In vitro characterization of new antiestrogens in human mammary tumor cells.

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.KeywordsHuman Breast Cancer Cell LineAmino GlutethimideRelative Binding AffinityHuman Mammary CarcinomaHuman Mammary Tumor CellThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.