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The effect of an estrone D-lactam steroid ester derivative on breast cancer cells and its predicted binding interactions with the ligand binding domain of estrogen receptor-alpha.
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In order to further improve the toxicity profile and the anticancer effect of chlorambucil (CBL), we have synthesized a new estrone D-lactam steroidal ester of CBL (ESBL). The aim of this study was to investigate the in vitro activity of ESBL against primary breast carcinoma (BC) cells of operable
Dietary soy isoflavones and estrone protect ovariectomized ERalphaKO and wild-type mice from carcinogen-induced colon cancer.
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Consumption of soy foods has been weakly associated with reduced colon cancer risk. Colon cancer risk is influenced by estrogen exposure, although the mechanism through which this occurs is not defined. Conversion of estradiol (E2) to estrone (E1) may be protective in the colon. We hypothesized that
Estrone and progesterone inhibit the growth of murine MC38 colon cancer line.
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The unsatisfactory effectiveness of reference chemotherapy in colon cancer (fluorouracil - FU) results in continuous search for agents, which could enhance the action of FU. Some epidemiological data such as a decreased risk of colorectal cancer among menopausal women receiving hormonal replacement
Conversion of estrone to 17-beta-estradiol in human non-small-cell lung cancer cells in vitro.
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It has recently been suggested that, in addition to genetic and environmental factors and tobacco exposure, estrogens also may be an independent risk factor in the development of lung cancer. Therefore, we evaluated the transcript and protein levels of 17-beta-hydroxysteroid-dehydrogenase type 1
Dehydroepiandrosterone and estrone 17-ketosteroid reductases in MCF-7 human breast cancer cells.
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The identification of several steroid-transforming enzymes within human breast cancers has led to speculation that the growth of some hormone-responsive tumors might be mediated in part by intracellularly derived estrogens. Reports that MCF-7 human breast cancer cells can transform both estrone
A novel cancer targeting approach based on estrone anchored stealth liposome for site-specific breast cancer therapy.
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We here report the successful utilization of estrogen receptor (ER) for the delivery of anticancer drug doxorubicin (DOX) encapsulated within pegylated liposome for the treatment of breast cancer. Estrone (ES) was anchored as ligand on to stealth liposome (ES-SL-DOX) for targeting to ERs. In vitro
Dual cancer targeting using estrogen functionalized chitosan nanoparticles loaded with doxorubicin-estrone conjugate: A quality by design approach
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In this study, estrone was used as targeting functionality in chitosan nanoparticles (DoxEs-CSEsNPs) carrying doxorubicin-estrone conjugate for dual targeted intracellular delivery to breast cancer cells. Estrone was conjugated with Dox and CS and characterized by FTIR and FT-NMR spectroscopy.
Estrone and 17beta-estradiol reverse breast cancer resistance protein-mediated multidrug resistance.
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Breast cancer resistance protein (BCRP), an adenosine triphosphate-binding cassette transporter, confers resistance to a series of anticancer reagents, including mitoxantrone, SN-38 and topotecan. In the present study, we found that estrone and 17beta-estradiol potentiated the cytotoxicity of
Inhibition of peripheral aromatization of androstenedione to estrone in postmenopausal women with breast cancer using delta 1-testololactone.
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To determine if delta 1-testololactone can inhibit the peripheral aromatization of androstenedione (delta), nine postmenopausal women with metastatic breast cancer were studied before and after 2 weeks of therapy with 250 mg of the drug, given every 6 h by mouth. The conversion ratio of delta to
Inhibition of placental estrone sulfatase activity and MCF-7 breast cancer cell proliferation by estrone-3-amino derivatives.
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Estrogen levels in breast tumors of post-menopausal women are as much as 10 times higher than in plasma, presumably due to in situ formation of estrogen. Several lines of evidence indicate that the major source of estrogen in breast cancer cells may be from conversion of estrone sulfate to estrone
Inhibition of estrone sulfatase activity by estrone-3-methylthiophosphonate: a potential therapeutic agent in breast cancer.
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Many breast tumors are hormone dependent, and there is evidence that hydrolysis of estrone sulfate (E1S) to estrone, by estrone sulfatase, is an important source of the estrogen which is found in tumors. In this study, we have developed a novel pathway for the synthesis of
Inhibition of estrone sulfatase and proliferation of human breast cancer cells by nonsteroidal (p-O-sulfamoyl)-N-alkanoyl tyramines.
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Estrogen levels in breast tumors of postmenopausal women are as much as 10 times higher than estrogen levels in plasma, presumably due to in situ formation of estrogen. The major source of estrogen in breast cancer cells may be the conversion of estrone sulfate to estrone by the enzyme estrone
Estrone sulfatase versus estrone sulfotransferase in human breast cancer: potential clinical applications.
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Estrone sulfate (E1S) is concentrated in high levels in human breast cancer tissue. The values are particularly high in postmenopausal women and many times those circulating in the plasma. Also, the tissular concentration of this conjugate are significantly higher in tumoural tissue than in the area
Effect of tibolone (Org OD14) and its metabolites on estrone sulphatase activity in MCF-7 and T-47D mammary cancer cells.
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Tibolone (Org OD14) is a synthetic steroid with weak estrogenic, progestagenic and androgenic properties which is used for the treatment of menopausal complaints. Since the compound possesses estrogenic activity, it is important to assess its effects on pathways in breast cells involved in the
Measurement of estrone sulfate in postmenopausal women: comparison of direct RIA and GC-MS/MS methods for monitoring response to endocrine therapy in women with breast cancer.
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BACKGROUND
High concentrations of estrone sulfate (EIS) are present in serum of pre- and postmenopausal women. Most assays for this estrogen conjugate involve enzyme hydrolysis and chromatographic purification prior to RIA. We have compared concentrations of serum EIS in postmenopausal women
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