Abstract:
:Synthetic antiestrogens such as Tamoxifen (Nolvadex) are currently used to treat postmenopausal breast cancer. Their mechanism of action is reviewed at the cellular and molecular level, through data of the literature and the current view of the author. Synthetic antiestrogens are mostly acting directly on breast cancer cells by interacting with the estrogen receptor (RE). They prevent estrogen action by competing with estrogens on the cytosol RE. The resulting complex is partially activated resulting in its nuclear localisation and a partial and dissociated stimulation of the expression of estrogen responsive genes. The explanation of the antitumoral effect of these drugs is more controversial, since the regulation of cell proliferation is not only due to estrogens but also to other hormones and factors. The antiestrogens can therefore block cancer cell growth by inhibiting estrogen action, or by a RE medicated cytotoxic effect and/or by any other mechanism involving indirect effects, or binding to other proteins than the RE.
journal_name
Biochimiejournal_title
Biochimieauthors
Rochefort Hdoi
10.1016/s0300-9084(82)80411-2subject
Has Abstractpub_date
1982-02-01 00:00:00pages
89-98issue
2eissn
0300-9084issn
1638-6183pii
S0300-9084(82)80411-2journal_volume
64pub_type
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