Breast Cancer Research and Treatment

, Volume 31, Issue 1, pp 5–9

Alternative mechanisms of action of anti-oestrogens

  • Anthony A. Colletta
  • John R. Benson
  • Michael Baum


The molecular mechanism of action of anti-oestrogens such as tamoxifen appears to be a complex mixture of antagonism of the mitogenic action of oestradiol at the level of the oestrogen receptor, plus a range of other activities from enzyme inhibition to growth factor modulation. This article will concentrate on two specific areas: 1) the inhibition of protein kinase C and calmodulin-dependent cAMP phosphodiesterase; and 2) the regulation by tamoxifen of peptide regulators of breast cancer epithelial cell growth such as insulin-like growth factor I (IGF I) and transforming growth factor beta (TGF-β). The elucidation of these mechanisms is potentially important in the treatment and chemoprevention of breast cancer — the quantitative contribution of each individual mechanism of the overall antineoplastic action of anti-oestrogens is central to developing new and possibly more effective anti-oestrogens and optimizing strategies for their use.

Key words

antiestrogens cAMP phosphodiesterase growth factors insulin-like growth factors protein kinase C tamoxifen transforming growth factor beta 


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Copyright information

© Kluwer Academic Publishers 1994

Authors and Affiliations

  • Anthony A. Colletta
    • 1
  • John R. Benson
    • 1
  • Michael Baum
    • 1
  1. 1.Section of Academic SurgeryInstitute of Cancer Research, Royal Marsden HospitalLondonUK

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