Abstract
(a) only 20% to 25% of breast cancer cells treated with 4-OHT in vitro die via caspase-dependent cell death; more typically, the antiestrogen-treated ER+ breast cancer cells express increased levels of macroautophagy and are viable; (b) 4-OHT-induced cell death, but not 4-OHT-induced macroautophagy,...
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PMID: 18790778
PDF is available here.
Abstract
Our data suggest that epigenetic modulators can alter stability through modulation of HuR subcellular distribution. Taken together, these data provide a novel anti-estrogenic mechanism for AZA and TSA in ER positive human breast cancer cells....
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PMID: 17891453
PDF is available here.
Abstract
We have measured allelic imbalance in genomic DNA from the breast cancer cell lines T47D, MDA-MB-231, two antiestrogen sensitive (MCF7N and MCF7L) and two resistant MCF7 cell lines (MMU2 and LCC9) using single nucleotide polymorphism (SNP) oligonucleotide microarrays. DNA from MCF7(L) and MMU2 cells...
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PMID: 17899364
PDF is available here.
Abstract
We have investigated the impact of estrogen-mediated extranuclear-initiated pathways on global gene expression by using estrogen-dendrimer conjugates (EDCs), which because of their charge and size remain outside the nucleus and can only initiate extranuclear signaling. Genome-wide cDNA microarray an...
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PMID: 18617595
PDF is available here.
Steven R Cummings,
Bruce Ettinger,
Pierre D Delmas,
Peter Kenemans,
Victoria Stathopoulos,
Pierre Verweij,
Mirjam Mol-Arts,
Lenus Kloosterboer,
Lori Mosca,
Claus Christiansen,
John Bilezikian,
Eduardo Mario Kerzberg,
Susan Johnson,
Jose Zanchetta,
Diederich E Grobbee,
Wilfried Seifert,
Richard Eastell and
LIFT Trial Investigators
Abstract
Tibolone reduced the risk of fracture and breast cancer and possibly colon cancer but increased the risk of stroke in older women with osteoporosis. (ClinicalTrials.gov number, NCT00519857.)
2008 Massachusetts Medical Society...
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PMID: 18703472
PDF is available here.
Abstract
We studied the effect of WT1 on tamoxifen responsiveness in ERalpha-positive MCF-7 cells. We found that overexpression of WT1 in MCF-7 markedly abrogated tamoxifen-induced cell apoptosis and 17beta-estradiol (E(2))-mediated cell proliferation. The expressions of ERalpha and its downstream target gen...
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PMID: 18708366
PDF is available here.
Abstract
We studied the effect of WT1 on tamoxifen responsiveness in ERalpha-positive MCF-7 cells. We found that overexpression of WT1 in MCF-7 markedly abrogated tamoxifen-induced cell apoptosis and 17beta-estradiol (E(2))-mediated cell proliferation. The expressions of ERalpha and its downstream target gen...
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PMID: 18708366
PDF is available here.
Abstract
Our study demonstrated that fulvestrant, an ER antagonist used in the treatment of ER-positive breast cancer, combined with E2 and DHD or in combination with tibolone, is not compromised in its efficacy in inducing apoptosis in ER-positive breast cancer cell lines in vitro....
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PMID: 18645697
PDF is available here.
Abstract
This review will discuss the structural determinants and requirements necessary for estrogen receptors alpha and beta selectivity and ligand-receptor binding affinity. In addition, strategies likely to result in the development of a pharmacophore model that account for the differences in estrogenic...
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PMID: 18691152
PDF is available here.
Abstract
For the past 10 years it is known that oestrogen functions through the activation of two oestrogen receptors (ERalpha and ERbeta). To the great surprise of endocrinologists, ERbeta was found to be widely distributed in tissues throughout the body including tissues previously considered as 'oestrogen...
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PMID: 18513343
PDF is available here.
Abstract
These results suggest that estradiol is locally produced in NSCLC mainly by aromatase and plays an important role in the growth of ERalpha- or ERbeta-positive NSCLC. Therefore, use of selective ER modulators and/or aromatase inhibitors may be clinically effective in NSCLC that are positive for both...
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PMID: 18579664
PDF is available here.
Abstract
We show that 3,3'4,4'5-pentachlorobiphenyl (PCB126 - a dioxin-like AhR agonist) produced estrogenic responses in the absence of ER agonist, in fish in vitro system. We exposed salmon primary hepatocytes to PCB126 (1, 10 and 50 pM) and the ER agonist nonylphenol (NP; 5 and 10 microM) singly and also...
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PMID: 18378297
PDF is available here.
Abstract
We examined the effects of apigenin, a dietary plant flavonoid with potential anticancer properties, on estrogen-responsive, antiestrogen-sensitive MCF7 breast cancer cells and two MCF7 sublines with acquired resistance to either OHT or fulvestrant. We found that apigenin can function as both an est...
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PMID: 18645020
PDF is available here.
Christiane Otto,
Iris Fuchs,
Helga Altmann,
Mario Klewer,
Gilda Schwarz,
Rolf Bohlmann,
Duy Nguyen,
Ludwig Zorn,
Richardus Vonk,
Katja Prelle,
Thua Osterman,
Chira Malmström and
Karl-Heinrich Fritzemeier
Abstract
We analyse the in vivo behaviour of ER ligands that stimulate nongenomic ER effects to the same extent as estradiol, but show clearly reduced activation of genomic ER effects in vitro. Using different readout parameters such as morphological changes, cellular proliferation, and target gene induction...
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PMID: 18606537
PDF is available here.
Abstract
Estrogen receptor (ER) is an important drug target, but it has multiple signaling pathways that are difficult to dissect. A new study reports the development of a multicolor bioluminescent probe that can measure a compound's ability to modulate ER-mediated transcription and to promote an interaction...
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PMID: 18570353
PDF is available here.
Abstract
I was conducting research for my PhD on an obscure group of estrogen derivatives called nonsteroidal antiestrogens. Antiestrogens had failed to fulfill their promise as postcoital contraceptives and were unlikely to be developed further by the pharmaceutical industry. In 1972, that perspective start...
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PMID: 18519949
PDF is available here.
Abstract
We have observed that despite long-lasting growth inhibition, tumors eventually begin to grow during continued letrozole treatment. In cells isolated from these long-term letrozole-treated tumors (LTLT-Ca), estrogen receptor-alpha (ERalpha) levels were decreased, whereas signaling proteins in the mi...
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PMID: 18559495
PDF is available here.
Abstract
From the big randomized clinical trials there are evidences that adjuvant endocrine therapy for hormone-sensitive early breast cancer in postmenopausal women should include an aromatase inhibitor (AI). Anastrozole or letrozole should be used upfront for 5 years (ATAC and BIG 1-98), the sequential ap...
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PMID: 18640889
PDF is available here.
Abstract
We studied insulin sensitivity in 15 premenopausal nonhuman primates consuming either a high isoflavone soy diet or a soy-free casein/lactalbumin diet for 4 months. Insulin sensitivity was measured by intravenous glucose tolerance testing, hyperinsulinemic-euglycemic clamps, and insulin-stimulated i...
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PMID: 19083434
PDF is available here.
Abstract
The Rheum palmatum L., a traditional medicine in Korea, was screened for their estrogenic activity in a recombinant yeast system with a human estrogen receptor (ER) expression plasmid and a reporter plasmid used in a previous study. The EC50 values of the n-hexane, dichloromethane, ethyl acetate, n-...
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PMID: 18563353
PDF is available here.
Abstract
There were no adverse events resulting from the stellate-ganglion block, although patients had temporary Horner's syndrome indicating the effectiveness of the block. Five patients had only one stellate-ganglion block and eight had two stellate-ganglion blocks. The total number of hot flushes decreas...
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PMID: 18485819
PDF is available here.