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lanosterol/cáncer de mama
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Effect of estradiol and antiestrogens on cholesterol biosynthesis in hormone-dependent and -independent breast cancer cell lines.
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The effects of estradiol and/or antiestrogens on cholesterol biosynthesis were studied in two breast cancer cell lines. Cholesterogenic activity was evaluated after labeling cells with sodium [14C]acetate for increasing periods of time (up to 24 h) and measuring the incorporation of the
Breast cancer and (25R)-26-hydroxycholesterol.
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(25R)-26-Hydroxycholesterol (27-hydroxycholesterol) has been found to accumulate in breast tissue and to stimulate tumor growth via the estrogen receptor. Although most tissues express CYP27A1, the highest levels are in macrophages and most attention had been given to the production of
Ligands of the antiestrogen-binding site induce active cell death and autophagy in human breast cancer cells through the modulation of cholesterol metabolism.
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We have recently reported that cytostatic concentrations of the microsomal antiestrogen-binding site (AEBS) ligands, such as PBPE (N-pyrrolidino-(phenylmethyphenoxy)-ethanamine,HCl) and tamoxifen, induced differentiation characteristics in breast cancer cells through the accumulation of
Inhibition of human CYP19 by azoles used as antifungal agents and aromatase inhibitors, using a new LC-MS/MS method for the analysis of estradiol product formation.
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Azoles are used as fungicides in agriculture or antifungal drugs in medicine. Their therapeutic activity is based on the inhibition of fungal lanosterol-14alpha-demethylase (CYP51). Azoles are also used for the treatment of estrogen-dependent diseases, e.g. in breast cancer therapy. Inhibition of
Molecular characterization of the microsomal tamoxifen binding site.
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Tamoxifen is a selective estrogen receptor modulator widely used for the prophylactic treatment of breast cancer. In addition to the estrogen receptor (ER), tamoxifen binds with high affinity to the microsomal antiestrogen binding site (AEBS), which is involved in ER-independent effects of
Comparative assessment of the inhibition of recombinant human CYP19 (aromatase) by azoles used in agriculture and as drugs for humans.
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Azoles (imidazoles and triazoles) are used as antifungal agents in agriculture and in medicine, and also for antiestrogen therapy, e.g., for breast cancer treatment. Antifungal activity is based on inhibition of fungal CYP51 (lanosterol 14alpha-demethylase), and estrogen biosynthesis reduction is
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