Karo Bio AB, Novum, SE-141 57 Huddinge, Sweden.
Nat Rev Drug Discov. 2011 Sep 16;10(10):778-92. doi: 10.1038/nrd3551.
The two oestrogen receptor subtypes α and β are hormone-regulated modulators of intracellular signalling and gene expression. Regulation of oestrogen receptor activity is crucial not only for development and homeostasis but also for the treatment of various diseases and symptoms. Classical selective oestrogen receptor modulators are well established in the treatment of breast cancer and osteoporosis, but emerging data suggest that the development of subtype-selective ligands that specifically target either oestrogen receptor-α or oestrogen receptor-β could be a more optimal approach for the treatment of cancer, cardiovascular disease, multiple sclerosis and Alzheimer's disease.
两种雌激素受体亚型 α 和 β 是激素调节的细胞内信号和基因表达的调节剂。雌激素受体活性的调节不仅对于发育和内稳态至关重要，而且对于各种疾病和症状的治疗也至关重要。经典的选择性雌激素受体调节剂在乳腺癌和骨质疏松症的治疗中得到了很好的确立，但新出现的数据表明，开发专门针对雌激素受体-α或雌激素受体-β的亚型选择性配体可能是治疗癌症、心血管疾病、多发性硬化症和阿尔茨海默病的更优化方法。
