摘要
雌激素受体(ER)介导了许多涉及血管炎症和粥样硬化过程中细胞和分子的有利效应。然而,也存在不利效应。实际上,绝经前女性与绝经后女性或同龄男性相比,患心血管疾病的风险显著降低,而绝经后女性与同龄绝经前女性相比心血管疾病发病率更高。ER受体亚型表达之间的平衡可能在雌激素矛盾特征(有利和有害效应)中起着重要作用。新发现的激活型雌激素受体GPR30,显示出可作为冠心病治疗靶点的潜力,但仍未清楚阐明介导GPR30功能的信号机制。本文诣在总结每个雌激素受体亚型作用的知识现状,这些受体在动脉粥样硬化炎症过程中介导不同细胞成分的直接雌激素活动。我们希望这些知识能为解释雌激素既有利又有害的矛盾特征带来曙光,并推进效益/风险比提高的特效ER激动剂和拮抗剂的研发。
关键词: 动脉粥样硬化,内皮细胞,雌激素受体α,雌激素受体β,GPR-30,血管炎症,血管平滑肌细胞。
Current Medicinal Chemistry
Title:Vascular Inflammation and Atherosclerosis: The Role of Estrogen Receptors
Volume: 22 Issue: 22
Author(s): Eva Kassi, Eliana Spilioti, Narjes Nasiri-Ansari, Christos Adamopoulos, Paraskevi Moutsatsou, Aggeliki Papapanagiotou, Gerasimos Siasos, Dimitris Tousoulis and Athanasios G. Papavassiliou
Affiliation:
关键词: 动脉粥样硬化,内皮细胞,雌激素受体α,雌激素受体β,GPR-30,血管炎症,血管平滑肌细胞。
摘要: Estrogen receptors mediate numerous favorable effects on cells and molecules implicated in vascular inflammation and atherogenic process. However, harmful effects have also been suggested. Actually, premenopausal women have a significantly lower risk for cardiovascular disease compared to postmenopausal women or age matched males while the incidence of cardiovascular disease is greater in postmenopausal than premenopausal women of the same age. The balance between the expression of ER subtypes may play an important role in the paradoxical characterization of estrogens as both beneficial and harmful. The activation of the newly discovered estrogen receptor GPR30 appears to be of great potential as therapeutic target in coronary heart disease, though the signaling mechanisms mediated GPR30 function still have not fully elucidated. The aim of this review is to summarize the current state of knowledge on the role of each estrogen receptor subtype in mediating the direct estrogen actions on different cellular components that participate in the atherosclerotic inflammatory process. We hope this knowledge will shed some light on the cause of the paradoxical characterization of estrogens as both beneficial and harmful, and advance the research in the development of specific ERagonists/ antagonists with improved benefit/risk ratio.
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Eva Kassi , Eliana Spilioti , Narjes Nasiri-Ansari , Christos Adamopoulos , Paraskevi Moutsatsou , Aggeliki Papapanagiotou , Gerasimos Siasos , Dimitris Tousoulis and Athanasios G. Papavassiliou , Vascular Inflammation and Atherosclerosis: The Role of Estrogen Receptors, Current Medicinal Chemistry 2015; 22 (22) . https://dx.doi.org/10.2174/0929867322666150608093607
DOI https://dx.doi.org/10.2174/0929867322666150608093607 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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