Journal ArticleDOI
The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site
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TLDR
The various elements in this model for the binding of steroidal estrogens by the estrogen receptor are consistent with evidence emerging from the crystal structures of related nuclear hormone receptor ligand complexes.About:
This article is published in Steroids.The article was published on 1997-03-01. It has received 619 citations till now. The article focuses on the topics: Estrogen receptor binding & Ligand (biochemistry).read more
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Journal ArticleDOI
Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta.
George G. J. M. Kuiper,J.G. Lemmen,Bo Carlsson,J. Christopher Corton,Stephen Safe,Paul T. van der Saag,Bart van der Burg,Jan-Åke Gustafsson +7 more
TL;DR: The estrogenic activity of environmental chemicals and phytoestrogens in competition binding assays with ERα or ERβ protein, and in a transient gene expression assay using cells in which an acute estrogenic response is created by cotransfecting cultures with recombinant human ERβ complementary DNA (cDNA) in the presence of an estrogen-dependent reporter plasmid are investigated.
Journal ArticleDOI
Molecular basis of agonism and antagonism in the oestrogen receptor.
Andrzej M. Brzozowski,Ashley C. W. Pike,Zbigniew Dauter,Roderick E. Hubbard,Tomas Bonn,Owe Engström,Lars Öhman,Geoffrey L. Greene,Jan-Åke Gustafsson,Mats Carlquist +9 more
TL;DR: The crystal structures of the LBD of ER in complex with the endogenous oestrogen, 17β-oestradiol, and the selective antagonist raloxifene provide a molecular basis for the distinctive pharmacophore of the ER and its catholic binding properties.
Journal ArticleDOI
Estrogen carcinogenesis in breast cancer.
James D. Yager,Nancy E. Davidson +1 more
TL;DR: Insight into the mechanisms of the causation of cancer by estrogen will identify determinants of susceptibility to breast cancer and new targets for prevention and therapeutic intervention.
Journal ArticleDOI
Structure of the Ligand-Binding Domain of Oestrogen Receptor Beta in the Presence of a Partial Agonist and a Full Antagonist
Ashley C. W. Pike,Andrzej M. Brzozowski,Roderick E. Hubbard,Tomas Bonn,Ann Gerd Thorsell,Owe Engström,Jan Ljunggren,Jan-Åke Gustafsson,Mats Carlquist +8 more
TL;DR: The three‐dimensional structure of the oestrogen receptor beta isoform (ERβ) ligand‐binding domain (LBD) in the presence of the phyto‐oestrogen genistein and the antagonist raloxifene is reported.
Journal ArticleDOI
The Estrogen Receptor Relative Binding Affinities of 188 Natural and Xenochemicals: Structural Diversity of Ligands
R. Blair,Hong Fang,William S. Branham,Bruce S. Hass,Stacey L. Dial,Carrie L. Moland,Weida Tong,Leming Shi,Roger Perkins,Daniel M. Sheehan +9 more
TL;DR: The current study provides the most structurally diverse ER RBA data set with the widest range of RBA values published to date.
References
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Book
CRC Handbook of Chemistry and Physics
TL;DR: CRC handbook of chemistry and physics, CRC Handbook of Chemistry and Physics, CRC handbook as discussed by the authors, CRC Handbook for Chemistry and Physiology, CRC Handbook for Physics,
Journal ArticleDOI
Development and use of quantum mechanical molecular models. 76. AM1: a new general purpose quantum mechanical molecular model
TL;DR: In this paper, a new parametric quantum mechanical molecular model, AM1 (Austin Model l), based on the NDDO approximation, is described, in which the major weaknesses of MNDO, in particular failure to reproduce hydrogen bonds, have been overcome without any increase in computing time.
Journal ArticleDOI
The steroid and thyroid hormone receptor superfamily
TL;DR: A superfamily of regulatory proteins that include receptors for thyroid hormone and the vertebrate morphogen retinoic acid is identified, suggesting mechanisms underlying morphogenesis and homeostasis may be more ubiquitous than previously expected.
Journal ArticleDOI
Cloning of a novel receptor expressed in rat prostate and ovary.
TL;DR: It is concluded that clone 29 cDNA encodes a novel rat ER, which is suggested be named rat ERbeta to distinguish it from the previously cloned ER (ERalpha) from rat uterus.
Book
Inorganic Chemistry: Principles of Structure and Reactivity
TL;DR: In this article, inorganic chemistry principles of structure and reactivity are presented. But, they do not cover how to use these principles in the design of products, and they are not available in any type of product.