Inhibition of the estradiol-induced growth of cultured human breast cancer cells by the anti-estrogens tamoxifen, desmethyl-tamoxifen, 4-hydroxy-tamoxifen and enclomiphene.
Inhibition of the estradiol-induced growth of cultured human breast cancer cells by the anti-estrogens tamoxifen, desmethyl-tamoxifen, 4-hydroxy-tamoxifen and enclomiphene.
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DOI：
10.1016/0006-2952(84)90007-8
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发表时间：
1984-12
影响因子：
5.8
通讯作者：
C. Marth;G. Daxenbichler;G. Buehring;F. Hofstädter;O. Dapunt
中科院分区：
文献类型：
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作者：
C. Marth;G. Daxenbichler;G. Buehring;F. Hofstädter;O. Dapunt
他莫昔芬（T）、去甲基-他莫昔芬（dMeT）、4-羟基-他莫昔芬（OHT）和恩氯米芬（Clo）对培养的人乳腺癌细胞系的生长作用与已发表的雌激素受体结合亲和力有关。只有在受雌激素刺激的细胞中，这些抗雌激素才能显著抑制生长。在检测的两种雌激素敏感细胞系734 B和ZR 75.1中，抗雌激素活性显示出相同的等级：OHT-Clo-T-dMeT;这种抗增殖效力与这些化合物对雌激素受体的报道亲和力一致。在含有确定量雌二醇的培养基中，我们观察到需要10，000倍摩尔过量的OHT来抑制雌二醇诱导的生长，但雌二醇非依赖性增殖不受影响。
The growth effects of tamoxifen (T), desmethyl-tamoxifen (dMeT), 4-hydroxy-tamoxifen (OHT) and enclomiphene (Clo) on cultured human breast cancer cell lines have been related to published binding affinities for the estrogen receptor. Only in cells which were stimulated by estrogens did these anti-estrogens markedly inhibit growth. In both estrogen sensitive cell lines tested, 734 B and ZR 75.1, the anti-estrogen activity showed the identical rank: OHT⪢ Clo≊ T∼≌ dMeT; this antiproliferative potency agrees with reported affinities of these compounds for the estrogen receptor. In culture media containing defined amounts of estradiol we observed that a 10,000-fold molar excess of OHT was required to inhibit the estradiol-induced growth, but the estradiol-independent proliferation was not affected.