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In Vitro Characterization of New Antiestrogens in Human Mammary Tumor Cells

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Predictive Drug Testing on Human Tumor Cells

Part of the book series: Recent Results in Cancer Research ((RECENTCANCER,volume 94))

Abstract

Nonsteroidal antiestrogens, whose chemical structures are based on or closely related to triphenylethylene, appear to have considerable potential for the treatment of hormone-dependent breast cancer. Especially Tamoxifen [trans-1-(4-β-dimethylaminoethoxyphenyl)-1.2-diphenyl but-1-ene] is now used routinely for the treatment of advanced breast cancer in women (Smith et al. 1981). Therapeutic response to Tamoxifen is correlated with the presence of estrogen receptors in mammary tumors (McGuire et al. 1978) In addition, these nonsteroidal compounds have successfully been used to suppress the growth of human breast cancer cell lines containing estrogen receptors (Lippman et al. 1976) and to elicit the regression of hormone-dependent mammary tumors in experimental animals (Rorke and Katzenellenbogen 1981). Although it is known that antiestrogens bind to the estrogen receptor in the respective target cells (Horwitz and McGuire 1978), the precise mechanism of antiestrogen action is not fully understood.

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References

  • Armelin HA, Wishikawa K, Sao GH (1974) Control of mammalian cell growth in culture: The action of protein and steroid hormones as effector substances. In: Clarkson B, Baserga R (eds) Control of proliferation in animal cells. Cold Spring Harbor Conferences on Cell Proliferation. vol 1. Cold Spring Harbor Laboratory, New York, pp 97–104

    Google Scholar 

  • Cowan S, Leake R (1979) The influence of the antiestrogen tamoxifen on DNA synthesis in the rat uterus. In: Agarwal M (ed) Antihormones. Elsevier, Amsterdam, pp 283–292

    Google Scholar 

  • Eckert LE, Katzenellenbogen BS (1982) Effects of estrogens and antiestrogens on estrogen receptor dynamics and the induction of progesterone receptor in MCF-7 human breast cancer cells. Cancer 42: 139–144

    CAS  Google Scholar 

  • Horwitz KB, McGuire WL (1978) Antiestrogens: Mechanism of action and effects in breast cancer. In: McGuire WL Jr (ed) Breast cancer: advances in research and treatment, vol 2. Plenum, New York, pp 155–204

    Google Scholar 

  • Horwitz KB, Costlow ME, McGuire WL (1975) A human breast cancer cell line with estrogen, androgen, progesterone and glucocorticoid receptors. Steroids 26: 785–795

    Article  PubMed  CAS  Google Scholar 

  • Kalb VF, Bernlohr RW (1977) A new spectrophotometric assay for protein in cell extracts. Anal Biochem 82: 362–371

    Article  PubMed  CAS  Google Scholar 

  • Korenman SG, Dukes BA (1970) Specific estrogen binding by the cytoplasm of human breast carcinoma. J Clin Endocrinol Metab 30: 639–645

    Article  PubMed  CAS  Google Scholar 

  • Lippman ME, Bolan G (1975) Oestrogen-responsive human breast cancer in long-term tissue culture. Nature 256: 592–593

    Article  PubMed  CAS  Google Scholar 

  • Lippman ME, Bolan G, Hiff K (1976) The effect of estrogens and antiestrogens on hormone-responsive human breast cancer in long-term tissue culture. Cancer Res 36: 4595–4601

    PubMed  CAS  Google Scholar 

  • Lowry OH, Rosebrough NJ, Farr AL, Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193: 265–275

    PubMed  CAS  Google Scholar 

  • McGuire WL, Zava DT, Horwitz KB, Chamness G (1978) Steroid receptors in breast tumours: current status. Curr Top Exp Endocrinol 3: 93–129

    PubMed  CAS  Google Scholar 

  • Nin EM, Neal RM, Pierce VK, Sherman MR (1981) Structural similarity of molybdate-stabilized steroid receptors in human breast tumors, uteri and leukolytes. J Steroid Biochem 15: 1–10

    Article  Google Scholar 

  • Richter A, Sanford KK, Evans VJ (1972) Influence of oxygen and culture media on plating efficiency of some mammalian tissue cells. J Natl Cancer Inst 49: 1705–1712

    PubMed  CAS  Google Scholar 

  • Rochefort H, Borgna J (1981) Differences between oestrogen receptor activation by oestrogen and anti-oestrogen. Nature 292: 257–259

    Article  PubMed  CAS  Google Scholar 

  • Roos W, Huber P, Oeze L, Eppenberger U (1982) Hormone dependency and the action of Tamoxifen in human mammary carcinoma cells. Anticancer Res 2: 157–162

    PubMed  CAS  Google Scholar 

  • Roos W, Oeze L, Löser R, Eppenberger U (1983) Antiestrogenic action of 3-hydroxytamoxifen in the human cancer cell line MCF-7. J Natl Cancer Inst 71: 55–59

    PubMed  CAS  Google Scholar 

  • Rorke EA, Katzenellenbogen BS (1981) Antitumor activities and estrogen receptor interactions of the metabolites of the antiestrogens C1628 and U23,469 in the 7.12-dimethylbenz(a)anthracene-induced rat mammary tumor system. Cancer Res 41: 1257–1262

    PubMed  CAS  Google Scholar 

  • Smith IE, Harris AL, Morgan M, Ford HT, Gazel JC, Harmer CL, White H, Parsons CA, Villardo A, Walsh G, McKinna JA (1981) Tamoxifen versus aminoglutethimide in advanced breast carcinoma: a randomized cross-over trial. Br Med J 283: 1432–1434

    Article  CAS  Google Scholar 

  • Soule HD, Vazquez J, Long A, Albert S, Brennan M (1973) A human cell line from a pleural effusion derived from a breast carcinoma. J Natl Cancer Inst 51: 1409–1416

    PubMed  CAS  Google Scholar 

  • Sutherland RL, Murphy LC, San Foo M, Green MD, Whybourne AM, Krozowski ZS (1980) High affinity antioestrogen-binding site distinct from the oestrogen receptor. Nature 288: 273–275

    Article  PubMed  CAS  Google Scholar 

  • Veith FO, Capony F, Garcia M, Chantelard J, Pujol H, Veith F, Zajdela A, Rochefort H (1983) Release of estrogen-induced glycoprotein with a molecular weight of 52.000 by breast cancer cells in primary culture. Cancer Res 43: 1861–1868

    PubMed  CAS  Google Scholar 

  • Westley B, Rochefort H (1980) A secreted glycoprotein induced by estrogen in human breast cancer cell lines. Cell 20: 353–362

    Article  PubMed  CAS  Google Scholar 

  • Zava DT, Wyler-von Ballmoos A, Goldhirsch A, Roos W, Takahashi A, Eppenberger U, Arrenbrecht S, Martz G, Losa G, Gomez F, Guelpa C (1982) A quality control study to assess the interlaboratory variability of routine estrogen and progesterone receptor assays. Eur J Cancer Clin Oncol 18: 713–721

    Article  PubMed  CAS  Google Scholar 

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© 1984 Springer-Verlag Berlin · Heidelberg

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Eppenberger, U., Küng, W., Löser, R., Roos, W. (1984). In Vitro Characterization of New Antiestrogens in Human Mammary Tumor Cells. In: Hofmann, V., Berens, M.E., Martz, G. (eds) Predictive Drug Testing on Human Tumor Cells. Recent Results in Cancer Research, vol 94. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-82295-7_27

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  • DOI: https://doi.org/10.1007/978-3-642-82295-7_27

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-82297-1

  • Online ISBN: 978-3-642-82295-7

  • eBook Packages: Springer Book Archive

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