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

Q Feng, BW O'Malley - Steroids, 2014 - Elsevier
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 …