Razel A J, Svensson J, Spelsberg T C, Coulam C B
Am J Obstet Gynecol. 1985 Oct 15;153(4):410-6. doi: 10.1016/0002-9378(85)90079-1.
Use of glycerol and the protease inhibitor phenylmethylsulfonyl fluoride resulted in a fourfold increase in the yield of androgen receptor from human neonatal foreskin and a tenfold increase in stability of this receptor. The general physical properties of the androgen-binding component isolated from the cytosol of human neonatal foreskin were found to be consistent with those previously reported for androgen receptors. The synthetic androgen methyltrienolone (R1881) was bound with high affinity (a mean dissociation constant of 0.51 nmol/L) and low capacity (5.6 fmol/mg of protein); maximum binding required 4 hours. Affinity of the receptor was highest for R1881 followed by dihydrotestosterone, testosterone, and progesterone. 17 beta-Estradiol showed little or no competition. The receptor exhibited a change of sedimentation coefficient from 8S to 4S upon treatment with 0.1 mol/L potassium chloride. Isoelectric focusing demonstrated the existence of two molecular species with apparent isoelectric points of 7.2 and 5.7.
使用甘油和蛋白酶抑制剂苯甲基磺酰氟，可使人新生儿包皮中雄激素受体的产量提高四倍，且该受体的稳定性提高十倍。从人新生儿包皮细胞质中分离出的雄激素结合成分的一般物理性质，与先前报道的雄激素受体的性质一致。合成雄激素甲基三烯醇酮（R1881）的结合具有高亲和力（平均解离常数为0.51 nmol/L）和低容量（5.6 fmol/mg蛋白质）；最大结合需要4小时。该受体对R1881的亲和力最高，其次是二氢睾酮、睾酮和孕酮。17β-雌二醇几乎没有竞争作用。用0.1 mol/L氯化钾处理后，该受体的沉降系数从8S变为4S。等电聚焦显示存在两种分子形式，其表观等电点分别为7.2和5.7。
