title: Comparative studies on the effects of steroidal and nonsteroidal oestrogen antagonists on the proliferation of human breast cancer cells.
abstract: Pure and partial agonist antioestrogens, exemplified by ICI 164,384 and tamoxifen or 4-hydroxytamoxifen (4'-OHT) respectively, differ in their capacity to inhibit the growth of MCF-7 human breast cancer cells. Under basal conditions which maintain but do not permit proliferation of MCF-7 cells, growth rate was enhanced by oestradiol, Phenol Red, insulin and 4'-OHT but not by ICI 164,384. Oestradiol and insulin together enhanced cell growth rate synergistically. 4'-OHT, but not ICI 164,384, similarly increased insulin-stimulated cell growth in the absence of oestradiol. ICI 164,384 blocked the stimulatory action of 4'-OHT. The stimulatory effect of the peptide growth factors TGF-alpha and IGFI on MCF-7 cells were attenuated by ICI 164,384 and 4'-OHT; ICI 164,384 was more effective than 4'-OHT. The antiproliferative action of ICI 164,384 on oestradiol or growth factor stimulated MCF-7 cells was only weakly inhibited by TGF-beta antibodies.
authors.affiliation: Bioscience Department, ICI Pharmaceuticals, Macclesfield, Cheshire, U.K.
authors.forename: A E
authors.initials: AE
authors.lastname: Wakeling
mesh_terms: D001943:Breast Neoplasms; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology*; D004965:Estrogen Antagonists / Q000494:pharmacology*; D005260:Female; D006801:Humans; D007328:Insulin / Q000494:pharmacology; D007700:Kinetics; D053284:Polyunsaturated Alkamides; D013329:Structure-Activity Relationship; D013629:Tamoxifen / Q000031:analogs & derivatives / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000166:cytology / Q000187:drug effects*
chemical_list: D004965:Estrogen Antagonists; D007328:Insulin; D053284:Polyunsaturated Alkamides; D013629:Tamoxifen; C016601:afimoxifene; D004958:Estradiol; C051781:ICI 164384