雄激素受体在乳腺癌他莫昔芬耐药中的作用和机制研究进展

他莫昔芬(tamoxifen，TAM)为人工合成的非甾体类抗雌激素药物，被普遍的应用于雌激素受体(estrogen receptor，ER)阳性的乳腺癌患者中。但大约一半的ER阳性的患者会出现耐药。可见内分泌耐药是当前临床迫切需要解决的问题。随着对耐药机制的深入研究:发现雄激素受体(androgen receptor，AR)在 72.9%的原发性乳腺癌病例中表达，并在约65%的乳腺癌中与ER同时表达。有研究显示:AR/ER越高预示着TAM治疗率越低；AR与人类表皮生长因子受体2（human epidermal growth factor receptor 2，HER2）之间所形成的正反馈循环能够增加TAM耐药；AR、髓样细胞白血病-1蛋白(myeloid cell leukemia-1，Mcl-1)与TAM耐药有可能相关。所以探讨AR在TAM耐药中的作用和机制是非常有意义的。为乳腺癌的靶向治疗掀开了新的一页。

Research progress of androgen receptor in the mechanism of tamoxifen resistance in breast cancer

Tamoxifen （TAM），a synthetic non-steroidal anti-estrogen，is commonly used in patients with estrogen receptor-positive breast cancer.However，about half of ER-positive patients develop resistance.Visible endocrine resistance is the urgent need to address the current clinical issues.With an in-depth study of resistance mechanisms，androgen receptor AR was found to be expressed in 72.9% of primary breast cancer cases and concurrently with ER in about 65% of breast cancers.Some studies have shown that:A higher AR/ER indicates a lower TAM treatment rate.A positive feedback loop formed between AR and human epidermal growth factor receptor 2 (HER2) can increase TAM resistance.AR，myeloid cell leukemia-1 (Mcl-1) may be related to TAM resistance.So it is very significant to explore the role and mechanism of AR in TAM resistance.Breast cancer targeted therapy opened a new page.