Department of Cancer and Cell Biology, University of Cincinnati, Ohio 45267-0521, USA.
Endocr Relat Cancer. 2010 Feb 25;17(2):R91-107. doi: 10.1677/ERC-09-0253. Print 2010 Jun.
Resistance to chemotherapy is a major complication in the treatment of advanced breast cancer. Estrogens and prolactin (PRL) are implicated in the pathogenesis of breast cancer but their roles in chemoresistance have been overlooked. A common feature to the two hormones is activation of their receptors by diverse compounds, which mimic or antagonize their actions. The PRL receptor is activated by lactogens (PRL, GH, or placental lactogen) originating from the pituitary, breast, adipose tissue, or the placenta. Estrogen receptors exist in multiple membrane-associated and cytoplasmic forms that can be activated by endogenous estrogens, man-made chemicals, and phytoestrogens. Here, we review evidence that low doses of PRL, estradiol (E(2)), and bisphenol A (BPA) antagonize multiple anticancer drugs that induce cell death by different mechanisms. Focusing on cisplatin, a DNA-damaging drug which is effective in the treatment of many cancer types but not breast cancer, we compare the abilities of PRL, E(2), and BPA to antagonize its cytotoxicity. Whereas PRL acts by activating the glutathione-S-transferase detoxification enzyme, E(2) and BPA act by inducing the antiapoptotic protein Bcl-2. The implications of these findings to patients undergoing chemotherapy are discussed.
化疗耐药是晚期乳腺癌治疗中的一个主要并发症。雌激素和催乳素(PRL)与乳腺癌的发病机制有关,但它们在化疗耐药中的作用被忽视了。这两种激素的一个共同特征是其受体被各种化合物激活,这些化合物模拟或拮抗它们的作用。PRL 受体被来自垂体、乳腺、脂肪组织或胎盘的催乳素(PRL、GH 或胎盘催乳素)激活。雌激素受体存在于多种膜相关和细胞质形式中,可被内源性雌激素、人工合成化学品和植物雌激素激活。在这里,我们回顾了一些证据,表明低剂量的 PRL、雌二醇(E2)和双酚 A(BPA)可以拮抗多种通过不同机制诱导细胞死亡的抗癌药物。我们以顺铂为例,顺铂是一种有效的 DNA 损伤药物,可用于治疗多种癌症,但对乳腺癌无效,我们比较了 PRL、E2 和 BPA 拮抗其细胞毒性的能力。PRL 通过激活谷胱甘肽-S-转移酶解毒酶起作用,而 E2 和 BPA 通过诱导抗凋亡蛋白 Bcl-2 起作用。这些发现对正在接受化疗的患者的意义将进行讨论。