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本文引用的文献

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Energy metabolism and fertility: a balance preserved for female health.能量代谢与生育力：女性健康的平衡点。
Nat Rev Endocrinol. 2014 Jan;10(1):13-23. doi: 10.1038/nrendo.2013.203. Epub 2013 Oct 22.
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Proteomic analysis of coregulators bound to ERα on DNA and nucleosomes reveals coregulator dynamics.蛋白质组学分析结合 ERα 的核心调节子在 DNA 和核小体上揭示了核心调节子的动态变化。
Mol Cell. 2013 Jul 25;51(2):185-99. doi: 10.1016/j.molcel.2013.06.007. Epub 2013 Jul 11.
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Regulation of estrogen receptor α N-terminus conformation and function by peptidyl prolyl isomerase Pin1.Pin1 通过调节雌激素受体 α N 端构象和功能。
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Oestrogen receptor-co-factor-chromatin specificity in the transcriptional regulation of breast cancer.雌激素受体共激活因子-染色质特异性在乳腺癌的转录调控中的作用。
EMBO J. 2011 Oct 14;30(23):4764-76. doi: 10.1038/emboj.2011.368.
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Steroid receptor coactivators 1, 2, and 3: critical regulators of nuclear receptor activity and steroid receptor modulator (SRM)-based cancer therapy.甾体激素受体共激活因子 1、2 和 3：核受体活性和甾体激素受体调节剂（SRM）为基础的癌症治疗的关键调节剂。
Mol Cell Endocrinol. 2012 Jan 30;348(2):430-9. doi: 10.1016/j.mce.2011.04.021. Epub 2011 Jun 1.
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Analysis of the human endogenous coregulator complexome.人类内源性共激活因子复合物组分析。
Cell. 2011 May 27;145(5):787-99. doi: 10.1016/j.cell.2011.05.006.
7
Effect of low-dose tamoxifen on steroid receptor coactivator 3/amplified in breast cancer 1 in normal and malignant human breast tissue.低剂量他莫昔芬对正常和恶性人乳腺组织中甾体激素受体共激活因子 3/乳腺癌扩增基因 1 的影响。
Clin Cancer Res. 2010 Apr 1;16(7):2176-86. doi: 10.1158/1078-0432.CCR-09-1859. Epub 2010 Mar 23.
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Normal and cancer-related functions of the p160 steroid receptor co-activator (SRC) family.p160类固醇受体共激活因子（SRC）家族的正常及癌症相关功能
Nat Rev Cancer. 2009 Sep;9(9):615-30. doi: 10.1038/nrc2695.
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Identification of novel ER-alpha target genes in breast cancer cells: gene- and cell-selective co-regulator recruitment at target promoters determines the response to 17beta-estradiol and tamoxifen.鉴定乳腺癌细胞中新型 ER-α 靶基因：靶启动子处基因和细胞选择性共调节因子募集决定了对 17β-雌二醇和他莫昔芬的反应。
Mol Cell Endocrinol. 2010 Jan 15;314(1):90-100. doi: 10.1016/j.mce.2009.08.008. Epub 2009 Aug 19.
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Expression of estrogen receptor co-regulators SRC-1, RIP140 and NCoR and their interaction with estrogen receptor in rat uterus, under the influence of ormeloxifene.奥美昔芬作用下大鼠子宫中雌激素受体共调节因子SRC-1、RIP140和NCoR的表达及其与雌激素受体的相互作用
J Steroid Biochem Mol Biol. 2009 Aug;116(1-2):93-101. doi: 10.1016/j.jsbmb.2009.05.006. Epub 2009 May 19.

核受体调节——共调节因子在选择性雌激素受体调节剂（SERM）作用中的角色。

Nuclear receptor modulation--role of coregulators in selective estrogen receptor modulator (SERM) actions.

作者信息

Feng Qin, O'Malley Bert W

机构信息

Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.

Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.

出版信息

Steroids. 2014 Nov;90:39-43. doi: 10.1016/j.steroids.2014.06.008. Epub 2014 Jun 16.

DOI:10.1016/j.steroids.2014.06.008
PMID:24945111
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4192004/
Abstract

Selective estrogen receptor modulators (SERMs) are a class of small-molecule chemical compounds that bind to estrogen receptor (ER) ligand binding domain (LBD) with high affinity and selectively modulate ER transcriptional activity in a cell- and tissue-dependent manner. The prototype of SERMs is tamoxifen, which has agonist activity in bone, but has antagonist activity in breast. Tamoxifen can reduce the risk of breast cancer and, at same time, prevent osteoporosis in postmenopausal women. Tamoxifen is widely prescribed for treatment and prevention of breast cancer. Mechanistically the activity of SERMs is determined by the selective recruitment of coactivators and corepressors in different cell types and tissues. Therefore, understanding the coregulator function is the key to understanding the tissue selective activity of SERMs.

摘要

选择性雌激素受体调节剂（SERMs）是一类小分子化合物，它们以高亲和力与雌激素受体（ER）配体结合域（LBD）结合，并以细胞和组织依赖性方式选择性调节ER转录活性。SERMs的原型是他莫昔芬，它在骨骼中具有激动剂活性，但在乳腺中具有拮抗剂活性。他莫昔芬可以降低乳腺癌风险，同时预防绝经后女性的骨质疏松症。他莫昔芬被广泛用于治疗和预防乳腺癌。从机制上讲，SERMs的活性取决于在不同细胞类型和组织中对共激活因子和共抑制因子的选择性募集。因此，了解共调节因子功能是理解SERMs组织选择性活性的关键。