Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 390 for “"Estrogen Receptor"”.
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Molecular mechanism of interactions between estrogen receptor and estrogen receptor selective genotoxins
… cells. Breast cancer cells often overexpress the estrogen receptor protein. By synthesizing a drug that not only binds and damages the DNA but also binds the abundant proteins in the cells, thereby blocking the damaged site from DNA repair proteins, a selective treatment of cancer cells can be …
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Estrogen Receptor Subtype Selective Ligands
Estrogen action is mediated through estrogen receptor alpha (ERalpha) and beta (ERbeta). We report on the identification of several groups of non-steroidal ligands that show pronounced subtype-selective differences in ligand binding and transactivation potency or efficacy, the study of the …
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Estrogen receptor beta modulates prostate carcinogenesis
… is characterised by dependence upon androgen receptor (AR) as its driving oncogene. When organ-confined, radical treatment can be curative, however there is no cure for advanced, castration-resistant prostate cancer (CRPC). There is therefore a need to better understand the biology of PC, and …
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Cross-Modulatory Actions of Estrogen Receptor Beta on Estrogen Receptor Alpha Transcriptional Activity in Breast Cancer Cells
Our observations indicate that the ability of ERalpha and ERbeta to serve as determinants of gene expression is greatly influenced by the nature of the ligand, ligand dose, and the ability of ligand-ER complexes to recruit coregulators at ER binding sites of hormone-regulated genes.
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Reengineering Estrogen Receptor Hormone Specificity Through Coordinated Changes at Key Contact Sites Between Estrogen Receptor and Estradiol
… that a hormonal ligand has with its cognate receptor. This interaction is defined by steric and electronic complementarity at certain sites at which portions of the ligand contact specific residues in its receptor. In the nuclear hormone receptors, mutational mapping studies, and more …
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Estrogen Receptor -Dependent and Estrogen Receptor-Independent Pathways for Tamoxifen and 4-Hydroxytamoxifen-Induced Programmed Cell Death
… common methods of breast cancer treatment is antiestrogen treatment. The therapeutic efficacy of the selective estrogen receptor modulator tamoxifen (TAM) in cancer therapy is thought to arise from its ability to compete with estrogens for binding to the ER. We show that TAM and its active …
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Estrogen Receptor Regulation of Vitellogenin Gene Expression
… vitellogenin in the liver. Injection of estrogen into male animals previously exposed to estrogen but subsequently withdrawn from the hormone leads to the much earlier appearance of vitellogenin mRNA and a four-fold higher rate of vitellogenin gene transcription in the restimulated …
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Development of Novel Subtype Selective Ligands for the Estrogen Receptor: I. 5,6-Diakyl-5,6,11,12-Tetrahydrochrysenes as Estrogen Receptor-Beta Selective Antagonists. II. Diarylpropionitriles as Estrogen Receptor-Beta Potency Selective Agonists
A series of ERbeta selective DPN analogs were prepared where the both the ligand core and the aromatic rings were modified by the repositioning of phenolic hydroxy groups and by the addition of alkyl substituents and nitrile groups. Another series of DPN analogs were synthesized where the nitrile …
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Evaluating Estrogen Receptor Signaling in Pancreatic β-Cells
Estrogen receptor signaling is involved in the etiology of multiple diseases including the development and progression of Type 2 Diabetes Mellitus, T2DM. The role of estrogen receptor signaling in peripheral insulin resistance has been shown through studies in post-menopausal women; however, …
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Circadian modulation of the estrogen receptor alpha transcription
… circadian disruption and the development of estrogen dependent tumors. The expression of estrogen receptor alpha (ERα) mRNA oscillates in a 24-hour period and, unlike Per2, ERα peaks during the light phase of the day. Because up regulation of ERα relates to tumor development, defining the …
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Estradiol and chlordecone interactions with the estrogen receptor
… pesticide, chlordecone, on the estradiol receptor of adult ovariectomized CDF-344 rats were examined. Chlordecone's competition for $\sp3$H-estradiol binding in vitro was similar whether receptors were derived from neural or uterine tissue. In vivo, chlordecone led to nuclear retention of …
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Isolation and Characterization of Estrogen Receptor- Interacting Proteins
<p>Estrogen fulfills a variety of physiological roles through its nuclear receptors, estrogen receptors (ERs). The action of ERs is modulated and mediated by diverse interacting cofactors. The initial aim of this thesis work was to identify ligand-, subtype- and/or cell typespecific ER-interacting …
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Characterization of estrogen receptor alpha in mouse osteoblasts
… in coordinating the reproductive function estrogens also affect the physiology of non-reproductive tissues such as bone. As a result they impact on the function of the two cell types operating bone homeostasis, osteoblasts and osteoclasts. Estrogens effects are entirely mediated by two …
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Estrogen Receptor Ligands and Regulation of Gene Expression
Keratin13 (KRT13) and calcitonin receptor (CALCR) gene expression is differentially regulated by estradiol (E2) and the selective estrogen receptor modulators (SERMs) tamoxifen and raloxifene. KRT13 is a cytoskeleton protein while CALCR mediates the biological effects of calcitonin. These two genes …
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Dominant negative mutants of the human estrogen receptor
We have characterized three human estrogen receptor (ER) mutants which, at low concentrations, are capable of blocking the intracellular activity of wild type ER. The mutants, a truncated ER (ER1-530), a point mutant (L540Q), and a frameshift (S554fs), were generated by random chemical mutagenesis …
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I. Design and synthesis of estrogen receptor gene switches. II. Design and synthesis of estrogen receptor ligands occupying an auxiliary binding pocket
The estrogen receptor (ER) is ligand-regulated nuclear hormone receptor and an important therapeutic target for breast cancer, hormone replacement therapy, contraception, and osteoporosis. Novel organic cores have been identified and developed as possible estrogen pharmaceuticals. The x-ray …
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Regulation of estrogen receptor-alpha mediated gene expression and endocrine resistance through estrogen receptor-alpha phosphorylation and micro-RNA in breast cancer
Estrogens are associated with the development and progression of breast cancer in addition to their role in normal reproductive physiology, and estrogen receptors (ER) mediate the actions of estrogen in target tissues by regulating the expression of numerous biologically important target genes. The …
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Genomic and Non-Genomic Actions of Estrogen Receptor Ligands
The physiological activities of estrogen are mediated by its binding to estrogen receptor proteins in target cells. In the nucleus, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta) serve as ligand activated transcription factors and upon estrogen binding, they can stimulate or …
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Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors
Key hydrophobic and hydrogen bonding moieties were incorporated onto a variety of core scaffolds including amphipathic benzene, bicyclo[2.2.2]octane, and urea, resulting in three different series of compounds that could be utilized as coactivator binding inhibitors (CBIs). A fluorescence-based …
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