微分雌激素受体拮抗剂对垂体lactotroph增殖的影响和催乳素释放。

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Kansra年代,山形,Sneade L,促进L, Ben-Jonathan N

微分雌激素受体拮抗剂对垂体lactotroph增殖的影响和催乳素释放。

摩尔细胞性。2005年7月15日,239 (2):27-36。

PubMed ID

15950373 (在PubMed

]

文摘

抗雌激素作用通过抑制雌激素受体(ER)的功能。展览与雷洛昔芬和三苯氧胺受体激动剂和拮抗剂性质,ICI 182780 (ICI)被认为是一个“纯”抗雌激素缺乏任何竞赛的活动。而有足够的信息抗雌激素在乳腺癌和子宫的影响,对他们的行动在垂体,对于主内分泌腺。beplayapp我们的目标是:(1)比较ICI的影响,他莫昔芬和雷洛昔芬lactotroph扩散在缺乏雌性激素的情况下,(2)确定他们的行动是否通过ER介导的,和(3)比较对催乳素(PRL)释放的影响。我们报告,这里是一个lactotroph扩散的有效抑制剂(MMQ和GH3细胞)与最大抑制45 - 50% 1海里。这里是几个数量级比雷洛昔芬的同时它莫西芬没有影响。无论是抗雌激素影响T47D乳腺癌细胞增殖。GH3细胞孵化与ICI 1 h只引起最大抑制细胞增殖,由co-incubation逆转与雌激素产生影响。这么短的接触ICI ERalpha的差别足以导致快速和持续对这些蛋白质,ERbeta的差别而对这些明显延迟;他莫昔芬和雷洛昔芬没有明显的对ER (s)水平的影响。 The ability of ICI to inhibit GH3 cell proliferation is dependent upon ERalpha, since an ERalpha, but not ERbeta, specific agonist reverses the effect of ICI. PRL release is differentially regulated by the anti-estrogens. ICI at 0.1nM suppresses PRL release from GH3 cells by 80%, with a similar strong suppression also seen with 10nM raloxifene. However, tamoxifen at 0.01nM inhibits PRL release but has no effect at 10nM. Cell co-incubation with ICI and estradiol results in a four-fold increase in PRL release. Taken together, our study shows that ICI, in the absence of exogenous estrogens, inhibits lactotroph proliferation and PRL release by downregulating or inactivating ERalpha. The dissimilar responses of cell proliferation and PRL release to the anti-estrogens suggest that both processes are regulated by different mechanisms. These data highlight the importance of studying the effects of anti-estrogens in multiple systems.

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