Androgen receptors in rat ventral prostate microsomes.
Androgen receptors in rat ventral prostate microsomes.
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大鼠腹侧前列腺微粒体中的雄激素受体。
DOI：
10.1016/0005-2736(74)90099-6
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发表时间：
1974
期刊：
影响因子：
--
通讯作者：
E. Baulieu
中科院分区：
文献类型：
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作者：
P. Robel;J. Blondeau;E. Baulieu
雄激素17β-羟基-5 α-雄甾烷-3-酮（雄甾烷酮、二氢睾酮）和5α-雄甾烷-3 β，17 β-二醇（3β-雄甾烷二醇）与成年大鼠腹侧前列腺“微粒体”（105 000× g沉积物）的单一特定成分结合。表观缔合常数为2.5±0.9 ·1010 M −1（平均值±S.E.）3β-雄甾烷酮为6.5±4.4 ·1010 M-1。结合位点的数量接近10 fmoles/mg微粒体蛋白。特异性结合被蛋白水解酶和-SH阻断剂抑制。竞争研究表明，睾酮和5α-雄甾烷-3 α，17 β-二醇是弱竞争者，而雌二醇、孕酮和皮质醇则无效。在大鼠肝微粒体中未观察到这种高亲和力结合。根据表观亲和力和类固醇特异性测定，微粒体受体似乎与先前在大鼠腹侧前列腺胞质中描述的雄激素受体不同。
The androgens 17β-hydroxy-5α-androstane-3-one (androstanolone, dihydrotestosterone) and 5α-androstane-3β,17β-diol (3β-androstanediol) bind to a single specific component of the “micrisomes” (105 000×gsediment) of adult rat ventral prostate. The apparent association constant is 2.5±0.9 · 1010M−1(mean ±S.E.) for androstanolone and 6.5±4.4 · 1010M−1for 3β-androstanediol. The number of binding sites approaches 10 fmoles/mg microsomal protiens. The specific binding is inhibited by proteolytic enzymes and-SH blocking agents. Competition studies show that testosterone and 5α-androstane-3α,17β-diol are weak competitors whereas estradiol, progesterone and cortisol are ineffective. No such high affinity binding was observed in rat liver microsomes. On the basis of apparent affinity and steroid specificity determinations, the microsomal receptor seems different from the androgen receptor previously described in rat ventral prostate cytosol.