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Anti-Growth Factor Activity of Antiestrogens in Human Breast Cancer Cells: A Review

  • Conference paper
Book cover Apoptosis in Hormone-Dependent Cancers

Part of the book series: Ernst Schering Research Foundation Workshop ((SCHERING FOUND,volume 14))

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Abstract

The conjunction of the long-recognized role of ovarian hormones on breast tumor growth (Beatson 1896) and the identification of intracellular estrogen receptors (ER; Jensen and Jacobson 1960) has prompted the design and therapeutic use of drugs which could selectively antagonize unfavorable steroid hormone action in their target tissues. Nonsteroidal antiestrogens were initially described by Lerner and coworkers in 1958; many structural derivatives of triphenylethylene have since been synthesized, the most widely used in breast cancer treatment being tamox-ifen (or Nolvadex) (Harper and Walpole 1966). Though their pharmacology is complex and often paradoxical, they all present common characteristic features. They interact with nuclear ER and display estrogen agonist activities which vary within species (human, chick, mouse, rat), tissue (uterus, breast, bone), or with the gene considered (progesterone receptor, cathepsin D, pS2). In the presence of estrogens, they act as competitive inhibitors for binding to nuclear steroid receptors and thus behave as strong hormone antagonists. On the basis of these recognized antagonistic properties, several antiestrogens have been tested clinically as agents for breast cancer therapy (Cole et al. 1971).

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Authors
  1. F. Vignon
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  2. H. Rochefort
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Editors and Affiliations

  1. W. Alton Jones Cell Science Center, 10 Old Barn Road, 12946, Lake Placid, NY, USA

    Martin Tenniswood

  2. Research Laboratories, Schering AG, Müllerstraße 170-178, 13342, Berlin, Germany

    Horst Michna

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© 1995 Springer-Verlag Berlin Heidelberg

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Vignon, F., Rochefort, H. (1995). Anti-Growth Factor Activity of Antiestrogens in Human Breast Cancer Cells: A Review. In: Tenniswood, M., Michna, H. (eds) Apoptosis in Hormone-Dependent Cancers. Ernst Schering Research Foundation Workshop, vol 14. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-03122-3_8

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  • DOI: https://doi.org/10.1007/978-3-662-03122-3_8

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-662-03124-7

  • Online ISBN: 978-3-662-03122-3

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