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雌激素和抗雌激素对雌激素受体活性的调节

Modulation of oestrogen receptor activity by oestrogens and anti-oestrogens.

作者信息

Green S

机构信息

Imperial Chemical Industries, Central Toxicology Laboratory, Macclesfield, Cheshire, England.

出版信息

J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):747-51. doi: 10.1016/0960-0760(90)90415-h.

DOI:10.1016/0960-0760(90)90415-h
PMID:2285586
Abstract

The oestrogen receptor is a member of a supergene family that includes receptors for steroid and thyroid hormones, vitamin D3, and retinoic acid. A number of additional members of the family have been cloned where the putative ligand remains to be identified. The oestrogen receptor is a ligand-activated transcription factor that modulates specific gene expression by binding to short DNA sequences (oestrogen response elements) located in the vicinity of oestrogen-regulated genes. Regions of the receptor responsible for hormone-binding. DNA-binding and activation of transcription, have been identified. The anti-oestrogen, tamoxifen (Nolvadex), behaves as a weak oestrogen agonist. A model, based upon our current understanding of the molecular mechanism of oestrogen action, will be presented to explain the cell and gene specific effects of some anti-oestrogens.

摘要

雌激素受体是一个超基因家族的成员,该家族包括类固醇和甲状腺激素、维生素D3及视黄酸的受体。该家族的许多其他成员已被克隆,但推定的配体仍有待确定。雌激素受体是一种配体激活的转录因子,通过与位于雌激素调节基因附近的短DNA序列(雌激素反应元件)结合来调节特定基因的表达。已确定了受体中负责激素结合、DNA结合及转录激活的区域。抗雌激素药物他莫昔芬(诺瓦得士)表现为一种弱雌激素激动剂。将基于我们目前对雌激素作用分子机制的理解提出一个模型,以解释某些抗雌激素药物对细胞和基因的特异性作用。

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Modulation of oestrogen receptor activity by oestrogens and anti-oestrogens.雌激素和抗雌激素对雌激素受体活性的调节
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[The elucidation of the antiestrogen and antitumoral mechanisms of tamoxifen].
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Mol Endocrinol. 1996 Mar;10(3):230-42. doi: 10.1210/mend.10.3.8833652.

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BMC Cell Biol. 2008 Jul 24;9:41. doi: 10.1186/1471-2121-9-41.
2
A case of painless thyroiditis possibly triggered by tamoxifen citrate, a synthetic antiestrogen.
J Endocrinol Invest. 1998 Jan;21(1):70-1. doi: 10.1007/BF03347290.
3
Fourteenth Gaddum Memorial Lecture. A current view of tamoxifen for the treatment and prevention of breast cancer.第十四届加德姆纪念讲座。他莫昔芬治疗和预防乳腺癌的现状
Br J Pharmacol. 1993 Oct;110(2):507-17. doi: 10.1111/j.1476-5381.1993.tb13840.x.
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Stimulation of erythropoiesis by the non-steroidal anti-androgen nilutamide in men with prostate cancer: evidence for an agonistic effect?非甾体类抗雄激素尼鲁米特对前列腺癌男性患者红细胞生成的刺激作用:存在激动效应的证据?
Br J Cancer. 1994 Mar;69(3):617-9. doi: 10.1038/bjc.1994.115.
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Combined effects of 1,25-dihydroxyvitamin D3 and tamoxifen on the growth of MCF-7 and ZR-75-1 human breast cancer cells.
Breast Cancer Res Treat. 1994 Feb;29(2):161-8. doi: 10.1007/BF00665677.