André J, Pfeiffer A, Rochefort H
Biochemistry. 1976 Jul 13;15(14):2964-9. doi: 10.1021/bi00659a005.
Ethidium bromide, an intercalating drug, was shown to inhibit the in vitro DNA binding of the uterine estradiol-receptor complex. The inhibition was reversible, dose dependent, complete for total saturation of DNA intercalating sites by the dye, and proportional to the extent of intercalated drug. The binding of the receptor to phosphocellulose and poly(adenylic acid)-cellulose was not decreased by this drug. Similar inhibition was also obtained with 9-hydroxyellipticine. Denatured DNA was more efficient at binding the estrogen receptor than phosphocellulose or poly(adenylic acid)-cellulose but less efficient than native DNA. We conclude that the DNA binding of the estrogen receptor cannot be simply interpreted in terms of electrostatic interactions but requires a particular double-helical structure of DNA.
溴化乙锭是一种嵌入性药物，已证明它能抑制子宫雌二醇受体复合物在体外与DNA的结合。这种抑制作用是可逆的，呈剂量依赖性，当染料完全饱和DNA嵌入位点时抑制作用完全，且与嵌入药物的量成正比。该药物不会降低受体与磷酸纤维素和聚（腺苷酸）纤维素的结合。9-羟基玫瑰树碱也能产生类似的抑制作用。变性DNA在结合雌激素受体方面比磷酸纤维素或聚（腺苷酸）纤维素更有效，但比天然DNA效率低。我们得出结论，雌激素受体与DNA的结合不能简单地用静电相互作用来解释，而是需要DNA特定的双螺旋结构。
