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仓鼠皮脂腺中雄激素受体的表征及激素调控

Characterization and hormonal control of the androgen receptor in the hamster sebaceous glands.

作者信息

Bonne C, Raynaud J P

出版信息

J Invest Dermatol. 1977 Apr;68(4):215-20. doi: 10.1111/1523-1747.ep12493243.

DOI:10.1111/1523-1747.ep12493243
PMID:845456
Abstract

The costovertebral organs [CVO] and seminel vesicles [SV] of the hamster exhibit high saturable androgen uptake. The physicochemcal characteristics of the cytoplasmic androgen receptor present in these tissues have been determined and compared to those obtained in rat prostate[P]. Using the synthetic androgen R 1881 [methyltrienolone] as a radioactive ligand, it has been shown that the affinity of this compound for the cytosol CVO receptor [Kd = 0.7 +/- 0.1 nM] is similar to that for the crytosol SV receptor [Kd = 2.4 +/- 0.9 nm] in hamsters and the cytosol P receptor [Kd = 0.6 +/- 0.1 nM] in rats. The hormonal specificity of binding in these tissues is restricted to androgens. Moreover, testosterone and dihydrotestosterone have the same relative binding affinity in CVO and SV compared to R 1881. Following castration, the total number of androgen sites, as measured by an exchange assay with R 1881, decreases rapidly and parallels with a fall in lipogenic activity. Administration of an androgen rapidly restores binding capacity.

摘要

仓鼠的肋椎器官(CVO)和精囊(SV)表现出高饱和性雄激素摄取。已确定这些组织中存在的细胞质雄激素受体的物理化学特性,并与在大鼠前列腺(P)中获得的特性进行了比较。使用合成雄激素R1881(甲基三烯olone)作为放射性配体,已表明该化合物对仓鼠细胞质CVO受体(Kd = 0.7 +/- 0.1 nM)的亲和力与对仓鼠细胞质SV受体(Kd = 2.4 +/- 0.9 nM)以及对大鼠细胞质P受体(Kd = 0.6 +/- 0.1 nM)的亲和力相似。这些组织中结合的激素特异性仅限于雄激素。此外,与R1881相比,睾酮和双氢睾酮在CVO和SV中具有相同的相对结合亲和力。去势后,通过与R1881的交换测定法测量的雄激素位点总数迅速减少,且与脂肪生成活性的下降平行。给予雄激素可迅速恢复结合能力。

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