DISPLACEMENT OF ESTRADIOL FROM ESTROGEN RECEPTORS BY SIMPLE ALKYL PHENOLS
DISPLACEMENT OF ESTRADIOL FROM ESTROGEN RECEPTORS BY SIMPLE ALKYL PHENOLS
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DOI：
10.1210/endo-102-5-1429
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发表时间：
1978-01-01
期刊：
影响因子：
4.8
通讯作者：
KIM, UH
中科院分区：
文献类型：
--
作者：
MUELLER, GC;KIM, UH
简单的烷基酚已被测试其能力，以防止结合的[3H]雌二醇和取代预先绑定的激素从雌激素受体的[大鼠]子宫胞质溶胶。四氢萘，雌二醇A和B环的类似物，在阻止雌二醇的正向结合方面非常有效。具有对应于雌二醇的B环的柔性烷基链的对仲戊基苯酚（pSAP）在0 ℃下是高度有效的。C取代受体预结合的雌二醇。两种化合物在0 ℃时更有效。C比23. C.这些数据进行了讨论，在顺序的构象变化，可能需要的天然激素的结合和释放及其可能的相关性受体的行动。
Simple alkyl phenols have been tested for their ability to prevent the binding of [3H]estradiol and to displace the prebound hormone from estrogen receptors of [rat] uterine cytosols. Tetrahydronaphthol, an analog of the A and B rings of estradiol, is highly effective in preventing the forward binding of estradiol. p-sec-Amyl phenol (pSAP) with a flexible alkyl chain corresponding to the B ring of estradiol is highly effective at 0.degree. C in displacing estradiol which was prebound by the receptor. Both compounds were more effective at 0.degree. C than at 23.degree. C. The data are discussed in terms of sequential conformational changes which might be required for the binding and release of the natural hormones and their possible relevance to receptor action.