MCF-7/6 cells

Chen, W.-J., Armour, S., Way, J., Chen, G., Watson, C., Irving, P., Cobb, J., Kadwell, S., Beaumont, K., Rimele, T., and Kenakin, T. P. (1997). Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptors. Mol. Pharmacol. 52 1164-1175. 

All dihydroxybenzoates with an o-hydroxy group are more active against MCF-7 cells than the substituted salicylates screened previously. ... 

HSIEH c Y, SANTELL R c, HASLAM s z, HELFERICH w G (1998) Estrogenic effects of genistein on the growth of estrogen receptor-positive human breast cancer (MCF-7) cells in vitro and in vivo. Cancer Res. 58 3883-3838. 

PANNO M L, SALERNO M, PEZZI V, SISCI D, MAGGIOLINI M, MAURO L, MORRONE E G, ANDO S (1996) Effect of oestradiol and insulin on the proliferation pattern of oestrogen and progesterone receptor contents in MCF-7 cells. J Cancer Res Clin Oncol. 122 745-9. 

YCUNG H J, DCERGE D R, KIMBERLY F A, ALLRED C D and HELFERICH W G (2002) Dietary genistein negates the inhibitory effect of tamoxifen on growth of estrogen-dependent human breast cancer (MCF-7) cells implanted in athymic mice. Cancer Res 62,2474-77. 

Fig. 21. Molecular structures of new aromatic [M(ATSM)] analogs (a) M — Zn(II) and (b) M = Cu(II), (c) cytotoxicity tests in MCF-7 cells for the Zn(II) complex (group 2) and Cu(II) complex (group 3) and comparison with control and with cis-platin over a range of concentrations, (d) cell uptake profile monitored over 90 min, (e) confocal fluorescence imaging of Zn(II) complex in MCF-7 cells, at 100 pM cone, in DMEM, 1% DMSO (112,113).

DNA breaks in human MCF-7 cells [65], Damaging effect of menadione was probably mediated by hydroxyl radicals as it was demonstrated by ESR spin-trapping method. The analogs of menadione 2-methylmethoxynaphthoquinone and 2-chloromethylnaphtho-quinone also stimulated DNA damage through the formation of superoxide and other free radicals [66]. Similar effects have been shown for hydroquinone, catechol, benzoquinone, and benzenetriol [67,68]. 

Segnitz B, Ghering U (1995) Native structure of the estrogen receptor of MCF-7 cells in vivo . Proc Natl Acad Sci USA 92 2179... 

Miproxifene (TAT-59) is a prodrug of 4-hydroxy-tamoxifen that has been developed for tamoxifen-resistant carcinoma, but relatively little information has been published on this drug. Compared with tamoxifen, miproxifene inhibits estradiol-stimulated proliferation of MCF-7 cells at a threefold lower dose than that of tamoxifen, and of dimethyl-benzanthracene (DMBA)-induced rat mammary tumors at a dose tenfold lower than tamoxifen (Toko et al. 1990). In any event, in preclinical castrated rat models, it shows an endometrial stimulation activity that is similar to that of tamoxifen, which means it has limited potential use in the prevention or treatment of osteoporosis or cardiovascular disease (Shibata et al. 2000). Similarly, considering the preclinical findings of endometrial stimulation reported on GW5638 (Willson et al. 1997), it is likely that this new SERM belonging to the triphenylethylene family will be limited in clinical use to the treatment of advanced tamoxifen-resistant breast cancer once its efficacy is demonstrated in human clinical trials. 

Pure antiestrogens also act as competitive inhibitors of the estradiol-ER complex. For instance, ICI164384 is a competitive antagonist of both ERa and ER/ (Barkhem et al. 1998). In MCF-7 cells, similar amounts of estradiol and RU58668 are bound to ER (Jensen and Khan 2004). 

When used in tumor cells, fulvestrant was initially described as a potent, competitive growth inhibitor of ER-positive, human breast cancer MCF-7 cells, whose growth is stimulated by estradiol. The compound was ineffective in tumor cell lines without ER, such as MDA-MB-231. The inhibitory effects were more pronounced with fulvestrant than with tamoxifen in the same cell line (Wakeling et al. 1991). 

Huff KK, Knabe C, Linsey R (1988) Multihormonal regulation of insulin-like growth factor-1-related protein in MCF-7 cells. Mol Endocrinol 2 200-208... 

Compound 14 (IC50 = 0.30 pM against AKT-1) is representative of a series of pyridopyrizine AKT inhibitors [26], This compound inhibited AKT-mediated phosphorylation of GSK3fi in IGF-1-stimulated MCF-7 cells (IC50 = 0.5 pM). No kinase selectivity data were reported. 

An example of a TIE approach is that described by Desbrow et al. [7]. In this work, the endocrine disrupting activity detected in effluents of seven UK WWTPs by means of a yeast-based screening assay [52] was mainly attributed to the presence of estradiol, estrone, and ethynylestradiol. However, to assess the estrogenic activity different bioassays may be used, e.g., the yeast-based recombinant estrogen receptor-reporter assay (YES), the MCF-7 cell proliferation (E-screen), and the estrogen receptor-mediated chemically activated... 

The results are shown in Table 1. All compounds inhibited MCF-7 cell proliferation at a concentration of 0.33 mM except drupanin. Kaempferide inhibited proliferation most efficiently of all the compounds. 

Sapino A, Pietribiasi F, Bussolati G, and Marchisio PC [1986] Estrogen- and tamoxifen-induced rearrangement of cytoskeletal and adhesion structures in breast cancer MCF-7 cells. Cancer Res 46 2526-2531... 

In MDR cells, a significant fraction of P-gp is found associated with caveolin-rich membranes, and there is a substantial increase in the number of caveolae and caveolin-1 protein level. For example, both multidrug resistant human colon adenocarcinoma HT-29 cells and adriamycin-resistant breast adenocarcinoma MCF-7 cells display about a 12-fold increase in caveolin expression, which correlates with an approximate fivefold increase in morphologically identifiable caveolae [55], In addition, these cells exhibit increased amounts of phospholipase D and lipids such as cholesterol, glucosylceramide, and sphingomyelin [56, 57], Similarly, taxol-resistant A549 cells display both increased caveolin expression and caveolae numbers [58], While these correlations track with MDR, they do not suggest a simple mechanism for the role of... 

A. Bielawska, K. Bielawski, K. Chrzanowski, S. Wolczynski, Prolinase-Activated Prodrug for Cancer Chemotherapy. Cytotoxic Activity of Proline Analogue of Chlorambucil in Breast Cancer MCF-7 Cells , Farmaco 2000, 55, 736-741. 

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