16α-[¹²⁵I]碘雌二醇与雌激素受体及其他类固醇结合蛋白的相互作用。
Interaction of 16 alpha-[125I]iodo-estradiol with estrogen receptor and other steroid-binding proteins.
作者信息
Hochberg R B, Rosner W
出版信息
Proc Natl Acad Sci U S A. 1980 Jan;77(1):328-32. doi: 10.1073/pnas.77.1.328.
Abstract
This communication describes the synthesis of 16 alpha-[125I]iodo-estradiol (125I-E2) with specific activities greater than 1000 Ci/mmol (1 Ci = 3.7 x 10(10) becquerels). We show that it binds to the same specific estrogen receptor sites as does [3H]estradiol and that it does so with an affinity that is indistinguishable from that for the latter steroid. This is true for receptor obtained from calf uterus and from a pool of human mammary carcinomas. There is no significant binding of 125 I-E2 to the testosterone-estradiol-binding globulin of human plasma. 125I-E2 also binds tightly to anti-estradiol antibodies raised against estradiol derivatized at carbons 3, 6, and 17. Finally, we show that unlabeled I-E2 is an active estrogen in vivo as demonstrated by its ability to increase uterine weight in ovariectomized rats.
摘要
本通讯描述了比活度大于1000居里/毫摩尔（1居里 = 3.7×10¹⁰贝可勒尔）的16α-[¹²⁵I]碘雌二醇（¹²⁵I-E₂）的合成。我们发现它与[³H]雌二醇一样，能结合到相同的特异性雌激素受体位点，且其结合亲和力与后者类固醇无法区分。从犊牛子宫和人乳腺癌组织库获得的受体都是如此。¹²⁵I-E₂与人血浆中的睾酮 - 雌二醇结合球蛋白没有显著结合。¹²⁵I-E₂还能紧密结合针对在3、6和17位碳上衍生化的雌二醇产生的抗雌二醇抗体。最后，我们表明未标记的I-E₂在体内是一种活性雌激素，这通过其增加去卵巢大鼠子宫重量的能力得到证明。
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Proc Natl Acad Sci U S A. 1980 Jan;77(1):328-32. doi: 10.1073/pnas.77.1.328.
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