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Cancer Prev Res (Phila). 2014 Jan;7(1):169-78. doi: 10.1158/1940-6207.CAPR-13-0299. Epub 2013 Nov 26.
Mutation of a single copy of the adenomatous polyposis coli (APC) gene results in familial adenomatous polyposis (FAP), which confers an extremely high risk for colon cancer. Apc(Min/+) mice exhibit multiple intestinal neoplasia (MIN) that causes anemia and death from bleeding by 6 months. Mechanistic target of rapamycin complex 1 (mTORC1) inhibitors were shown to improve Apc(Min/+) mouse survival when administered by oral gavage or added directly to the chow, but these mice still died from neoplasia well short of a natural life span. The National Institute of Aging Intervention Testing Program showed that enterically targeted rapamycin (eRapa) extended life span for wild-type genetically heterogeneous mice in part by inhibiting age-associated cancer. We hypothesized that eRapa would be effective in preventing neoplasia and extend survival of Apc(Min/+) mice. We show that eRapa improved survival of Apc(Min/+) mice in a dose-dependent manner. Remarkably, and in contrast to previous reports, most of the Apc(Min/+) mice fed 42 parts per million eRapa lived beyond the median life span reported for wild-type syngeneic mice. Furthermore, chronic eRapa did not cause detrimental immune effects in mouse models of cancer, infection, or autoimmunity, thus assuaging concerns that chronic rapamycin treatment suppresses immunity. Our studies suggest that a novel formulation (enteric targeting) of a well-known and widely used drug (rapamycin) can dramatically improve its efficacy in targeted settings. eRapa or other mTORC1 inhibitors could serve as effective cancer preventatives for people with FAP without suppressing the immune system, thus reducing the dependency on surgery as standard therapy.
单个腺瘤性结肠息肉病(APC)基因突变会导致家族性腺瘤性息肉病(FAP),从而使结肠癌的风险极高。Apc(Min/ +)小鼠表现出多发性肠肿瘤(MIN),这会导致贫血,并在 6 个月内因出血而死亡。已显示雷帕霉素靶蛋白复合物 1(mTORC1)抑制剂通过口服灌胃或直接添加到饲料中给药可改善 Apc(Min/ +)小鼠的存活,但这些小鼠仍因肿瘤而死亡,远远未达到自然寿命。美国国立衰老研究所干预测试计划表明,肠靶向雷帕霉素(eRapa)通过抑制与年龄相关的癌症,部分延长了遗传异质性野生型小鼠的寿命。我们假设 eRapa 将有效预防肿瘤并延长 Apc(Min/ +)小鼠的存活。我们表明,eRapa 以剂量依赖性方式改善了 Apc(Min/ +)小鼠的存活。值得注意的是,与以前的报告相反,大多数喂食 42 百万分率 eRapa 的 Apc(Min/ +)小鼠的存活时间超过了与野生型同基因小鼠报告的中位寿命。此外,慢性 eRapa 不会在癌症、感染或自身免疫的小鼠模型中引起有害的免疫效应,从而消除了人们对慢性雷帕霉素治疗抑制免疫的担忧。我们的研究表明,一种新型制剂(肠靶向)的已知且广泛使用的药物(雷帕霉素)可以在靶向治疗中显著提高其疗效。eRapa 或其他 mTORC1 抑制剂可以作为 FAP 患者的有效癌症预防药物,而不会抑制免疫系统,从而减少对手术作为标准治疗的依赖。