Koseki Y, Zava D T, Chamness G C, McGuire W L
Steroids. 1977 Aug;30(2):169-77. doi: 10.1016/0039-128x(77)90079-4.
Daily injections of estradiol or the antiestrogen tamoxifen initially stimulate uterine weight increase and progesterone receptor synthesis, though continued tamoxifen fails to maintain the increased weight. The stimulatory actions of both estradiol and tamoxifen are inhibited or reversed by a single injection of progesterone. It has been hypothesized that progesterone antagonizes estrogen action by reducing estrogen receptor levels, but in the present experiments neither cytoplasmic nor nuclear estrogen receptor was affected. We conclude that progesterone acts at a point beyond estrogen receptor availability or translocation to antagonize estrogen action.
每日注射雌二醇或抗雌激素他莫昔芬最初会刺激子宫重量增加和孕酮受体合成,不过持续使用他莫昔芬无法维持增加的重量。单次注射孕酮可抑制或逆转雌二醇和他莫昔芬的刺激作用。据推测,孕酮通过降低雌激素受体水平来拮抗雌激素作用,但在本实验中,细胞质和细胞核中的雌激素受体均未受到影响。我们得出结论,孕酮在雌激素受体可用性或易位之外的某个点起作用,以拮抗雌激素作用。