INHIBITION OF GLUCOCORTICOSTEROID ACTION IN CULTURED L-929 MOUSE FIBROBLASTS BY RU486, A NEW ANTI-GLUCOCORTICOSTEROID OF HIGH-AFFINITY FOR THE GLUCOCORTICOSTEROID RECEPTOR
INHIBITION OF GLUCOCORTICOSTEROID ACTION IN CULTURED L-929 MOUSE FIBROBLASTS BY RU486, A NEW ANTI-GLUCOCORTICOSTEROID OF HIGH-AFFINITY FOR THE GLUCOCORTICOSTEROID RECEPTOR
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DOI：
10.1016/0014-4827(83)90282-3
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发表时间：
1983-01-01
影响因子：
3.7
通讯作者：
BAULIEU, EE
中科院分区：
文献类型：
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作者：
JUNGTESTAS, I;BAULIEU, EE
糖皮质激素地塞米松（dex）可抑制L-929小鼠成纤维细胞的体外生长，并使细胞增殖抑制。RU 486，一种新的合成抗激素类固醇，在含血清培养基和无血清，化学成分确定的培养基中，这些作用被废除。RU 486没有显示任何糖皮质激素样活性。3 H-RU 486以高亲和力（Kdeq. 0.4 nM）与dex相同的高亲和力受体结合位点（Kd apprx. 0.5 nM），如Scatchard图、梯度超离心和竞争研究所示。在37 ℃下用3 H-RU 486孵育全细胞后，C，在细胞核中发现了放射性抗凋亡素-受体复合物。然而，与3 H-dex相比的定量研究表明，拮抗剂比激动剂引起更少的核受体复合物。
The rate growth of L-929 mouse fibroblasts in vitro is decreased by the glucocorticosteroid dexamethasone (dex) in vitro, and cell adhesiveness. These effects were abolished by RU 486, a new synthetic anti-hormone steroid, in both serum-containing medium and serum-free, chemically defined culture medium. RU 486 did not display any glucocorticosteroid-like activity. 3H-RU 486 binds with high affinity (Kdeq .apprx. 0.4 nM) to the same high affinity receptor-binding sites as dex (Kd .apprx. 0.5 nM) in the cell cytosol, as indicated by Scatchard plot, gradient-ultracentrifugation and competition studies. After incubation of whole cells with 3H-RU 486 at 37.degree. C, a radioactive antihormone-receptor complex was found in the nucleus. However, quantitative studies vs. 3H-dex indicated that the antagonist provokes less nuclear receptor complex than the agonist.