雌激素受体和选择性雌激素受体调节剂的研究进展

Research progress in estrogen receptor and selective estrogen receptor modulators

雌激素受体属于核受体超家族成员,是一类重要的核转录因子,它在生殖系统、骨组织、心血管和中枢神经系统中发挥着重要的生理作用,是治疗骨质疏松和乳腺癌的重要药物作用靶标。已知的雌激素受体有α和β两种亚型,它们由两个不同的基因编码组成。选择性雌激素受体调节剂是一类在不同的组织细胞中对雌激素受体发挥不同调节作用的化合物,用于治疗绝经后妇女的骨质疏松和乳腺癌等。对近年来有关这两方面的研究情况进行综述。

Estrogen receptor （ER）, an important transcription factor belonging to the nuclear receptor superfamily, plays a key role in reproductive, cardiovascular and central nervous systems and bone tissue. Thus, it is a key drug target for the treatment of osteoporosis and breast cancer. ER comprises two subtypes ERa and ER β, which encoded by two distinct genes. Selective estrogen receptor modulators （SERMs） are kinds of compounds that exert different biological effects on ER in different tissues and can be used in the treatment of osteoporosis and breast cancer of postmenopausal women.