Jänne O A, Bardin C W
Annu Rev Physiol. 1984;46:107-18. doi: 10.1146/annurev.ph.46.030184.000543.
Recent studies have demonstrated that androgenic stimulation of early and late responding genes depends on the nuclear uptake of the receptor-steroid complex. The longer the complex is retained in the nucleus, the shorter the lag period and the greater the magnitude of the response. Most antiandrogens or their metabolites bind to the cytosolic androgen receptor, but the relative receptor binding affinities do not strictly relate to their biological activities, since the former assay does not differentiate antagonists from weak agonists. Alternatively, androgen antagonists are believed to abrogate the action of androgenic steroids by interfering with the receptor function. However, the exact mechanisms by which antiandrogens bring about their actions remain to be established.
最近的研究表明，雄激素对早期和晚期反应基因的刺激取决于受体 - 类固醇复合物的核摄取。复合物在细胞核中保留的时间越长，滞后时间越短，反应幅度越大。大多数抗雄激素或其代谢产物与胞质雄激素受体结合，但相对受体结合亲和力并不严格与其生物学活性相关，因为前一种检测方法无法区分拮抗剂和弱激动剂。另外，雄激素拮抗剂被认为是通过干扰受体功能来消除雄激素类固醇的作用。然而，抗雄激素发挥其作用的确切机制仍有待确定。
