期刊
STEROIDS
卷 90, 期 -, 页码 39-43出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.steroids.2014.06.008
关键词
SERM; Nuclear receptor; Coregulator
资金
- NICHD NIH HHS [R01 HD007857, R01 HD008188] Funding Source: Medline
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.
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