Selective estrogen receptor modulators and coronary heart disease

Citation
Z. Bian et al., Selective estrogen receptor modulators and coronary heart disease, TREND CARD, 11(5), 2001, pp. 196-202
Citations number
75
Language
INGLESE
art.tipo
Review
Categorie Soggetti
Cardiovascular & Hematology Research
Journal title
TRENDS IN CARDIOVASCULAR MEDICINE
ISSN journal
1050-1738 → ACNP
Volume
11
Issue
5
Year of publication
2001
Pages
196 - 202
Database
ISI
SICI code
1050-1738(200107)11:5<196:SERMAC>2.0.ZU;2-D
Abstract
The vasculature has been recognized as an important target of estrogen acti on through rapid non-genomic effects and/or via the classic pathway (genomi c effects) involving estrogen receptors (ER-alpha and ER-beta). Multiple me chanisms participate in the regulation of different estrogen-controlled gen es, providing a wide spectrum of possibilities for development of drugs, in cluding pure agonists or antagonists or mixed agonists/antagonists, the so- called selective estrogen receptor modulators (SERM). In theory, an ideal S ERM should reduce the risks of coronary heart disease (CHD) and preserve bo ne density, without or with very low incidences of breast and endometrial n eoplasms or venous thromboembolism (VTE). The precise mechanism for the pro tective effects of estrogens and their receptors on cardiovascular diseases is not yet fully established. In this review, we summarize the recent adva nces in understanding the action of ERs/ligands, the therapeutic implicatio ns for CHD, and highlight the recent progress of both clinical and basic st udies on the protection issue. Finally, a number of newly developed SERMs a nd their clinical applications as well as the laboratory investigations are discussed. (C) 2001, Elsevier Science Inc.