Nilsson S, Kuiper G, Gustafsson J A
Karo Bio AB, Huddinge, Sweden.
Trends Endocrinol Metab. 1998 Dec;9(10):387-95. doi: 10.1016/s1043-2760(98)00096-4.
There is increasing interest in developing better drugs for improving the health of women. Because of the multiple target organs for estrogens and the occurrence of both beneficial and unwanted effects during treatment, the key to improvement in drug therapy is the development of estrogen receptor modulators with better tissue selectivity. The recent discovery that there are not one but two estrogen receptors, ERalpha and ERbeta, each with its unique tissue distribution and with differing and sometimes opposing actions on certain genes, promises new hope for the development of novel, tissue-selective estrogens. Our present knowledge of the tissue distribution of ERalpha and ERbeta suggests that development of selective therapies for treatment and/or prevention of menopausal symptoms, osteoporosis, cardiovascular disease, type II diabetes, Alzheimer's disease and urinary incontinence is an achievable goal in the foreseeable future. Furthermore, it is possible that future estrogen therapy might be beneficial for men.
研发更有效的药物以改善女性健康正引发越来越多的关注。由于雌激素作用于多个靶器官,且治疗过程中会出现有益和不良两种效应,改善药物治疗的关键在于研发具有更好组织选择性的雌激素受体调节剂。最近发现存在两种而非一种雌激素受体,即ERα和ERβ,它们各自具有独特的组织分布,对某些基因有着不同乃至有时相反的作用,这为新型组织选择性雌激素的研发带来了新希望。我们目前对ERα和ERβ组织分布的了解表明,在可预见的未来,开发用于治疗和/或预防更年期症状、骨质疏松症、心血管疾病、II型糖尿病、阿尔茨海默病和尿失禁的选择性疗法是一个可以实现的目标。此外,未来雌激素疗法对男性可能也有益处。