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Estrogen Receptor Modulators (2):
Recent article
Estrogen Receptor Modulators
Neuroscience Letters (481)3 2010
Abstract
We determined that inhibition of Notch-2 by liquiritigenin was probably ERbeta-dependent. These findings highlight the possible role of liquiritigenin in the repair and regeneration of injured brain tissue of patients with neurodegenerative diseases and support further investigation of the Notch-2 s...
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PMID: 20600596
PDF is available here.
PDF is available here.
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Abstract
In total, 31 (81.6%) women who received estradiol gel and 38 (100.0%) women who received tibolone completed treatment. Intent-to-treat analysis showed that, after 6 months of treatment, the total MRS score was significantly reduced in the tibolone group compared with the transdermal estradiol gel gr...
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PMID: 20570264
PDF is available here.
PDF is available here.
Abstract
Estrogen receptor ERalpha and ERbeta heterodimerization has been implicated in cancer chemoprevention. The discovery, structural elucidation, and total synthesis of a new natural product, actinopolymorphol A (1), from Actinopolymorpha rutilus (YIM45725) that preferentially induces ERalpha/beta heter...
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PMID: 20593804
PDF is available here.
PDF is available here.
Abstract
Approximately 70% of breast cancers express the estrogen receptor (ER) and endocrine therapy is the most important component of systemic therapy for hormone-responsive breast cancer. Unfortunately, endocrine-resistant ER-positive disease represents up to one-quarter of all breast can...
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PMID: 20384578
PDF is available here.
PDF is available here.
Abstract
Abstract
A mixture of the (Z)- and (E)-isomers of 4-hydroxy-N-desmethyltamoxifen was conveniently prepared in four steps. These geometrical isomers were then neatly separated by semi-preparative Reverse Phase High Performance Liquid Chromatography (RP-HPLC) using specified conditions. Additionally, the isola...
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PMID: 20400308
PDF is available here.
PDF is available here.
Abstract
We investigated antiestrogen activity of SK in breast cancer cells. In human breast cancer cells, we observed that treatment with SK inhibits tumor cell growth in estrogen receptor alpha (ERalpha)-positive, but not ERalpha-negative breast cancer cells. Estrogen-dependent cell growth was inhibited by...
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PMID: 19760501
PDF is available here.
PDF is available here.
Climacteric (13)2 2010
Abstract
After treatment, all subscores in the GCS improved in the tibolone and CEE/MPA groups (p < 0.01), except the sexual subscore in the CEE/MPA group, compared with baseline. There were significant differences in the FSFI in the tibolone and CEE/MPA groups in comparison to the control group after treatm...
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PMID: 19731119
PDF is available here.
PDF is available here.
Expert Opinion on Investigational Drugs (19 Suppl 1)s1 2010
Abstract
We need the results from ongoing studies to decide what may be the optimal duration of therapy and regimen (sequential treatment versus monotherapy; one drug compared with another). Further, there is a need to critically assess optimal use of endocrine therapy for metastatic disease among patients p...
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PMID: 20374026
PDF is available here.
PDF is available here.
Abstract
We previously reported that fulvestrant-induced ERalpha degradation depends on the interaction of ERalpha with cytokeratins 8 and 18 (CK8/CK18). Here we further investigate the role of these two cytokeratins in the antagonistic activity of the SERD. Using ER-responsive reporter assays, we demonstrat...
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PMID: 20061804
PDF is available here.
PDF is available here.
Abstract
tibolone causes a significant reduction of HDL-c and total cholesterol and has a deleterious effect on the body weight of oophorectomized rats, which may be related to the lower food ingestion by these animals....
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PMID: 20305947
PDF is available here.
PDF is available here.
Abstract
We and others showed that autophagy is critical to estrogen receptor positive (ER+) breast cancer cell survival and the development of antiestrogen resistance. Consequently, new approaches are warranted for targeting autophagy in breast cancer cells undergoing antiestrogen therapy. Because crosstalk...
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PMID: 20110775
PDF is available here.
PDF is available here.
BMC Medical Genomics (3)1 2010
Abstract
We constructed a hierarchical empirical Bayes model to investigate the simultaneous change of gene expression and promoter DNA methylation profiles among wild type (WT) and OHT/ICI resistant MCF7 breast cancer cell lines.
We found that compared with the WT cell lines, almost all of t...
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PMID: 21108837
PDF is available here.
PDF is available here.
Minerva ginecologica (61)6 2009
Abstract
We will discuss them mainly as used in the treatment and prevention of breast cancer. Tamoxifen is the widely investigated and most used representative of these drugs and has been introduced in the advanced disease, in the neoadjuvant and adjuvant setting and for prevention of the disease. Its role...
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PMID: 19942839
PDF is available here.
PDF is available here.
Abstract
Our results showed that xanthorrhizol significantly increased Gal-4/ER luciferase activity in a dose-dependent manner and induced the endogenous ER-estrogen response element (ERE) interaction in MCF-7 cells. Xanthorrhizol also significantly enhanced the expression of the pS2 gene in MCF-7 cells. In...
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PMID: 19881304
PDF is available here.
PDF is available here.
Abstract
The primary objective in metastatic breast cancer is tumor control and symptom palliation. Factors to be considered are: efficacy, tolerance and quality of life as well as patient preferences. In the Hormone Receptor Positive Group, Hormonal treatment is the best choice because of it's effectiveness...
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PMID: 19902677
PDF is available here.
PDF is available here.
Abstract
Chlorination is widely used in wastewater reclamation, however harmful disinfection byproducts (DBPs) may be formed during disinfection. These DBPs are considered as a potential and important source of endocrine-disruption. In this study, the effects of chlorination on estrogenic and antiestrogenic...
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PMID: 19673289
PDF is available here.
PDF is available here.
Oncology Reports (22)1 2009
Abstract
Pregnancy lowers the risk of breast cancer, largely attributable to alpha-fetoprotein (AFP). A small AFP-derived peptide (AFPep) which mimics the active site of AFP has been developed and may be useful for decreasing the risk of breast cancer for women. AFPep has been shown previously to stop the gr...
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PMID: 19513504
PDF is available here.
PDF is available here.
Evaluating the role of serotonin in hot flashes after breast cancer using acute tryptophan depletion
Abstract
Physiologically documented and self-reported hot flashes were not exacerbated by tryptophan depletion. Additional mechanistic research is needed to better understand the etiology of hot flashes....
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PMID: 19265726
PDF is available here.
PDF is available here.
Abstract
Although many estrogen receptor-positive (ER+) breast cancers are effectively treated with selective estrogen receptor modulators and down-regulators (SERM/SERD), some are highly resistant. Resistance is more likely if primary cancers are devoid of progesterone receptors (PR-) or have high levels of...
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PMID: 19401525
PDF is available here.
PDF is available here.
Abstract
We were interested in studying the effects of androgens on breast cancer cell proliferation under profound estrogen-deprived conditions. Using in vitro models of estrogen-dependent breast cancer cell growth we show that the androgens testosterone and 5alpha-dihydrotestosterone induce the growth of M...
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PMID: 18521740
PDF is available here.
PDF is available here.
Cancer Letters (275)2 2009
Abstract
We investigated how c-Src activity affects cell adhesion using a tamoxifen-resistant variant of MCF-7 cells (MTR-3) containing elevated c-Src activity. In MTR-3 cells, adhesion proteins beta-catenin and E-cadherin are mislocalized, forming novel structures perpendicular to cell-cell junctions. c-Src...
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PMID: 19026486
PDF is available here.
PDF is available here.
Cancer Letters (275)2 2009
Abstract
We tested if order of administration of the DNMT (5-aza 2' deoxycytidine/AZA) or HDAC (trichostatin A/TSA) inhibitors and tamoxifen affected ER re-expression and tamoxifen sensitivity. Treatment with AZA followed by co-administration of TSA plus tamoxifen resulted in the greatest ER re-expression an...
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PMID: 19013015
PDF is available here.
PDF is available here.
Abstract
high doses of tibolone, given for long periods of time to castrated female rats, have an estrogenic effect which can be dose-dependent, causing proliferation in the endometrium and causing changes in the cell differentiation (squamous metaplasia), but do not lead to hyperplasia....
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PMID: 19547887
PDF is available here.
PDF is available here.
Journal of Hypertension (27)3 2009
Nebivolol decreases endothelial cell stiffness via the estrogen receptor beta: a nano-imaging study.
Abstract
Both NEB as well as E2 decreased cellular stiffness to a similar extent (NEB: 0.83 +/- 0.03 pN/nm, E2: 0.87 +/- 0.03 pN/nm, vehicle: 2.19 +/- 0.07 pN/nm), whereas metoprolol had no effect on endothelial stiffness (2.07 +/- 0.04 pN/nm, all n = 60, P < 0.01). The decrease in stiffness occurred as soon...
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PMID: 19330906
PDF is available here.
PDF is available here.
Abstract
The linear naphtho-gamma-pyrone (LNGP) moiety is a naturally occurring scaffold with broad biological activity ranging through antimicrobial, antiviral, insecticidal and anti-estrogenic activity. This review, the first of its kind, surveys the chemical literature in an effort directed toward assembl...
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PMID: 19275720
PDF is available here.
PDF is available here.
Chinese Medical Journal (122)4 2009
Abstract
Estrogen deficiency deteriorates bladder ultra structure and histology. Supplementary estrogen can improve bladder function which may be due to inhibition of collagen hyperplasia and increased SM density. ERbeta has an important role in mediating estrogen function in the bladder. Tibolone has a mild...
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PMID: 19302740
PDF is available here.
PDF is available here.
Abstract
We describe the synthesis of an 11β isomer 3 of the steroidal antiestrogen fulvestrant 2. Partial fluorination of the 11β side chain in 3 leads to 4, which still shows strong antiproliferative activity on MCF-7 cells. However, unlike 2 and 3, compound 4 fails to down-regulate estrogen receptor α (...
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PMID: 19133777
PDF is available here.
PDF is available here.
Abstract
We find that combination therapy with the multitargeted growth factor receptor inhibitor vandetanib and the estrogen receptor antagonist fulvestrant inhibit tumor growth more effectively than either treatment administered alone. Thus, incorporation of antiestrogen treatment strategies in standard an...
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PMID: 19250205
PDF is available here.
PDF is available here.
Oncology Reports (21)2 2009
Abstract
We performed growth studies of estradiol and antiestrogens on estrogen receptor positive Ishikawa cells. The effects of estradiol and antiestrogens on the induction of VEGF and estrogen-responsive finger protein (Efp) were measured by QRT-PCR and ELISA or Western blotting. The siRNA method was used...
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PMID: 19148513
PDF is available here.
PDF is available here.
Abstract
We briefly review the recent clinical trials supporting the use of these agents in both the adjuvant and metastatic settings. We will discuss possible mechanisms of resistance to endocrine agents that could be exploited therapeutically to improve the outcome for patients with hormone receptor-positi...
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PMID: 19192957
PDF is available here.
PDF is available here.
Abstract
We applied suppression subtractive hybridization (SSH) to identify genes that are regulated by PEs through either the classic nuclear-based estrogen receptor or membrane-based estrogen receptor pathways. SSH, using mRNA from genistein (GE) treated MCF-7 cells as testers, resulted in a significant in...
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PMID: 19170076
PDF is available here.
PDF is available here.
Urologia Internationalis (82)2 2009
Abstract
Most current combination therapies consist of orphan medications without industry support. Andrology research centers and other dedicated departments and units need to conduct randomized controlled trials of sufficient duration, sample number and robust design for groups most likely to benefit from...
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PMID: 19321995
PDF is available here.
PDF is available here.
Neonatology (96)2 2009
Abstract
Treatment with ICI 182,780 increased ER-alpha mRNA, especially in cerebellum and hippocampus. There were no changes in ER-alpha protein and no changes in ER-beta at either the mRNA or protein level. CONCLUSION: Expression of ER-alpha is influenced by endogenous estrogens in the ovine fetal brain.
Co...
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PMID: 19279395
PDF is available here.
PDF is available here.
Journal of Andrology (30)5 2009
Abstract
Efferent ductules of the male reproductive tract contain high concentrations of estrogen receptors (ER), which are essential for the regulation of fluid reabsorption and maintenance of normal epithelial morphology. Treatments with the antiestrogen ICI 182,780 and 17beta-estradiol cause a reduction i...
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PMID: 19269934
PDF is available here.
PDF is available here.
Acta Oncologica (48)8 2009
Abstract
While novel endocrine treatment options have been implemented in the advanced - as well as adjuvant setting, recent results suggest a place for "old-fashioned" additive treatment with estrogens in advanced breast cancer. This paper reviews the biological rationale for endocrine therapy in general an...
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PMID: 19863216
PDF is available here.
PDF is available here.
Abstract
Estrogen-progestin combination HRT decreased measures of insulin resistance and hsCRP levels, but had no effect on platelet function tests in postmenopausal women.
Copyright 2008 S. Karger AG, Basel....
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PMID: 19060490
PDF is available here.
PDF is available here.
Molecular Biotechnology (41)1 2009
Abstract
We constructed a biosensor identified as bipartite recombinant yeast system (BRYS) to screen and evaluate subtype-selective ER ligands. Uniform design and immunoblotting was used to determine an optimal dose of copper which control the expression of ERs through a copper inducible metallothionine pro...
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PMID: 18751932
PDF is available here.
PDF is available here.
BMC Genomics (10)1 2009
Abstract
Steroidogenesis was down-regulated by EE(2) as reflected by the reduced plasma levels of testosterone in the exposed fish and down-regulation of genes in the steroidogenic pathway. Microarray analysis of testis of fathead minnows treated with 5 ng EE(2)/L or with the mixture of 5 ng EE(2)/L and 100...
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PMID: 19594897
PDF is available here.
PDF is available here.
Anti-Cancer Drugs (20)1 2009
Abstract
We have established estrogen-independent and antiestrogen-resistant cell lines from hormone-dependent MCF-7 breast cancer cells by long-term culture in the absence of estrogen, or in the presence of antiestrogen toremifene, respectively. By using a cDNA microarray we compared gene expression profile...
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PMID: 19343000
PDF is available here.
PDF is available here.
International Journal of Cancer (123)12 2008
Abstract
We hypothesized that, (1) dysregulation of gene expression and protein phosphorylation of the insulin-like growth factor (IGF) and steroid hormone receptor-signaling occur early in benign endometrial tissues and (2) signaling differences would be detected between patients with or without tamoxifen t...
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PMID: 18814240
PDF is available here.
PDF is available here.
Abstract
Endocrine disruptors refer to chemical compounds in the environment which interfere with the endocrine systems of organisms. Among them, environmental estrogens pose serious problems to aquatic organisms, in particular fish. It is therefore important and necessary to have a fast and low-cost system...
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PMID: 18980245
PDF is available here.
PDF is available here.
Journal of Clinical Oncology (26)35 2008
Abstract
Carcinogenesis (29)12 2008
Abstract
Our results show that artemisinin switches proliferative human breast cancer cells from expressing a high ERalpha:ERbeta ratio to a condition in which ERbeta predominates, which parallels the physiological state linked to antiproliferative events in normal mammary epithelium....
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PMID: 18784357
PDF is available here.
PDF is available here.
Abstract
We identify genes associated with response to endocrine therapy that may distinguish ER+, hormone responsive breast cancers, from ER+ tumors that exhibit intrinsic or de novo resistance. We suggest that the estrogen signaling pathway is aberrant in ER+ tumors with intrinsic resistance. Lastly, the s...
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PMID: 18327671
PDF is available here.
PDF is available here.
Abstract
PURPOSE: The risk factors for and risk assessment of breast cancer, recommendations for risk reduction, and roles of tamoxifen and raloxifene in the prevention of breast cancer are discussed. SUMMARY: Breast cancer either may be a familial syndrome or develop sporadically. In familial syndromes, can...
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PMID: 19020189
PDF is available here.
PDF is available here.
Abstract
No significant changes in lipid profile were found in patients continuing on tamoxifen. In the exemestane group, serum HDL-cholesterol (HDL-C) and triglycerides (TG) decreased significantly (p < 0.01) and serum LDL-cholesterol (LDL-C) increased significantly (p < 0.05) with respect to baseline. The...
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PMID: 19046724
PDF is available here.
PDF is available here.
Abstract
the 2.5 mg dose of tibolone had no effect on the Doppler velocimetry indexes of the ophthalmic and retinal arteries....
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PMID: 19148430
PDF is available here.
PDF is available here.
Ginekologia polska (79)11 2008
Abstract
Tibolone therapy leads to low rates of vaginal bleeding and atrophic changes of the endometrium. Tibolone is a safe and effective alternative to hormonal therapy in postmenopausal women....
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PMID: 19140498
PDF is available here.
PDF is available here.
Abstract
We report the antiproliferative effects of these compounds on human MCF-7 breast tumor cells. These heterocyclic compounds contain the triarylethylene arrangement as exemplified by tamoxifen, conformationally restrained through the incorporation of the benzoxepin ring system. The compounds demonstra...
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PMID: 18835176
PDF is available here.
PDF is available here.
Endocrinology (149)10 2008
Abstract
We report that TamR cells have increased levels of zinc and zinc transporter, ZIP7 [solute carrier family 39 (zinc transporter) member 7, also known as SLC39A7], resulting in an enhanced response to exogenous zinc, which is manifested as a greatly increased growth factor receptor activation, leading...
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PMID: 18583420
PDF is available here.
PDF is available here.
Abstract
Myomas (both leiomyomas and fibromas) are the most frequent benign uterine tumors in women, they can be found in 77% of hysterectomy specimens. There are reports that previous hormonal therapy (estrogen-progestin), more than five years, is associated with high risk (fourfold higher) of leiomyomas. A...
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PMID: 19062511
PDF is available here.
PDF is available here.
Abstract
We attempted to verify in an experimental model the role of cytoplasmic clusterin (CLU), a cytoprotective protein found to be up-regulated in antiestrogen-resistant patients, following neoadjuvant treatment with toremifene. The role of cytoplasmic clusterin in modulating response to two antiestrogen...
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PMID: 18813793
PDF is available here.
PDF is available here.
Molecular Endocrinology (22)10 2008
Abstract
Estradiol (E(2)) acts as a potent feedback molecule between the ovary and hypothalamic GnRH neurons, and exerts both positive and negative regulatory actions on GnRH synthesis and secretion. However, the extent to which these actions are mediated by estrogen receptors (ERs) expressed in GnRH neurons...
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PMID: 18701637
PDF is available here.
PDF is available here.
Biogerontology (9)5 2008
Abstract
These results suggest that the effects of gonad steroid on brain and blood physiology change significantly with aging, and that evaluating hormonal treatment types and doses could be the key factor in the potential use of a specific hormone therapy....
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PMID: 18386154
PDF is available here.
PDF is available here.
Abstract
There are large-scale molecular differences between estrogen receptor (ER)-positive and ER-negative breast cancers. Endocrine therapy has become the most important treatment option for women with ER-positive breast cancer, and approximately 70% of primary breast cancers express ERalpha. Endocrine th...
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PMID: 18946747
PDF is available here.
PDF is available here.
Cancer Letters (268)2 2008
Abstract
We have reported that the ectopic expression of progesterone receptor (PR) in MCF-7 cells disrupted the effects of estradiol-17beta (E2), and this anti-estrogenic effect of PR was associated with heightened E2 metabolism and inhibition of estrogen receptor (ER) binding to estrogen response element (...
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PMID: 18477500
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity ligands. All compounds had similar ERalpha and ERbe...
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PMID: 18722117
PDF is available here.
PDF is available here.