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

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

Author information

1
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.
2
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA. Electronic address: berto@bcm.edu.

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.

KEYWORDS:

Coregulator; Nuclear receptor; SERM

PMID:
24945111
PMCID:
PMC4192004
DOI:
10.1016/j.steroids.2014.06.008
[Indexed for MEDLINE]
Free PMC Article

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