In vitro and in vivo binding of progestins to the androgen receptor of mouse kidney: correlation with biological activities.
In vitro and in vivo binding of progestins to the androgen receptor of mouse kidney: correlation with biological activities.
复制标题
孕激素与小鼠肾脏雄激素受体的体外和体内结合：与生物活性的相关性。
作者：
T. Brown;L. Bullock;C. Bardin
孕激素对雄激素反应组织具有促雄激素、抗雄激素和促联雄激素活性。最近的几项研究表明，这些行动中的一些或全部可能是通过与雄激素受体的相互作用在小鼠肾脏中启动。所研究的所有孕激素，包括醋酸甲羟孕酮[6 α-甲基-17 α-羟基-孕甾-4-烯-3，20-二酮醋酸酯（MPA）]、醋酸环丙孕酮[6-氯-17 α-羟基-la，2a-亚甲基-孕甾-4，6-二烯-3，20-二酮醋酸酯（CPA）]、6 α-甲基孕酮（6 MP）和孕酮（P），有效地与[3 H]睾酮（[3 H]T）竞争小鼠肾胞质溶胶中雄激素受体上的结合位点。它们的相对结合亲和力为T>> 6 MP> CPA > MPA = P，表明MPA（最具生物学效力的雄激素类雄激素）与细胞质雄激素受体的结合亲和力低于6 MP或抗雄激素类雄激素CPA。为了进一步研究结合亲和力和孕激素的生物活性之间的关系，一种测定使用。
Progestins possess androgenic, antiandrogenic, and synandrogenic activities on androgen-responsive tissues. Several recent studies suggest that some or all of these actions may be initiated in mouse kidney via progestin interaction with the androgen receptor. All of the progestins studied, including medroxyprogesterone acetate [6a-methyl-17a-hydroxy-pregn-4-ene-3,20-dione acetate (MPA)], cyproterone acetate [6-chloro-17a-hydroxy-la,2a-methylene-pregna-4,6-diene-3,20-dione acetate (CPA)], 6a-methylprogesterone (6MP), and progesterone(P), effectively competed with [3H]testosterone ([3H]T) for binding sites on androgen receptors in mouse kidney cytosol. Their relative binding affinities were T » 6MP > CPA > MPA = P, indicating that MPA, the most biologically potent androgenic progestin, bound to the cytoplasmic androgen receptor with less affinity than 6MP or the antiandrogenic progestin CPA. To further investigate the relationship between binding affinity and biological activity of progestins, an assay usin...