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6α-甲基孕酮在小鼠肾脏中的受体结合

Receptor binding of 6 alpha-methylprogesterone in mouse kidney.

作者信息

Houben P W, Bullock L P

出版信息

Horm Res. 1985;21(4):261-9. doi: 10.1159/000180059.

DOI:10.1159/000180059
PMID:4007785
Abstract

6 alpha-Methylprogesterone (6MP) is an androgenic progestin that binds to the androgen receptor. However, results from an in vivo study suggested that 6MP was also bound by a second receptor. In the present study, we found that 6MP was bound in kidney cytosol from adrenalectomized/ovariectomized female mice as well as Tfm/Y mice, which lack androgen receptors. 6MP was bound with high affinity (Kd = 1.2 X 10(-8) M) by a binder that was present in 7-8 times greater concentration than the androgen receptor and had the specificity of a glucocorticoid receptor. 6MP was bound with similar specificity in liver cytosol. These data indicate that, despite its androgenic effects, 6MP binds primarily to a glucocorticoid receptor in mouse kidney.

摘要

6α-甲基孕酮(6MP)是一种与雄激素受体结合的雄激素类孕激素。然而,一项体内研究结果表明,6MP还可与另一种受体结合。在本研究中,我们发现6MP可与去肾上腺/去卵巢雌性小鼠以及缺乏雄激素受体的Tfm/Y小鼠的肾脏胞质溶胶结合。6MP与一种结合剂以高亲和力(Kd = 1.2×10⁻⁸ M)结合,该结合剂的浓度比雄激素受体高7 - 8倍,且具有糖皮质激素受体的特异性。6MP在肝脏胞质溶胶中也以类似的特异性结合。这些数据表明,尽管6MP具有雄激素作用,但它主要与小鼠肾脏中的糖皮质激素受体结合。

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