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Chapter 40,819

Nonsteroidal antiestrogens are estrogen-receptor-targeted growth inhibitors that can act in the absence of estrogens

Rochefort, H.

Hormone Research 28(2-4): 196-201

1987


ISSN/ISBN: 0301-0163
PMID: 3331372
DOI: 10.1159/000180944
Accession: 040818893

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The mechanism of the antiproliferative effect of nonsteroidal antiestrogens (tamoxifen, hydroxytamoxifen) is discussed from studies performed in human breast cancer cell lines. At least two types of mechanism have been evidenced. In the presence of estrogens, antiestrogens behave as classical antihormones and their inhibition of cell proliferation is likely due to inhibition of the synthesis and release of several estrogen-induced mitogens (growth factors and proteases). In the absence of estrogens (cells cultured in phenol-red-free medium), antiestrogens can still inhibit the effect of growth factors (EGF, insulin). At concentrations less than or equal to 4 microM, antiestrogens are also cytotoxic and they require accessible estrogen receptors for their action. 'Estrogen-receptor-targeted drugs' is therefore a better general term than 'antiestrogens' to describe the mechanism of action of these drugs, which can also function without inhibiting estrogen action.

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