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儿茶酚雌激素与雌三醇(1,3,5(10)-雌三烯-3,15α,16α,17β-四醇)的子宫雌激素受体结合

Uterine estrogen receptor binding of catecholestrogens and of estetrol (1,3,5(10)-estratriene-3,15alpha,16alpha,17beta-tetrol).

作者信息

Martucci C, Fishman J

出版信息

Steroids. 1976 Mar;27(3):325-33. doi: 10.1016/0039-128x(76)90054-4.

DOI:10.1016/0039-128x(76)90054-4
PMID:178074
Abstract

The binding affinities for the catecholestrogen metabolites of estradiol and of their methyl ethers for the rat uterine cytosol estrogen receptors were examined. Similarly the binding of the fetal estradiol metabolite, 15alpha-hydroxyestriol (estertrol) was also measured. All of the catecholestrogens showed binding affinities far in excess of their uterotrophic potency. This is different from estriol, the product of the alternative metabolic pathways and suggests that the direction of estradiol metabolism may have an important role in the modulation of estrogenic activity of the female sex hormone.

摘要

研究了雌二醇及其甲基醚的儿茶酚雌激素代谢物与大鼠子宫胞质溶胶雌激素受体的结合亲和力。同样,也测定了胎儿雌二醇代谢物15α-羟基雌三醇(依斯特罗)的结合情况。所有儿茶酚雌激素显示出的结合亲和力远远超过其子宫营养效能。这与替代代谢途径的产物雌三醇不同,表明雌二醇代谢方向可能在调节女性性激素的雌激素活性中起重要作用。

相似文献

1
Uterine estrogen receptor binding of catecholestrogens and of estetrol (1,3,5(10)-estratriene-3,15alpha,16alpha,17beta-tetrol).儿茶酚雌激素与雌三醇(1,3,5(10)-雌三烯-3,15α,16α,17β-四醇)的子宫雌激素受体结合
Steroids. 1976 Mar;27(3):325-33. doi: 10.1016/0039-128x(76)90054-4.
2
Precursor role of 15alpha-hydroxyestradiol and 15alpha-hydroxyandrostenedione in the formation of estetrol.15α-羟基雌二醇和15α-羟基雄烯二酮在雌三醇形成中的前体作用。
Can J Biochem. 1978 Feb;56(2):101-6. doi: 10.1139/o78-016.
3
Direction of estradiol metabolism as a control of its hormonal action--uterotrophic activity of estradiol metabolites.雌二醇代谢方向作为其激素作用的调控——雌二醇代谢产物的子宫营养活性
Endocrinology. 1977 Dec;101(6):1709-15. doi: 10.1210/endo-101-6-1709.
4
Competition of estetrol and ethynylestradiol with estradiol for nuclear binding in human endometrium.雌三醇和乙炔雌二醇与雌二醇在人子宫内膜中对核结合的竞争。
J Steroid Biochem. 1976 Oct;7(10):817-22. doi: 10.1016/0022-4731(76)90184-9.
5
Comparison of effects of estertrol and tamoxifen with those of estriol and estradiol on the immature rat uterus.
Biol Reprod. 1980 May;22(4):913-26. doi: 10.1095/biolreprod22.4.913.
6
Heterogeneity of saturable estradiol binding sites in nuclei of human endometrium. Estetrol studies.人子宫内膜细胞核中可饱和雌二醇结合位点的异质性。雌三醇研究。
J Steroid Biochem. 1978 Dec;9(12):1145-8. doi: 10.1016/0022-4731(78)90003-1.
7
Comparative properties of the catechol estrogens, I: methylation by catechol-O-methyltransferase and binding to cytosol estrogen receptors.儿茶酚雌激素的比较特性,I:儿茶酚-O-甲基转移酶介导的甲基化作用及与胞质雌激素受体的结合
Steroids. 1980 Jul;36(1):1-11. doi: 10.1016/0039-128x(80)90062-8.
8
15- and 16-hydroxylations of androgens and estrogens in the human fetal liver: a critical step in estetrol biosynthesis.人胎儿肝脏中雄激素和雌激素的15-和16-羟基化:雌三醇生物合成的关键步骤。
J Steroid Biochem. 1985 Feb;22(2):195-201. doi: 10.1016/0022-4731(85)90112-8.
9
Temporal relationships between hormone receptor binding and biological responses in the uterus: studies with short- and long-acting derivatives of estriol.子宫中激素受体结合与生物学反应之间的时间关系:使用雌三醇短效和长效衍生物的研究。
Endocrinology. 1976 Jan;98(1):220-7. doi: 10.1210/endo-98-1-220.
10
[16-alpha-heterosubstituted estradiols (estradiol analogs). Preparation and binding power at receptors of rat uterus in vitro].[16-α-杂取代雌二醇(雌二醇类似物)。体外制备及其对大鼠子宫受体的结合力]
Pharmazie. 1975 Jan;30(1):32-4.

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Altered drug metabolism during pregnancy: hormonal regulation of drug-metabolizing enzymes.
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Estradiol-17beta and its cytochrome P450- and catechol-O-methyltransferase-derived metabolites stimulate proliferation in uterine artery endothelial cells: role of estrogen receptor-alpha versus estrogen receptor-beta.雌二醇-17β及其细胞色素 P450 和儿茶酚-O-甲基转移酶衍生代谢物刺激子宫动脉内皮细胞增殖:雌激素受体-α与雌激素受体-β的作用。
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Invest New Drugs. 2007 Feb;25(1):41-8. doi: 10.1007/s10637-006-9008-5. Epub 2006 Sep 13.
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Synthesis and evaluation of catechol analogs of diethylstilbestrol on a hormone-dependent human mammary carcinoma implanted in nude mice.己烯雌酚儿茶酚类似物在裸鼠体内移植的激素依赖性人乳腺癌上的合成与评价
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