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.
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。
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