摘要
他莫昔芬(tamoxifen,TAM)是治疗雌激素受体(estrogen receptor,ER)阳性乳腺癌最有效且应用时间最长的一线内分泌治疗药物,能够有效降低ER阳性乳腺癌患者的死亡率和复发率。然而,临床资料显示约50%的ER阳性乳腺癌患者对内分泌治疗显示出固有耐药,而在对TAM治疗有反应的患者中,30%-40%可发展成获得性耐药。本文从ERα36、G蛋白偶联雌激素受体(G protein-coupled estrogen receptor,GPER)、前梯度蛋白2(anterior gradient 2,AGR2)和乳腺癌扩增性抗原1(amplii ed in breast cancer 1,AIB1)这些与ERα及其信号通路有关的蛋白着眼,阐释ER阳性乳腺癌TAM耐药的机制,以期为ER阳性乳腺癌的治疗提供新思路。
Tamoxifen (TAM) has emerged as the most effective drug ancl acts as a first-line therapy in the treatment of estrogen receptor (ER)-positive breast cancer in the past four decades. Moreover, it can reduce the recurrence rate and the mortality of patients with ER-positive breast cancer. However, clinical studies have reported that approximately 50% of ER-positive breast cancer has a de novo resistance to TAM, and 30% to 40% of the remaining responsive patients will acquire resistance to TAM. This review focuses on ERα36, G protein-coupled estrogen receptor (GPER), anterior gradient 2 (AGR2) and amplified in breast cancer 1 (AIB1), which were correlated with ERa and ERa- related singal pathway, to explain the mechanism of TAM resistance and discuss their possible clinical roles.
出处
《肿瘤》
CAS
CSCD
北大核心
2015年第9期1039-1044,共6页
Tumor
基金
国家自然科学基金资助项目(编号:81271914)
浙江省科学技术厅重大科技专项重点社会发展项目(编号:2012C13019-2)
浙江省医药卫生平台计划(编号:2015RCA016)~~
关键词
乳腺肿瘤
雌激素受体阳性
他莫昔芬
耐药
Breast neoplasms
Estrogen receptor-positive
Tamoxifen
Drug resistance