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

被引：40

作者：

Feng, Qin ^{[1
]}

O'Malley, Bert W. ^{[1
]}

机构：

[1] Baylor Coll Med, Dept Mol & Cellular Biol, Houston, TX 77030 USA

来源：

STEROIDS | 2014年 / 90卷

关键词：

SERM; Nuclear receptor; Coregulator; HORMONE-REPLACEMENT THERAPY; BREAST-CANCER CELLS; STEROID-RECEPTOR; TAMOXIFEN RESISTANCE; ER-ALPHA; N-COR; HISTONE ACETYLTRANSFERASE; MOLECULAR DETERMINANTS; COREPRESSOR BINDING; SIGNALING PATHWAYS;

D O I：

10.1016/j.steroids.2014.06.008

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2014 Elsevier Inc. All rights reserved.

引用

页码：39 / 43

页数：5

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