Translational Research Department, Institut Curie, Paris, France.
PLoS One. 2012;7(8):e42252. doi: 10.1371/journal.pone.0042252. Epub 2012 Aug 6.
Almost all prostate cancers respond to androgen deprivation treatment but many recur. We postulated that risk of hormone escape--frequency and delay--are influenced by hormone therapy modalities. More, hormone therapies induce crucial biological changes involving androgen receptors; some might be targets for escape prevention. We investigated the relationship between the androgen deprivation treatment and the risk of recurrence using nude mice bearing the high grade, hormone-dependent human prostate cancer xenograft PAC120. Tumor-bearing mice were treated by Luteinizing-Hormone Releasing Hormone (LHRH) antagonist alone, continuous or intermittent regimen, or combined with androgen receptor (AR) antagonists (bicalutamide or flutamide). Tumor growth was monitored. Biological changes were studied as for genomic alterations, AR mutations and protein expression in a large series of recurrent tumors according to hormone therapy modalities. Therapies targeting Her-2 or AKT were tested in combination with castration. All statistical tests were two-sided. Tumor growth was inhibited by continuous administration of the LH-RH antagonist degarelix (castration), but 40% of tumors recurred. Intermittent castration or complete blockade induced by degarelix and antiandrogens combination, inhibited tumor growth but increased the risk of recurrence (RR) as compared to continuous castration (RR(intermittent): 14.5, RR(complete blockade): 6.5 and 1.35). All recurrent tumors displayed new quantitative genetic alterations and AR mutations, whatever the treatment modalities. AR amplification was found after complete blockade. Increased expression of Her-2/neu with frequent ERK/AKT activation was detected in all variants. Combination of castration with a Her-2/neu inhibitor decreased recurrence risk (0.17) and combination with an mTOR inhibitor prevented it. Anti-hormone treatments influence risk of recurrence although tumor growth inhibition was initially similar. Recurrent tumors displayed genetic instability, AR mutations, and alterations of phosphorylation pathways. We postulated that Her-2/AKT pathways allowed salvage of tumor cells under castration and we demonstrated that their inhibition prevented tumor recurrence in our model.
几乎所有的前列腺癌对雄激素剥夺治疗有反应,但许多都会复发。我们推测,激素逃逸的风险(频率和延迟)受到激素治疗方式的影响。此外,激素治疗会诱导涉及雄激素受体的关键生物学变化;其中一些可能是预防逃逸的靶点。我们使用携带高等级、激素依赖性人前列腺癌异种移植物 PAC120 的裸鼠研究了雄激素剥夺治疗与复发风险之间的关系。荷瘤小鼠单独用促黄体激素释放激素(LHRH)拮抗剂、连续或间歇性方案治疗,或与雄激素受体(AR)拮抗剂(比卡鲁胺或氟他胺)联合治疗。监测肿瘤生长。根据激素治疗方式,研究了大量复发性肿瘤的基因组改变、AR 突变和蛋白表达的生物学变化。还测试了针对 Her-2 或 AKT 的治疗方法与去势联合应用。所有统计检验均为双侧检验。连续给予 LH-RH 拮抗剂 degarelix(去势)可抑制肿瘤生长,但 40%的肿瘤复发。与连续去势相比,间歇性去势或 degarelix 和抗雄激素联合完全阻断可抑制肿瘤生长,但增加复发风险(RR:间歇性:14.5,RR:完全阻断:6.5 和 1.35)。无论治疗方式如何,所有复发性肿瘤均显示出新的定量遗传改变和 AR 突变。完全阻断后发现 AR 扩增。所有变异体中均检测到 Her-2/neu 的表达增加和频繁的 ERK/AKT 激活。去势联合 Her-2/neu 抑制剂可降低复发风险(0.17),联合 mTOR 抑制剂可预防复发。尽管最初肿瘤生长抑制相似,但抗激素治疗会影响复发风险。复发性肿瘤显示出遗传不稳定性、AR 突变和磷酸化途径改变。我们推测,Her-2/AKT 途径允许在去势下挽救肿瘤细胞,并且我们在我们的模型中证明了抑制这些途径可预防肿瘤复发。
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