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雌激素受体配体在致病性炎症控制中的作用

Estrogen receptor ligands in the control of pathogenic inflammation.

作者信息

Harnish Douglas C

机构信息

Cardiovascular and Metabolic Disease Research, Wyeth Research, 500 Arcola Rd, Collegeville, PA 19246, USA.

出版信息

Curr Opin Investig Drugs. 2006 Nov;7(11):997-1001.

Abstract

Inflammation is recognized as a key component in a number of diseases, including rheumatoid arthritis, inflammatory bowel disease and atherosclerosis. Although well known for their classic effects on the reproductive tract and action by means of estrogen response elements in gene promoters, estrogens are also known to possess anti-inflammatory activity. This was originally highlighted with the observation that pregnancy ameliorates symptoms of rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease. Furthermore, the antagonistic cross talk between nuclear factor kappaB and estrogen receptor signaling pathways has been well documented. Recently, novel estrogen receptor ligands, pathway-selective ligands and estrogen receptor beta-selective ligands have been identified which demonstrate potent anti-inflammatory activity; these ligands are being analyzed for their therapeutic potential in pathogenic inflammation.

摘要

炎症被认为是许多疾病的关键组成部分,包括类风湿性关节炎、炎症性肠病和动脉粥样硬化。尽管雌激素以其对生殖道的经典作用以及通过基因启动子中的雌激素反应元件发挥作用而闻名,但它们也具有抗炎活性。最初这一点通过观察到怀孕可改善类风湿性关节炎、多发性硬化症和炎症性肠病的症状而得到突出体现。此外,核因子κB和雌激素受体信号通路之间的拮抗相互作用已有充分记载。最近,已鉴定出新型雌激素受体配体、途径选择性配体和雌激素受体β选择性配体,它们具有强大的抗炎活性;正在分析这些配体在致病性炎症中的治疗潜力。

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