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    The novel estrogen 17alpha-20Z-21-[(4-amino)phenyl]-19-norpregna-1,3,5(10),20-tetraene-3,17be ta-diol induces apoptosis in prostate cancer cell lines at nanomolar concentrations in vitro

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    Authors
    Mobley, James A.
    L'Esperance, James O.
    Wu, Mengchu
    Friel, Carolyn J.
    Hanson, Robert H.
    Ho, Shuk-Mei
    UMass Chan Affiliations
    Department of Surgery, Division of Urology
    Graduate School of Biomedical Sciences
    Document Type
    Journal Article
    Publication Date
    2004-05-14
    Keywords
    Apoptosis; Blotting, Western; Bromodeoxyuridine; Caspase 3; Caspases; Cell Cycle; Cell Line, Tumor; Drug Screening Assays, Antitumor; Estradiol; Estrogen Receptor alpha; Estrogen Receptor beta; Flow Cytometry; Humans; Male; Models, Molecular; Prostatic Neoplasms; Protein Binding
    Life Sciences
    Medicine and Health Sciences
    
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    Link to Full Text
    http://mct.aacrjournals.org/content/3/5/587.long
    Abstract
    Prostate cancer remains the number one cause of noncutaneous cancer, with 220,900 new cases predicted for the year 2003 alone. Of the more promising classes of compounds studied thus far for the treatment of prostate cancer, estrogens of various types have consistently exhibited antitumor activities both in vitro and in vivo. For this reason, we have synthesized and screened a library of unique 17alpha/11beta modified 17beta-estradiol (E(2)) analogues designed for estrogen receptor beta (ER-beta) specificity and a potential for cytotoxic activity directed toward prostate cancer cells. From this library, the novel compound 17alpha-20Z-21-[(4-amino)phenyl]-19-norpregna-1,3,5(10),20-tetraene-3,17be ta-diol (APVE(2)) was identified as the primary lead, found to induce a high level (>90%) of cell death through an apoptotic mechanism, with an EC(50) of 1.4, 2.7, and 16 nM in the LNCaP, PC3, and DU145 cell lines, respectively. APVE(2) was found to bind to ER-beta, albeit weakly, with an EC(50) of 250 nM and a binding activity of 6.2% relative to E(2), nearly two orders of magnitude less than the concentration required to induce apoptosis. APVE(2) bound preferentially to ER-beta by 7-fold over ER-alpha, and did not induce growth in the MCF-7 cell line, thus indicating that it is not a classical ER agonist. Furthermore, the cytotoxic actions of APVE(2) were not reversed by co-treatment with a 50-fold excess E(2). In summary, a novel 17 modified estrogen APVE(2) was identified as a lead compound, capable of inducing apoptosis in three prostate cancer cell lines at low nanomolar concentrations, through a mechanism inconsistent with an ER-mediated mechanism.
    Source

    Mol Cancer Ther. 2004 May;3(5):587-95.

    Permanent Link to this Item
    http://hdl.handle.net/20.500.14038/34218
    PubMed ID
    15141016
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