the transactivation domain of the LBD, providing structural evidence of the mechanism of antagonism.
  Selected figure(s)  
Figure 2.
Figure 2 Agonist and antagonist binding modes. a, The 3.1-┼ resolution, six-fold averaged electron-density map (using model phases) for the ER LBD-E[2] complex. b, The experimental, 2.6-┼ resolution electron-density map for the ER LBD-RAL complex after DMMULTI multicrystal averaging. In both cases, the map is contoured at 1 and overlaid on the final refined models. c, d, Schematic representation of the interactions made by E[2] (c) and RAL (d) within the binding cavity. Residues that interact with ligand and/or line the cavity are shown in theirapproximate positions. Those that make direct hydrogen bonds are depictedin ball-and-stick style with broken lines between the interacting atoms.The hydrogen-bond distances shown are averaged between the six (E[2]) or two (RAL) monomers. The atom names and ring nomenclature of E[2] are also given.
Figure 3.
Figure 3 Positioning of helix H12. Position is shown in a, the ER LBD-E[2] complex; and b, the ER LBD-RAL complex. H12 is drawn as a cylinder and coloured blue (E[2] complex) or green (RAL complex). The remainder of the ER LBD is shown in red. Dotted lines indicate unmodelled regions of the structures. Hydrophobic residues located in the groove between H3 and H5 (yellow) and Lys 362 (K362, pink) are depicted in space-filling form. The locations of Asp 538, Glu 542 and Asp 545 are highlighted (brown spheres) along with the helices that interact with H12 in the two complexes.
  The above figures are reprinted by permission from Macmillan Publishers Ltd: Nature (1997, 389, 753-758) copyright 1997.  
  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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18271749 E.R.Prossnitz, J.B.Arterburn, H.O.Smith, T.I.Oprea, L.A.Sklar, and H.J.Hathaway (2008).
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18980187 H.Xu, W.L.Kraus, and M.L.Shuler (2008).
Development of a stable dual cell-line GFP expression system to study estrogenic endocrine disruptors.
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17949972 J.L.Blum, M.O.James, L.D.Stuchal, and N.D.Denslow (2008).
Stimulation of transactivation of the largemouth bass estrogen receptors alpha, beta-a, and beta-b by methoxychlor and its mono- and bis-demethylated metabolites in HepG2 cells.
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Amphipathic benzenes are designed inhibitors of the estrogen receptor alpha/steroid receptor coactivator interaction.
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18787702 J.T.Bridgham, J.E.Brown, A.Rodríguez-Marí, J.M.Catchen, and J.W.Thornton (2008).
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18552192 J.Y.Damián-Almazo, A.Moreno, A.López-Munguía, X.Soberón, F.González-Muñoz, and G.Saab-Rincón (2008).
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18502379 J.Zhang, and D.S.Geller (2008).
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17512592 K.E.Tollefsen, and A.Julie Nilsen (2008).
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18462184 L.Gennari, D.Merlotti, V.D.Paola, and R.Nuti (2008).
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18655705 M.Paris, K.Pettersson, M.Schubert, S.Bertrand, I.Pongratz, H.Escriva, and V.Laudet (2008).
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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.
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17992702 R.H.Gee, A.Charles, N.Taylor, and P.D.Darbre (2008).
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18322525 R.Métivier, R.Gallais, C.Tiffoche, C.Le Péron, R.Z.Jurkowska, R.P.Carmouche, D.Ibberson, P.Barath, F.Demay, G.Reid, V.Benes, A.Jeltsch, F.Gannon, and G.Salbert (2008).
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19337586 S.L.Nott, Y.Huang, B.R.Fluharty, A.M.Sokolov, M.Huang, C.Cox, and M.Muyan (2008).
Do Estrogen Receptor beta Polymorphisms Play A Role in the Pharmacogenetics of Estrogen Signaling?
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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).
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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).
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Ab initio fragment molecular orbital study of ligand binding to human progesterone receptor ligand-binding domain.
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GPR30: A G protein-coupled receptor for estrogen.
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The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene.
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Molecular aspects of phytoestrogen selective binding at estrogen receptors.
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Oestrogen-receptor-mediated transcription and the influence of co-factors and chromatin state.
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The embryonic pregnancy signal oestradiol influences gene expression at the level of translational initiation in porcine endometrial cells.
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Hormone replacement therapy and lung cancer risk in Chinese.
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Structural characterization of the human androgen receptor ligand-binding domain complexed with EM5744, a rationally designed steroidal ligand bearing a bulky chain directed toward helix 12.
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Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development.
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Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134).
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27-Hydroxycholesterol is an endogenous SERM that inhibits the cardiovascular effects of estrogen.
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Structural insights into corepressor recognition by antagonist-bound estrogen receptors.
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Selective estrogen-receptor modulators and aromatase inhibitors: promising new medical therapies for endometriosis?
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17280694 P.Wolohan, and D.E.Reichert (2007).
CoMSIA and docking study of rhenium based estrogen receptor ligand analogs.
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The differential effects of bisphosphonates, SERMS (selective estrogen receptor modulators), and parathyroid hormone on bone remodeling in osteoporosis.
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Chemoprevention of breast cancer with selective oestrogen-receptor modulators.
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New insights into the metabolism of tamoxifen and its role in the treatment and prevention of breast cancer.
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Ockham's razor and selective androgen receptor modulators (SARMs): are we overlooking the role of 5alpha-reductase?
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Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
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PKA-induced resistance to tamoxifen is associated with an altered orientation of ERalpha towards co-activator SRC-1.
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CAR and PXR: the xenobiotic-sensing receptors.
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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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Combinatorial roles of nuclear receptors in inflammation and immunity.
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O-GlcNAc integrates the proteasome and transcriptome to regulate nuclear hormone receptors.
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Lactandrate: a D-homo-aza-androsterone alkylator in the treatment of breast cancer.
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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.
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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.
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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.
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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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16610793 J.W.Seo, J.S.Comninos, D.Y.Chi, D.W.Kim, K.E.Carlson, and J.A.Katzenellenbogen (2006).
Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: synthesis and structure-affinity relationship study of potential positron emission tomography agents for imaging estrogen receptors in breast cancer.
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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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16767794 K.Shimizu, M.Yamanaka, M.Gyokusen, S.Kaneko, M.Tsutsui, J.Sato, I.Sato, M.Sato, and R.Kondo (2006).
Estrogen-like activity and prevention effect of bone loss in calcium deficient ovariectomized rats by the extract of Pleurotus eryngii.
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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).
Disruption of estrogen receptor DNA-binding domain and related intramolecular communication restores tamoxifen sensitivity in resistant breast cancer.
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16990259 L.Wang, W.J.Zuercher, T.G.Consler, M.H.Lambert, A.B.Miller, L.A.Orband-Miller, D.D.McKee, T.M.Willson, and R.T.Nolte (2006).
X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation.
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PDB codes: 2gp7 2gpo 2gpp 2gpu 2gpv
16533397 L.Zhao, and R.D.Brinton (2006).
Select estrogens within the complex formulation of conjugated equine estrogens (Premarin) are protective against neurodegenerative insults: implications for a composition of estrogen therapy to promote neuronal function and prevent Alzheimer's disease.
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16835908 M.Raviscioni, Q.He, E.M.Salicru, C.L.Smith, and O.Lichtarge (2006).
Evolutionary identification of a subtype specific functional site in the ligand binding domain of steroid receptors.
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16418513 M.S.Beattie, J.P.Costantino, S.R.Cummings, D.L.Wickerham, V.G.Vogel, M.Dowsett, E.J.Folkerd, W.C.Willett, N.Wolmark, and S.E.Hankinson (2006).
Endogenous sex hormones, breast cancer risk, and tamoxifen response: an ancillary study in the NSABP Breast Cancer Prevention Trial (P-1).
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16914190 P.Ascenzi, A.Bocedi, and M.Marino (2006).
Structure-function relationship of estrogen receptor alpha and beta: impact on human health.
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16891362 P.Carlsson, S.Burendahl, and L.Nilsson (2006).
Unbinding of retinoic acid from the retinoic acid receptor by random expulsion molecular dynamics.
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16489580 P.D.Darbre (2006).
Metalloestrogens: an emerging class of inorganic xenoestrogens with potential to add to the oestrogenic burden of the human breast.
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18850212 P.Galluzzo, and M.Marino (2006).
Nutritional flavonoids impact on nuclear and extranuclear estrogen receptor activities.
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17043219 R.Paulmurugan, and S.S.Gambhir (2006).
An intramolecular folding sensor for imaging estrogen receptor-ligand interactions.
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16648639 R.W.Hsieh, S.S.Rajan, S.K.Sharma, Y.Guo, E.R.DeSombre, M.Mrksich, and G.L.Greene (2006).
Identification of ligands with bicyclic scaffolds provides insights into mechanisms of estrogen receptor subtype selectivity.
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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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16983671 S.Y.Huang, and X.Zou (2006).
An iterative knowledge-based scoring function to predict protein-ligand interactions: II. Validation of the scoring function.
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16451093 T.E.Vogelvang, M.J.van der Mooren, V.Mijatovic, and P.Kenemans (2006).
Emerging selective estrogen receptor modulators: special focus on effects on coronary heart disease in postmenopausal women.
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16978016 T.S.Dowers, Z.H.Qin, G.R.Thatcher, and J.L.Bolton (2006).
Bioactivation of Selective Estrogen Receptor Modulators (SERMs).
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16402113 V.C.Jordan (2006).
Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer.
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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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16823031 Y.Hamuro, S.J.Coales, J.A.Morrow, K.S.Molnar, S.J.Tuske, M.R.Southern, and P.R.Griffin (2006).
Hydrogen/deuterium-exchange (H/D-Ex) of PPARgamma LBD in the presence of various modulators.
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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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16633364 Y.Shang (2006).
Molecular mechanisms of oestrogen and SERMs in endometrial carcinogenesis.
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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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15743834 A.Fritah, C.Saucier, J.Mester, G.Redeuilh, and M.Sabbah (2005).
p21WAF1/CIP1 selectively controls the transcriptional activity of estrogen receptor alpha.
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16222726 A.K.Galande, K.S.Bramlett, J.O.Trent, T.P.Burris, J.L.Wittliff, and A.F.Spatola (2005).
Potent inhibitors of LXXLL-based protein-protein interactions.
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16356126 A.K.Garg, T.A.Buchholz, and B.B.Aggarwal (2005).
Chemosensitization and radiosensitization of tumors by plant polyphenols.
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16127422 A.M.Tari, A.M.Simeone, Y.J.Li, Y.Gutierrez-Puente, S.Lai, and W.F.Symmans (2005).
Cyclooxygenase-2 protein reduces tamoxifen and N-(4-hydroxyphenyl)retinamide inhibitory effects in breast cancer cells.
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16278617 C.B.Lau, T.C.Ho, T.W.Chan, and S.C.Kim (2005).
Use of dong quai (Angelica sinensis) to treat peri- or postmenopausal symptoms in women with breast cancer: is it appropriate?
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15964799 C.C.Valley, R.Métivier, N.M.Solodin, A.M.Fowler, M.T.Mashek, L.Hill, and E.T.Alarid (2005).
Differential regulation of estrogen-inducible proteolysis and transcription by the estrogen receptor alpha N terminus.
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16129672 C.E.Bohl, D.D.Miller, J.Chen, C.E.Bell, and J.T.Dalton (2005).
Structural basis for accommodation of nonsteroidal ligands in the androgen receptor.
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PDB codes: 2ax6 2ax7 2ax8 2ax9 2axa
15688188 C.M.Rassi, M.Lieberherr, G.Chaumaz, A.Pointillart, and G.Cournot (2005).
Modulation of osteoclastogenesis in porcine bone marrow cultures by quercetin and rutin.
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15705806 C.M.Revankar, D.F.Cimino, L.A.Sklar, J.B.Arterburn, and E.R.Prossnitz (2005).
A transmembrane intracellular estrogen receptor mediates rapid cell signaling.
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15767587 C.Oostenbrink, and W.F.van Gunsteren (2005).
Free energies of ligand binding for structurally diverse compounds.
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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
15496458 F.Acconcia, P.Ascenzi, A.Bocedi, E.Spisni, V.Tomasi, A.Trentalance, P.Visca, and M.Marino (2005).
Palmitoylation-dependent estrogen receptor alpha membrane localization: regulation by 17beta-estradiol.
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15809979 F.Commodari, A.Khiat, S.Ibrahimi, A.R.Brizius, and N.Kalkstein (2005).
Comparison of the phytoestrogen trans-resveratrol (3,4',5-trihydroxystilbene) structures from x-ray diffraction and solution NMR.
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15870696 G.Reid, R.Métivier, C.Y.Lin, S.Denger, D.Ibberson, T.Ivacevic, H.Brand, V.Benes, E.T.Liu, and F.Gannon (2005).
Multiple mechanisms induce transcriptional silencing of a subset of genes, including oestrogen receptor alpha, in response to deacetylase inhibition by valproic acid and trichostatin A.
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15632292 G.Skretas, and D.W.Wood (2005).
Regulation of protein activity with small-molecule-controlled inteins.
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15699347 H.J.Garbán, D.C.Márquez-Garbán, R.J.Pietras, and L.J.Ignarro (2005).
Rapid nitric oxide-mediated S-nitrosylation of estrogen receptor: regulation of estrogen-dependent gene transcription.
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15738620 H.Kobayashi, and E.Hamaya (2005).
[Raloxifene hydrochloride (Evista Tablet 60 mg) for postmenopausal osteoporosis: mode of action and clinical efficacy]
  Nippon Yakurigaku Zasshi, 125, 37-48.  
16355216 H.Wu, Y.Chen, J.Liang, B.Shi, G.Wu, Y.Zhang, D.Wang, R.Li, X.Yi, H.Zhang, L.Sun, and Y.Shang (2005).
Hypomethylation-linked activation of PAX2 mediates tamoxifen-stimulated endometrial carcinogenesis.
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15505803 H.Zhong, and H.A.Carlson (2005).
Computational studies and peptidomimetic design for the human p53-MDM2 complex.
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In vitro and in vivo structure-activity relationships of novel androgen receptor ligands with multiple substituents in the B-ring.
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15908963 J.Fagart, J.Huyet, G.M.Pinon, M.Rochel, C.Mayer, and M.E.Rafestin-Oblin (2005).
Crystal structure of a mutant mineralocorticoid receptor responsible for hypertension.
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PDB codes: 1y9r 1ya3
15726586 J.M.Yang, and T.W.Shen (2005).
A pharmacophore-based evolutionary approach for screening selective estrogen receptor modulators.
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15770472 J.Wang, P.Xie, A.Kettrup, and K.W.Schramm (2005).
Evaluation of soot particles of biomass fuels with endocrine-modulating activity in yeast-based bioassay.
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15710879 J.Zhang, J.Simisky, F.T.Tsai, and D.S.Geller (2005).
A critical role of helix 3-helix 5 interaction in steroid hormone receptor function.
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15883974 J.von Langen, K.H.Fritzemeier, S.Diekmann, and A.Hillisch (2005).
Molecular basis of the interaction specificity between the human glucocorticoid receptor and its endogenous steroid ligand cortisol.
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15389851 K.F.Geoghegan, and M.A.Kelly (2005).
Biochemical applications of mass spectrometry in pharmaceutical drug discovery.
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15521089 K.Fukuzawa, K.Kitaura, M.Uebayasi, K.Nakata, T.Kaminuma, and T.Nakano (2005).
Ab initio quantum mechanical study of the binding energies of human estrogen receptor alpha with its ligands: an application of fragment molecular orbital method.
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15709961 K.W.Nettles, and G.L.Greene (2005).
Ligand control of coregulator recruitment to nuclear receptors.
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15696347 L.C.Hall, J.M.Rogers, M.S.Denison, and M.L.Johnson (2005).
Identification of the herbicide Surflan and its active ingredient oryzalin, a dinitrosulfonamide, as xenoestrogens.
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15980170 L.Martínez, M.T.Sonoda, P.Webb, J.D.Baxter, M.S.Skaf, and I.Polikarpov (2005).
Molecular dynamics simulations reveal multiple pathways of ligand dissociation from thyroid hormone receptors.
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16269315 L.Zhao, K.O'Neill, and R.Diaz Brinton (2005).
Selective estrogen receptor modulators (SERMs) for the brain: current status and remaining challenges for developing NeuroSERMs.
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15598662 M.C.Hodgson, I.Astapova, S.Cheng, L.J.Lee, M.C.Verhoeven, E.Choi, S.P.Balk, and A.N.Hollenberg (2005).
The androgen receptor recruits nuclear receptor CoRepressor (N-CoR) in the presence of mifepristone via its N and C termini revealing a novel molecular mechanism for androgen receptor antagonists.
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16282588 M.J.Lucey, D.Chen, J.Lopez-Garcia, S.M.Hart, F.Phoenix, R.Al-Jehani, J.P.Alao, R.White, K.B.Kindle, R.Losson, P.Chambon, M.G.Parker, P.Schär, D.M.Heery, L.Buluwela, and S.Ali (2005).
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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15662513 M.Miyashita, T.Shimada, H.Miyagawa, and M.Akamatsu (2005).
Surface plasmon resonance-based immunoassay for 17beta-estradiol and its application to the measurement of estrogen receptor-binding activity.
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16351736 P.D'Ursi, E.Salvi, P.Fossa, L.Milanesi, and E.Rovida (2005).
Modelling the interaction of steroid receptors with endocrine disrupting chemicals.
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15886208 Q.Li, L.Wu, D.K.Oelschlager, M.Wan, C.R.Stockard, W.E.Grizzle, N.Wang, H.Chen, Y.Sun, and X.Cao (2005).
Smad4 inhibits tumor growth by inducing apoptosis in estrogen receptor-alpha-positive breast cancer cells.
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15737489 R.H.Schreurs, E.Sonneveld, P.T.van der Saag, B.van der Burg, and W.Seinen (2005).
Examination of the in vitro (anti)estrogenic, (anti)androgenic and (anti)dioxin-like activities of tetralin, indane and isochroman derivatives using receptor-specific bioassays.
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16359432 R.J.Fletterick (2005).
Molecular modelling of the androgen receptor axis: rational basis for androgen receptor intervention in androgen-independent prostate cancer.
  BJU Int, 96, 2-9.  
15967794 R.K.Bledsoe, K.P.Madauss, J.A.Holt, C.J.Apolito, M.H.Lambert, K.H.Pearce, T.B.Stanley, E.L.Stewart, R.P.Trump, T.M.Willson, and S.P.Williams (2005).
A ligand-mediated hydrogen bond network required for the activation of the mineralocorticoid receptor.
  J Biol Chem, 280, 31283-31293.
PDB codes: 2aa2 2aa5 2aa6 2aa7 2aax 2ab2
15987442 S.R.Johnston (2005).
Endocrinology and hormone therapy in breast cancer: selective oestrogen receptor modulators and downregulators for breast cancer - have they lost their way?
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15965534 V.J.Nesatyy, B.V.Rutishauser, R.I.Eggen, and M.J.Suter (2005).
Identification of the estrogen receptor Cd-binding sites by chemical modification.
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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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16159155 W.Gao, C.E.Bohl, and J.T.Dalton (2005).
Chemistry and structural biology of androgen receptor.
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15914921 Y.C.Chen, Y.Sugiyama, N.Abe, R.Kuruto-Niwa, R.Nozawa, and A.Hirota (2005).
DPPH radical-scavenging compounds from dou-chi, a soybean fermented food.
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Molecular Basis of Steroid Action in the Prostate.
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Automated microscopy identifies estrogen receptor subdomains with large-scale chromatin structure unfolding activity.
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Interplay between estrogen response element sequence and ligands controls in vivo binding of estrogen receptor to regulated genes.
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A new series of estrogen receptor modulators: effect of alkyl substituents on receptor-binding affinity.
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14708019 A.W.Norman, M.T.Mizwicki, and D.P.Norman (2004).
Steroid-hormone rapid actions, membrane receptors and a conformational ensemble model.
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15466465 B.Sandler, P.Webb, J.W.Apriletti, B.R.Huber, M.Togashi, S.T.Cunha Lima, S.Juric, S.Nilsson, R.Wagner, R.J.Fletterick, and J.D.Baxter (2004).
Thyroxine-thyroid hormone receptor interactions.
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PDB codes: 1xzx 1y0x
15229223 B.del Río, J.M.García Pedrero, C.Martínez-Campa, P.Zuazua, P.S.Lazo, and S.Ramos (2004).
Melatonin, an endogenous-specific inhibitor of estrogen receptor alpha via calmodulin.
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Free energies of binding of polychlorinated biphenyls to the estrogen receptor from a single simulation.
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15483339 C.S.Lee, S.J.Kwon, S.Y.Na, S.P.Lim, and J.H.Lee (2004).
Genistein supplementation inhibits atherosclerosis with stabilization of the lesions in hypercholesterolemic rabbits.
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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
16281598 F.Conrad, and R.Paus (2004).
Estrogens and the hair follicle.
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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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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
15167276 H.Ogita, K.Node, H.Asanuma, S.Sanada, J.Kim, S.Takashima, T.Minamino, M.Hori, and M.Kitakaze (2004).
Raloxifene improves coronary perfusion, cardiac contractility, and myocardial metabolism in the ischemic heart: role of phosphatidylinositol 3-kinase/Akt pathway.
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15322366 H.Sato, S.Nishida, H.Tomoyori, M.Sato, I.Ikeda, and K.Imaizumi (2004).
Oxysterol regulation of estrogen receptor alpha-mediated gene expression in a transcriptional activation assay system using HeLa cells.
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14982928 K.Duda, Y.I.Chi, and S.E.Shoelson (2004).
Structural basis for HNF-4alpha activation by ligand and coactivator binding.
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PDB code: 1pzl
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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14770416 L.A.Abou-Zeid, and A.M.El-Mowafy (2004).
Differential recognition of resveratrol isomers by the human estrogen receptor-alpha: molecular dynamics evidence for stereoselective ligand binding.
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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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15610734 L.Shan, J.Vincent, J.S.Brunzelle, I.Dussault, M.Lin, I.Ianculescu, M.A.Sherman, B.M.Forman, and E.J.Fernandez (2004).
Structure of the murine constitutive androstane receptor complexed to androstenol: a molecular basis for inverse agonism.
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PDB code: 1xnx
15340912 M.I.Zavodszky, M.Lei, M.F.Thorpe, A.R.Day, and L.A.Kuhn (2004).
Modeling correlated main-chain motions in proteins for flexible molecular recognition.
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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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A new class of phytoestrogens; evaluation of the estrogenic activity of deoxybenzoins.
  Chem Biol, 11, 397-406.  
15060164 N.Heldring, M.Nilsson, B.Buehrer, E.Treuter, and J.A.Gustafsson (2004).
Identification of tamoxifen-induced coregulator interaction surfaces within the ligand-binding domain of estrogen receptors.
  Mol Cell Biol, 24, 3445-3459.  
  15531431 N.N.Bulayeva, and C.S.Watson (2004).
Xenoestrogen-induced ERK-1 and ERK-2 activation via multiple membrane-initiated signaling pathways.
  Environ Health Perspect, 112, 1481-1487.  
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.
  Crit Rev Oncol Hematol, 51, 55-67.  
  15630230 O.J.Park (2004).
Comparison of estrogen and genistein in their antigenotoxic effects, apoptosis and signal transduction protein expression patterns.
  Biofactors, 21, 379-382.  
15659824 O.J.Park, and J.I.Shin (2004).
Proapoptotic potentials of genistein under growth stimulation by estrogen.
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15468062 R.Kasher, B.Gayer, T.Kulik, D.Somjen, N.Venkatesh, M.Fridkin, E.Katchalski-Katzir, and F.Kohen (2004).
Design, synthesis, and evaluation of peptides with estrogen-like activity.
  Biopolymers, 76, 404-420.  
15023859 R.Liew, M.A.Stagg, K.T.MacLeod, and P.Collins (2004).
Raloxifene acutely suppresses ventricular myocyte contractility through inhibition of the L-type calcium current.
  Br J Pharmacol, 142, 89-96.  
15343269 R.Métivier, G.Penot, R.P.Carmouche, M.R.Hübner, G.Reid, S.Denger, D.Manu, H.Brand, M.Kos, V.Benes, and F.Gannon (2004).
Transcriptional complexes engaged by apo-estrogen receptor-alpha isoforms have divergent outcomes.
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14966133 R.Shi, and S.X.Lin (2004).
Cofactor hydrogen bonding onto the protein main chain is conserved in the short chain dehydrogenase/reductase family and contributes to nicotinamide orientation.
  J Biol Chem, 279, 16778-16785.
PDB codes: 1qyv 1qyw 1qyx
15108352 S.Bord, E.Frith, D.C.Ireland, M.A.Scott, J.I.Craig, and J.E.Compston (2004).
Estrogen stimulates differentiation of megakaryocytes and modulates their expression of estrogen receptors alpha and beta.
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15238146 S.Bord, E.Frith, D.C.Ireland, M.A.Scott, J.I.Craig, and J.E.Compston (2004).
Synthesis of osteoprotegerin and RANKL by megakaryocytes is modulated by oestrogen.
  Br J Haematol, 126, 244-251.  
15461668 S.Ito, K.Takeyama, A.Yamamoto, S.Sawatsubashi, Y.Shirode, A.Kouzmenko, T.Tabata, and S.Kato (2004).
In vivo potentiation of human oestrogen receptor alpha by Cdk7-mediated phosphorylation.
  Genes Cells, 9, 983-992.  
15572757 S.Martino, J.A.Cauley, E.Barrett-Connor, T.J.Powles, J.Mershon, D.Disch, R.J.Secrest, and S.R.Cummings (2004).
Continuing outcomes relevant to Evista: breast cancer incidence in postmenopausal osteoporotic women in a randomized trial of raloxifene.
  J Natl Cancer Inst, 96, 1751-1761.  
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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15094156 S.T.Pearce, and V.C.Jordan (2004).
The biological role of estrogen receptors alpha and beta in cancer.
  Crit Rev Oncol Hematol, 50, 3.  
15300835 S.Top, A.Vessières, P.Pigeon, M.N.Rager, M.Huché, E.Salomon, C.Cabestaing, J.Vaissermann, and G.Jaouen (2004).
Selective estrogen-receptor modulators (SERMs) in the cyclopentadienylrhenium tricarbonyl series: synthesis and biological behaviour.
  Chembiochem, 5, 1104-1113.  
15050912 V.C.Jordan (2004).
Selective estrogen receptor modulation: concept and consequences in cancer.
  Cancer Cell, 5, 207-213.  
  15121513 W.Körner, A.M.Vinggaard, B.Térouanne, R.Ma, C.Wieloch, M.Schlumpf, C.Sultan, and A.M.Soto (2004).
Interlaboratory comparison of four in vitro assays for assessing androgenic and antiandrogenic activity of environmental chemicals.
  Environ Health Perspect, 112, 695-702.  
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.  
15314175 X.Li, J.Huang, P.Yi, R.A.Bambara, R.Hilf, and M.Muyan (2004).
Single-chain estrogen receptors (ERs) reveal that the ERalpha/beta heterodimer emulates functions of the ERalpha dimer in genomic estrogen signaling pathways.
  Mol Cell Biol, 24, 7681-7694.  
15048828 X.Li, M.P.Jacobson, and R.A.Friesner (2004).
High-resolution prediction of protein helix positions and orientations.
  Proteins, 55, 368-382.  
15159406 Z.Chen, B.S.Katzenellenbogen, J.A.Katzenellenbogen, and H.Zhao (2004).
Directed evolution of human estrogen receptor variants with significantly enhanced androgen specificity and affinity.
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12529333 A.Chauchereau, L.Amazit, M.Quesne, A.Guiochon-Mantel, and E.Milgrom (2003).
Sumoylation of the progesterone receptor and of the steroid receptor coactivator SRC-1.
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13680814 A.L.Ososki, and E.J.Kennelly (2003).
Phytoestrogens: a review of the present state of research.
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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
14517908 A.Nayeem, S.Krystek, and T.Stouch (2003).
An assessment of protein-ligand binding site polarizability.
  Biopolymers, 70, 201-211.  
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.  
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.  
12686538 B.Kauppi, C.Jakob, M.Färnegårdh, J.Yang, H.Ahola, M.Alarcon, K.Calles, O.Engström, J.Harlan, S.Muchmore, A.K.Ramqvist, S.Thorell, L.Ohman, J.Greer, J.A.Gustafsson, J.Carlstedt-Duke, and M.Carlquist (2003).
The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism.
  J Biol Chem, 278, 22748-22754.
PDB codes: 1nhz 1p93
12559765 B.M.Necela, and J.A.Cidlowski (2003).
Crystallization of the human glucocorticoid receptor ligand binding domain: a step towards selective glucocorticoids.
  Trends Pharmacol Sci, 24, 58-61.  
12714604 C.L.Hsu, Y.L.Chen, S.Yeh, H.J.Ting, Y.C.Hu, H.Lin, X.Wang, and C.Chang (2003).
The use of phage display technique for the isolation of androgen receptor interacting peptides with (F/W)XXL(F/W) and FXXLY new signature motifs.
  J Biol Chem, 278, 23691-23698.  
12488554 D.Yin, Y.He, M.A.Perera, S.S.Hong, C.Marhefka, N.Stourman, L.Kirkovsky, D.D.Miller, and J.T.Dalton (2003).
Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor.
  Mol Pharmacol, 63, 211-223.  
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.  
12667452 G.Reid, M.R.Hübner, R.Métivier, H.Brand, S.Denger, D.Manu, J.Beaudouin, J.Ellenberg, and F.Gannon (2003).
Cyclic, proteasome-mediated turnover of unliganded and liganded ERalpha on responsive promoters is an integral feature of estrogen signaling.
  Mol Cell, 11, 695-707.  
  12676613 H.Tamura, H.Yoshikawa, K.W.Gaido, S.M.Ross, R.K.DeLisle, W.J.Welsh, and A.M.Richard (2003).
Interaction of organophosphate pesticides and related compounds with the androgen receptor.
  Environ Health Perspect, 111, 545-552.  
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.
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12602925 K.Christov, A.Ikui, A.Shilkaitis, A.Green, R.Yao, M.You, C.Grubbs, V.Steele, R.Lubet, and I.B.Weinstein (2003).
Cell proliferation, apoptosis, and expression of cyclin D1 and cyclin E as potential biomarkers in tamoxifen-treated mammary tumors.
  Breast Cancer Res Treat, 77, 253-264.  
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.  
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
12894986 M.J.McPhaul (2003).
Factors that mediate and modulate androgen action.
  J Investig Dermatol Symp Proc, 8, 1-5.  
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.  
12733718 M.T.Mizwicki, and A.W.Norman (2003).
Two key proteins of the vitamin D endocrine system come into crystal clear focus: comparison of the X-ray structures of the nuclear receptor for 1alpha,25(OH)2 vitamin D3, the plasma vitamin D binding protein, and their ligands.
  J Bone Miner Res, 18, 795-806.  
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.  
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.  
12794857 N.Lozovaya, and A.D.Miller (2003).
Chemical neuroimmunology: health in a nutshell bidirectional communication between immune and stress (limbic-hypothalamic-pituitary-adrenal) systems.
  Chembiochem, 4, 466-484.  
12518336 P.D.Darbre, J.R.Byford, L.E.Shaw, S.Hall, N.G.Coldham, G.S.Pope, and M.J.Sauer (2003).
Oestrogenic activity of benzylparaben.
  J Appl Toxicol, 23, 43-51.  
12544654 P.Nestel (2003).
Isoflavones: their effects on cardiovascular risk and functions.
  Curr Opin Lipidol, 14, 3-8.  
  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.  
14675539 R.Métivier, G.Penot, M.R.Hübner, G.Reid, H.Brand, M.Kos, and F.Gannon (2003).
Estrogen receptor-alpha directs ordered, cyclical, and combinatorial recruitment of cofactors on a natural target promoter.
  Cell, 115, 751-763.  
12854100 R.S.Prichard, A.D.Hill, B.Dijkstra, E.W.McDermott, and N.J.O'Higgins (2003).
The prevention of breast cancer.
  Br J Surg, 90, 772-783.  
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.  
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.  
14668813 S.R.Johnston, and M.Dowsett (2003).
Aromatase inhibitors for breast cancer: lessons from the laboratory.
  Nat Rev Cancer, 3, 821-831.  
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.  
12970175 S.Svensson, T.Ostberg, M.Jacobsson, C.Norström, K.Stefansson, D.Hallén, I.C.Johansson, K.Zachrisson, D.Ogg, and L.Jendeberg (2003).
Crystal structure of the heterodimeric complex of LXRalpha and RXRbeta ligand-binding domains in a fully agonistic conformation.
  EMBO J, 22, 4625-4633.
PDB code: 1uhl
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.  
12736258 S.Williams, R.K.Bledsoe, J.L.Collins, S.Boggs, M.H.Lambert, A.B.Miller, J.Moore, D.D.McKee, L.Moore, J.Nichols, D.Parks, M.Watson, B.Wisely, and T.M.Willson (2003).
X-ray crystal structure of the liver X receptor beta ligand binding domain: regulation by a histidine-tryptophan switch.
  J Biol Chem, 278, 27138-27143.
PDB code: 1p8d
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.  
12668685 T.Janvilisri, H.Venter, S.Shahi, G.Reuter, L.Balakrishnan, and H.W.van Veen (2003).
Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis.
  J Biol Chem, 278, 20645-20651.  
12951324 T.L.McCarthy, W.Z.Chang, Y.Liu, and M.Centrella (2003).
Runx2 integrates estrogen activity in osteoblasts.
  J Biol Chem, 278, 43121-43129.  
12616628 T.Mordasini, A.Curioni, R.Bursi, and W.Andreoni (2003).
The binding mode of progesterone to its receptor deduced from molecular dynamics simulations.
  Chembiochem, 4, 155-161.  
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.  
12878603 V.Y.Lin, E.M.Resnick, and M.A.Shupnik (2003).
Truncated estrogen receptor product-1 stimulates estrogen receptor alpha transcriptional activity by titration of repressor proteins.
  J Biol Chem, 278, 38125-38131.  
12842037 Y.Li, M.H.Lambert, and H.E.Xu (2003).
Activation of nuclear receptors: a perspective from structural genomics.
  Structure, 11, 741-746.  
12774125 Z.Wang, G.Benoit, J.Liu, S.Prasad, P.Aarnisalo, X.Liu, H.Xu, N.P.Walker, and T.Perlmann (2003).
Structure and function of Nurr1 identifies a class of ligand-independent nuclear receptors.
  Nature, 423, 555-560.
PDB code: 1ovl
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
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
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.  
12085458 D.J.Theodorou, S.J.Theodorou, and D.J.Sartoris (2002).
Treatment of osteoporosis: current status and recent advances.
  Compr Ther, 28, 109-122.  
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.  
12220494 G.B.Wisely, A.B.Miller, R.G.Davis, A.D.Thornquest, R.Johnson, T.Spitzer, A.Sefler, B.Shearer, J.T.Moore, A.B.Miller, T.M.Willson, and S.P.Williams (2002).
Hepatocyte nuclear factor 4 is a transcription factor that constitutively binds fatty acids.
  Structure, 10, 1225-1234.
PDB code: 1lv2
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.  
11997506 H.Kitagawa, J.Yanagisawa, H.Fuse, S.Ogawa, Y.Yogiashi, A.Okuno, H.Nagasawa, T.Nakajima, T.Matsumoto, and S.Kato (2002).
Ligand-selective potentiation of rat mineralocorticoid receptor activation function 1 by a CBP-containing histone acetyltransferase complex.
  Mol Cell Biol, 22, 3698-3706.  
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.  
12198482 J.C.Young, and F.U.Hartl (2002).
Chaperones and transcriptional regulation by nuclear receptors.
  Nat Struct Biol, 9, 640-642.  
11815387 J.D.Croxtall, P.T.van Hal, Q.Choudhury, D.W.Gilroy, and R.J.Flower (2002).
Different glucocorticoids vary in their genomic and non-genomic mechanism of action in A549 cells.
  Br J Pharmacol, 135, 511-519.  
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
14993393 K.J.Ho, and J.K.Liao (2002).
Non-nuclear actions of estrogen: new targets for prevention and treatment of cardiovascular disease.
  Mol Interv, 2, 219-228.  
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.  
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.  
12009019 L.L.Issa, G.M.Leong, R.L.Sutherland, and J.A.Eisman (2002).
Vitamin D analogue-specific recruitment of vitamin D receptor coactivators.
  J Bone Miner Res, 17, 879-890.  
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.  
11883412 M.D.Jürgens, K.I.Holthaus, A.C.Johnson, J.L.Smith, M.Hetheridge, and R.J.Williams (2002).
The potential for estradiol and ethinylestradiol degradation in English rivers.
  Environ Toxicol Chem, 21, 480-488.  
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