
DOI . ORG {
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Title[redir]:
Selective estrogen receptor modulators: tissue specificity and clinica | CIA
Description:
Selective estrogen receptor modulators: tissue specificity and clinical utility Stephen Martinkovich,* Darshan Shah,* Sonia Lobo Planey, John A ArnottDepartment of Basic Sciences, The Commonwealth Medical College, Scranton, PA, USA*These authors contributed equally to this workAbstract: 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 induced by ligand binding. To date, the major clinical applications of SERMs are their use in the prevention and treatment of breast cancer, the prevention of osteoporosis, and the maintenance of beneficial serum lipid profiles in postmenopausal women. However, SERMs have also been found to promote adverse effects, including thromboembolic events and, in some cases, carcinogenesis, that have proven to be obstacles in their clinical utility. In this review, we discuss the mechanisms of SERM tissue specificity and highlight the therapeutic application of well-known and emergent SERMs.Keywords: selective estrogen receptor modulators, SERMs, estrogen receptors
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Keywords {π}
tamoxifen, cancer, estrogen, breast, receptor, effects, raloxifene, endometrial, women, treatment, phase, selective, serms, postmenopausal, erΞ±, res, bone, idoxifene, activity, cell, risk, trial, droloxifene, bazedoxifene, serm, binding, tissue, patients, cells, compared, group, osteoporosis, drug, dna, trials, chem, arzoxifene, clinical, erΞ², effect, response, study, tor, estrogens, therapy, determined, growth, results, increased, lasofoxifene,
Topics {βοΈ}
population-based case-control study raloxifene-estrogen receptor-alpha complex tamoxifen-bound estrogen receptor-alpha pre-osteoclast apoptosis lambda/laci transgenic rats dove medical press estrogen receptor/coactivator recognition selective estrogen receptor-beta estrogen receptor-selective coregulator including fast-track processing mixed agonism/antagonism profile tissue-selective estrogen complex ligand-dependent receptor conformational er-positive breast cancer manuscript login hormone receptors estrogen-alpha eralpha-agonist induced proliferation tamoxifen-complexed estrogen receptor ligand-dependent nuclear er distinct chromatin-modifying complexes histone de-acetylase activity endometrial k-ras mutations study progression-free survival ligand-induced transcriptional activation anti-estrogenic side chain selective receptor modulators specific author advanced breast cancer favored authors patient-level meta-analysis hormone-sensitive advanced shorter serum half-life tamoxifen-derived dna adducts single chloride atom cellular eralpha/erbeta ratio indole-based er ligand dna adduct-forming ability strong anti-estrogenic effects women mid-luteal phase differential time-dependent inactivation placebo-controlled crossover study nonsteroidal estrogen agonist/antagonist anti-estrogenic erΞ± complex partial estrogen-agonist properties androgen deprivation therapy bazedoxifene-conjugated estrogens combination prevent endometrial-breast cancer human estrogen receptor early breast cancer tissue-specific effects compared
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