他莫昔芬与子宫内膜癌：一种双面性药物。
Tamoxifen and Endometrial Cancer: A Janus-Headed Drug.
作者信息
Emons Günter, Mustea Alexander, Tempfer Clemens
机构信息
Department of Obstetrics and Gynecology, Georg-August-University, 37075 Göttingen, Germany.
Department of Gynecology and Gynecological Oncology, University Hospital, 53127 Bonn, Germany.
出版信息
Cancers (Basel). 2020 Sep 7;12(9):2535. doi: 10.3390/cancers12092535.
Tamoxifen is a selective estrogen receptor modulator used for the treatment and prevention of estrogen receptor (ER)-positive breast cancer. However, tamoxifen increases the risk of endometrial cancer (EC) by about 2-7 fold, and more aggressive types of EC with poor prognoses are observed in tamoxifen users. On the other hand, tamoxifen is an efficacious treatment for advanced or recurrent EC with low toxicity. The differential agonistic or antagonistic effects of tamoxifen on ERα are explained by the tissue-specific expression profiles of co-activators and co-repressors of the receptor. The estrogen-agonistic effect of tamoxifen in endometrial cancers can also be explained by the expression of G-protein coupled estrogen receptor 1 (GPER-1), a membrane-bound estrogen receptor for which tamoxifen and other "antiestrogens" are pure agonists.
他莫昔芬是一种选择性雌激素受体调节剂，用于治疗和预防雌激素受体（ER）阳性乳腺癌。然而，他莫昔芬会使子宫内膜癌（EC）的风险增加约2至7倍，并且在服用他莫昔芬的患者中观察到更具侵袭性、预后较差的子宫内膜癌类型。另一方面，他莫昔芬是一种治疗晚期或复发性子宫内膜癌的有效药物，且毒性较低。他莫昔芬对ERα的差异激动或拮抗作用可通过该受体共激活剂和共抑制剂的组织特异性表达谱来解释。他莫昔芬在子宫内膜癌中的雌激素激动作用也可以通过G蛋白偶联雌激素受体1（GPER-1）的表达来解释，GPER-1是一种膜结合雌激素受体，他莫昔芬和其他“抗雌激素”对其是纯激动剂。
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