Westley B R, May F E
University Department of Pathology, Royal Victoria Infirmary, Newcastle upon Tyne, United Kingdom.
Biochem Biophys Res Commun. 1988 Sep 30;155(3):1113-8. doi: 10.1016/s0006-291x(88)81255-5.
The EFM-19 human breast cancer cell line contains high levels of oestrogen receptor mRNA and is oestrogen responsive for growth. The oestrogen receptor gene appears to be specifically regulated by oestrogens in EFM-19 cells. The induction by oestradiol is half-maximal in the presence of 3 x 10(-11) M oestradiol. LY117018 is a potent antioestrogen with a similar affinity to oestradiol for the oestrogen receptor. LY117018 completely blocks the induction of the oestrogen receptor mRNA by oestradiol when it is present in a 50-fold molar excess. The ability of oestrogens to control the levels of their own receptor in human breast cancer cells has implications for the understanding of oestrogen responsiveness and the amelioration of endocrine therapy.
EFM - 19人乳腺癌细胞系含有高水平的雌激素受体mRNA,且对雌激素刺激生长有反应。雌激素受体基因在EFM - 19细胞中似乎受到雌激素的特异性调控。在存在3×10⁻¹¹ M雌二醇的情况下,雌二醇诱导作用达到半数最大效应。LY117018是一种强效抗雌激素,对雌激素受体的亲和力与雌二醇相似。当LY117018以50倍摩尔过量存在时,它能完全阻断雌二醇对雌激素受体mRNA的诱导。雌激素控制其自身受体在人乳腺癌细胞中的水平的能力,对于理解雌激素反应性和改善内分泌治疗具有重要意义。