Fox T O
Proc Natl Acad Sci U S A. 1975 Nov;72(11):4303-7. doi: 10.1073/pnas.72.11.4303.
Androgen- and estrogen-binding macromolecules from the hypothalamus plus preoptic area of 3- to 4-week-old mice have been detected and partially characterized. These components bind the respective hormones with high affinity (saturating at 4-8 nM) and sediment with rates typical of presumed steroid receptors (4.0-4.5 S in 0.15 M NaCl, 5.0-7.5 S without salt). A 90-95% reduction in androgen binding found in the androgen-insensitivity mutant mouse, testicular feminization (Tfm), provides a genetic control for the specificity of binding. This reduced androgen binding with Tfm/Y mutants and blocking experiments with non-radioactive estradiol [estra-1,3,5(10)-triene-3,17beta-diol] and testosterone (17beta-hydroxy-4-androsten-3-one) indicate the existence of at least two binding components: one with high affinity only for estradiol, the other with affinity for both androgens and estrogen. Based on these properties, a receptor mechanism that detects relative concentrations of androgens and estrogens is proposed.
已在3至4周龄小鼠的下丘脑加视前区检测到雄激素和雌激素结合大分子，并对其进行了部分表征。这些成分以高亲和力结合各自的激素（在4-8 nM时达到饱和），并以推测的类固醇受体的典型速率沉降（在0.15 M NaCl中为4.0-4.5 S，无盐时为5.0-7.5 S）。在雄激素不敏感突变小鼠睾丸雌性化（Tfm）中发现雄激素结合减少90-95%，这为结合特异性提供了遗传控制。Tfm/Y突变体中雄激素结合减少以及用非放射性雌二醇[estra-1,3,5(10)-三烯-3,17β-二醇]和睾酮（17β-羟基-4-雄烯-3-酮）进行的阻断实验表明至少存在两种结合成分：一种仅对雌二醇具有高亲和力，另一种对雄激素和雌激素都具有亲和力。基于这些特性，提出了一种检测雄激素和雌激素相对浓度的受体机制。
