Selective estrogen receptor modulation

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Selective estrogen receptor modulation: a personal perspective.

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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...

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Estrogen, selective estrogen receptor modulation, and coronary heart disease: something or nothing.

In terms of lifetime risk, one in three women will die of heart disease and one in six of stroke; in contrast, one in nine women will develop breast carcinoma, and only one in 25 will eventually die of it (1). It is, therefore, clear that a successful therapeutic intervention to improve death rates for coronary heart disease (CHD), however modest, will have a disproportionately large benefit on...

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Selective 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...

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Selective Estrogen Receptor Down-Regulator and Selective Estrogen Receptor Modulators Differentially Regulate Lactotroph Proliferation

BACKGROUND We recently reported that estrogen receptor alpha (ERalpha), even in absence of estrogen (E2), plays a critical role in lactotroph homeostasis. The anti-estrogen ICI 182780 (ICI), but not tamoxifen or raloxifene, rapidly promoted the degradation of ERalpha, and inhibited cell proliferation. However, all three ER antagonists suppressed PRL release, suggesting that receptor occupation ...

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ژورنال

عنوان ژورنال: Cancer Cell

سال: 2004

ISSN: 1535-6108

DOI: 10.1016/s1535-6108(04)00059-5