Kimmel G L, Harmon J R, Slikker W
Teratog Carcinog Mutagen. 1983;3(4):355-65. doi: 10.1002/1520-6866(1990)3:4<355::aid-tcm1770030405>3.0.co;2-k.
Cytosol receptor binding of 17 beta-estradiol was demonstrated in the uterus of the late-gestation, fetal rhesus monkey. Sucrose density gradient analysis performed in low-ionic strength buffer indicated a binding component with a sedimentation coefficient of 6-7 S. Under high-ionic strength conditions, the component shifted to a sedimentation coefficient of approximately 4 S. The specificity of the receptor for estrogens was indicated by inhibition of [3H]estradiol binding by both natural and synthetic estrogen competitors, but not by progesterone. Saturation analysis indicated a high degree of nonspecific binding with saturation of specific binding occurring at 2-3 nM. Computer-assisted Scatchard analysis of the data resolved a one-receptor model having a limited number of binding sites and an apparent dissociation constant of 10(-10) M. The interaction of estrogens with the fetal uterus and the cellular mechanisms which permit this interaction are discussed in relation to the development of models for extrapolation to the human.
在妊娠后期恒河猴胎儿的子宫中证实了17β-雌二醇与胞质溶胶受体的结合。在低离子强度缓冲液中进行的蔗糖密度梯度分析表明,存在一种沉降系数为6 - 7 S的结合成分。在高离子强度条件下,该成分的沉降系数转变为约4 S。天然和合成雌激素竞争剂均能抑制[3H]雌二醇结合,而孕酮则不能,这表明该受体对雌激素具有特异性。饱和分析表明存在高度的非特异性结合,特异性结合在2 - 3 nM时达到饱和。对数据进行计算机辅助的Scatchard分析解析出一个单受体模型,该模型具有有限数量的结合位点,表观解离常数为10(-10) M。结合人类外推模型的发展,讨论了雌激素与胎儿子宫的相互作用以及允许这种相互作用的细胞机制。