摘要
抗雌激素疗法是雌激素受体依赖型乳腺癌内分泌疗法的重要手段之一。抗雌激素药物主要包括选择性雌激素受体调节剂(SERMs)和纯抗雌激素剂。SERMs有三苯乙烯类、苯并噻吩类、萘类、苯并吡喃类、吲哚类等类型,纯抗雌激素剂有甾体类和非甾体类。芳构化酶抑制剂通过抵抗雌激素生成显示类似抗雌激素疗效。抗雌激素药物主要通过消除雌激素与雌激素受体的相互作用促使癌细胞凋亡。现综述抗雌激素药物和芳构化酶抑制剂的作用机制、作用特点及最新研究进展。
Antiestrogens have proven to be highly effective in the treatment of estrogen receptordependent breast cancer. Two major types of antiestrogenic agents are structurally categorized as selective estrogen receptor modulators （SERMs） and pure antiestrogens. The former includes triphenylethylenes, benzothiophenes, naphthalenes, benzopyrans, indoles, and the latter consists of both steroidal and nonsteroidal compounds. Aromatase inhibitors play a mimic anti-estrogenic role by suppressing the biosynthesis of endogenous estrogen. Antiestrogens function the apoptosis of cancer cells by preventing estrogen from activating estrogen receptors. This review details the mechanisms, effects and research advances of antiestrogens and aromatase inhibitors.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2006年第13期1051-1057,共7页
Chinese Journal of New Drugs
