Preclinical characterization of selective estrogen receptor beta agonists: new insights into their therapeutic potential.

H A Harris
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引用次数: 26

Abstract

It has now been over 10 years since Jan-Ake Gustafsson revealed the existence of a second form of the estrogen receptor (ERbeta) at a 1996 Keystone Symposium. Since then, substantial success has been made in distinguishing its potential biological functions from the previously known form (now called ERalpha) and how it might be exploited as a drug target. Subtype selective agonists have been particularly useful in this regard and suggest that ERbeta agonists may be useful for a variety of clinical applications without triggering classic estrogenic side effects such as uterine stimulation. These applications include inflammatory bowel disease, rheumatoid arthritis, endometriosis, and sepsis. This manuscript will summarize illustrative data for three ERbeta selective agonists, ERB-041, WAY-202196, and WAY-200070.

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选择性雌激素受体激动剂的临床前特征:对其治疗潜力的新见解。
自从Jan-Ake Gustafsson在1996年的Keystone研讨会上揭示了第二种雌激素受体(ERbeta)的存在以来,已经过去了10多年。从那时起,在将其潜在的生物学功能与以前已知的形式(现在称为erα)区分开来以及如何将其作为药物靶点加以利用方面取得了重大成功。亚型选择性激动剂在这方面特别有用,这表明erβ激动剂可用于各种临床应用,而不会引发经典的雌激素副作用,如子宫刺激。这些应用包括炎症性肠病、类风湿性关节炎、子宫内膜异位症和败血症。本文将总结三种erβ选择性激动剂,ERB-041, WAY-202196和WAY-200070的说明性数据。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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