Estrogen receptor AF-2 mutation results in antagonist reversal and reveals tissue selective function of estrogen receptor modulators
نویسندگان
چکیده
منابع مشابه
Selective Estrogen Receptor Modulators
Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive differ...
متن کاملSelective estrogen receptor modulators (SERMS).
Hormone receptors and, specifically, estrogen receptors were described about four decades ago. For estrogens, there are two receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). The two receptors are coded by different genes and their tissue expression varies across organs. ERalpha is predominantly expressed in reproductive tissues (uterus, breast, ovaries) liver and...
متن کاملSelective estrogen receptor modulators: tissue specificity and clinical utility
Selective estrogen receptor modulators (SERMs) are a diverse group of nonsteroidal compounds that function as agonists or antagonists for estrogen receptors (ERs) in a target gene-specific and tissue-specific fashion. SERM specificity involves tissue-specific expression of ER subtypes, differential expression of co-regulatory proteins in various tissues, and varying ER conformational changes in...
متن کاملSelective estrogen receptor modulators and cardiovascular events.
ost of the previous observational studies suggest that estrogen replacement therapy reduces cardiovascular risks,1 but meta-analysis of randomized clinical trials showed increased risk of hormone replacement therapy for cardiovascular events.2 Both hypercoagulability and upregulation of inflammation-sensitive proteins could underline the increased risk of estrogen treatment in coronary artery d...
متن کاملSelective estrogen receptor modulators and phytoestrogens.
Scientific achievements in the last two decades have revolutionized the treatment and prevention of breast cancer. This is mainly because of targeted therapies and a better understanding of the relationship between estrogen, its receptor, and breast cancer. One of these discoveries is the use of synthetic selective estrogen modulators (SERMs) such as tamoxifen in the treatment strategy for estr...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 2011
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.1109180108