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孕酮与雌激素及抗雌激素在大鼠子宫中的相互作用——受体效应

Progesterone interaction with estrogen and antiestrogen in the rat uterus--receptor effects.

作者信息

Koseki Y, Zava D T, Chamness G C, McGuire W L

出版信息

Steroids. 1977 Aug;30(2):169-77. doi: 10.1016/0039-128x(77)90079-4.

DOI:10.1016/0039-128x(77)90079-4
PMID:201053
Abstract

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.

摘要

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。

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1
Progesterone interaction with estrogen and antiestrogen in the rat uterus--receptor effects.孕酮与雌激素及抗雌激素在大鼠子宫中的相互作用——受体效应
Steroids. 1977 Aug;30(2):169-77. doi: 10.1016/0039-128x(77)90079-4.
2
Modulation of rat uterine steroid hormone receptors by estrogen and antiestrogen.雌激素和抗雌激素对大鼠子宫甾体激素受体的调节作用。
Endocrinology. 1980 Dec;107(6):2011-20. doi: 10.1210/endo-107-6-2011.
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Tamoxifen decreases the estradiol induced progesterone receptors by interfering with nuclear estrogen receptor accumulation.他莫昔芬通过干扰核雌激素受体的积累来降低雌二醇诱导的孕酮受体。
J Steroid Biochem. 1989 Jul;33(1):133-9. doi: 10.1016/0022-4731(89)90368-3.
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J Steroid Biochem. 1985 Jun;22(6):687-91. doi: 10.1016/0022-4731(85)90272-9.
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Modulation of tamoxifen-specific binding sites and estrogen receptors by estradiol and progesterone in the neonatal uterus of guinea pig.雌二醇和孕酮对豚鼠新生子宫中他莫昔芬特异性结合位点和雌激素受体的调节作用。
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Biochim Biophys Acta. 1979 Jun 1;585(1):24-33. doi: 10.1016/0304-4165(79)90321-0.
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Time-related effects of a triphenylethylene antiestrogen on estrogen-induced changes in uterine weight, estrogen receptors, and endometrial sensitivity in rats.三苯乙烯类抗雌激素对大鼠子宫重量、雌激素受体及子宫内膜敏感性的雌激素诱导变化的时间相关影响。
Contraception. 1995 Jun;51(6):367-79. doi: 10.1016/0010-7824(95)00103-h.
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Progesterone antagonizes the effects of estradiol in the fetal uterus of guinea pig.孕酮可拮抗雌二醇对豚鼠胎儿子宫的作用。
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Antiestrogen action in the uterus: biological ineffectiveness of nuclear bound estradiol after antiestrogen.抗雌激素在子宫中的作用:抗雌激素作用后核结合雌二醇的生物学无活性
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Facilitation and inhibition of the estrogen-induced luteinizing hormone surge in the rat by progesterone: effects on cytoplasmic and nuclear estrogen receptors in the hypothalamus-preoptic area, pituitary, and uterus.孕酮对大鼠雌激素诱导的促黄体生成素高峰的促进和抑制作用:对下丘脑-视前区、垂体和子宫中细胞质和细胞核雌激素受体的影响。
Endocrinology. 1981 Apr;108(4):1487-96. doi: 10.1210/endo-108-4-1487.

引用本文的文献

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Cancer Chemother Pharmacol. 1993;32(5):353-8. doi: 10.1007/BF00735918.
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A new triphenylethylene derivative, TAT-59; hormone receptors; insulin-like growth factor 1; and growth suppression of hormone-dependent MCF-7 tumors in athymic mice.一种新型三苯乙烯衍生物TAT - 59;激素受体;胰岛素样生长因子1;以及无胸腺小鼠中激素依赖性MCF - 7肿瘤的生长抑制
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Antioestrogenic derivatives of nafoxidine stimulate progesterone receptor synthesis in vivo [proceedings].
奈法唑酮的抗雌激素衍生物在体内刺激孕酮受体合成[会议论文集]
Br J Pharmacol. 1980 Jan;68(1):156P-157P.
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Steroid hormone regulation of free secretory component in the rat uterus.类固醇激素对大鼠子宫中游离分泌成分的调节作用。
Immunology. 1983 Jun;49(2):379-86.
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Metabolites of tamoxifen in animals and man: identification, pharmacology, and significance.他莫昔芬在动物和人体内的代谢产物:鉴定、药理学及意义
Breast Cancer Res Treat. 1982;2(2):123-38. doi: 10.1007/BF01806449.
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The binding of [3H]-oestradiol-17 beta in the immature rat uterus during the sequential administration of non-steroidal anti-oestrogens.在连续给予非甾体类抗雌激素药物过程中,[3H]-雌二醇-17β在未成熟大鼠子宫中的结合情况。
Br J Pharmacol. 1979 Feb;65(2):167-73. doi: 10.1111/j.1476-5381.1979.tb07815.x.