Structure of Estrogen Receptors

Baker, M. Insights from the Structure of Estrogen Receptor into the Evolution of Estrogens Implications for Endocrine Disruption. cal Pharmacology 82 (2011) 1-8. 

Gao H, Williams C, Labute P, Bajorath J. Binary quantitative structure-activity relationship (QSAR) analysis of estrogen receptor ligands. / Chem Inf Comput Sci 1999 39 164-8. 

This book represents the effort of a group of scientists and clinicians to offer the reader an updated view of the main advances occurred in the field in the recent years. Every author has been selected because of his/her experience with modulators of estrogen receptors, either in basic or clinical grounds. This explains the structure of the book, which reviews the main basic concepts in the first part, to immediately concentrate in the recent news on the many uses of SERMs in clinical practice. We are very grateful with all of them for his excellent contribution. To conclude, we also would like to express our gratitude to Springer-Verlag for the excellent technical support as well as to those who, from different perspectives, are at the base of our work, our patients and our families. 

Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL (1998) The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell 95 927... 

Hall JM, McDonnell DP, Korach KS Allosteric regulation of estrogen receptor structure, function, and co-activator recruitment by different estrogen response elements. Mol Endocrinol 2002 16 469. [PMID 11875105]... 

We also studied the structure-activity relationships with computation modeling of these estrogenic phenols (Table 8) and non-estrogenic phenols [45]. For the examination of molecular modeling of the iso-prenoid-substituted phenols, we made a space model of estrogen receptor (SMER) with an imaginary compound (103), Fig. (26), that built up with... 

Mekenyan, O., Walker, J.D. and Bradbury, S. (2003) Quantitative structure-activity relationship models for prediction of estrogen receptor binding affinity of structurally diverse chemicals. Environ. Toxicol. Chem., 22 (8), 1844-1854. 

Shi, L.M., Xie, Q., Wu, J., Perkins, R., Walker, J.D., Branham, W. and Sheehan, D.M. (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 (1), 29-36. 

Parker MG. 1995. Structure and function of estrogen receptors. Vi tarn Horn 51 267-287. 

Traish, A. M., Al-Fadhi, S., Klinge, C., Kounine, M., and Quick, T. C. 1995. Identification of structurally altered estrogen receptors in human breast cancer by site-directed monoclonal antibodies. Steroids 60 467-474. 

Sippl, W. Receptor-based 3D Quantitative Structure-Activity Relationships of Estrogen Receptor Ligands./. Comput.-Aided. Mol. Des., 2000, 14, 559-572. 

Tamoxifen [ta MOX i fen] is an estrogen antagonist, structurally related to the synthetic estrogen, diethylstilbestrol, and is active in the treatment of estrogen receptor-positive breast cancer. Tamoxifen has weak estrogenic activity. 

Estradiol is a pure agonist of estrogen receptor-a and the structure of this complex (PDB entry IQKU) [8] shows how an agonist ligand precisely and productively folds ER-a and stabilizes the unique agonist position of helix-12 (Figs. 1.4 and... 

Shiau, A.K., Barstad, D., Radek, J.T., Meyers, M.J., Nettles, K.W., Katzenel-lenbogen, B.S., Katzenellenbogbn, J.A., Agard, D.A., Greene, G.L Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism. Nat. Struct. 

Wurtz, J. M., Egner, U., Heinrich. N., Moras, D., Mueller-Fahrnow, A. Three-Dimensional Models of Estrogen Receptor Ligand Binding Domain Complexes, Based on Related Crystal Structures and Mutational and Structure-Activity Relationships Data,/. Med. Chem. 1998, 41, 1803-1814. 

Shiau, A. K., Barstad, D., Loria, P. M., Cheng, L., Kushner, P. J., Agard, D. A., Greene, G.L. The Structural Basis of Estrogen Receptor/Coactivator Recognition and the Antagonism of this Interaction by Tamoxifen, Cell 1998, 95, 927-937. 

Shiau AK, et al. The structural basis of estrogen receptor/ coactivator recognition and the antagonism of this interaction... 

Gao, H., Williams, C, Labute, P. and Bajorath, J. (1999). Binary Quantitative Structure-Activity Relationship (QSAR) Analysis of Estrogen Receptor Ligands. J.Chem.lnf.Comput.Sci., 39, 164-168. 

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