McCampbell A S, Mittelstadt M L, Dere R, Kim S, Zhou L, Djordjevic B, Soliman P T, Zhang Q, Wei C, Hursting S D, Lu K H, Broaddus R R, Walker C L
Institute of Biosciences and Technology, Texas A&M Health Science Center, Center for Translational Cancer Research, 2121 W. Holcombe Blvd., Houston, Texas 77030, USA.
Curr Mol Med. 2016;16(3):252-65. doi: 10.2174/1566524016666160225153307.
Endometrial carcinoma (EC) exhibits the strongest association with obesity of all cancers. Growth of these tumors is driven by PI3K/AKT activation, and opposed by tumor suppressors, including the tuberous sclerosis complex 2 (TSC-2) and p27, with inactivation of TSC2 and loss or cytoplasmic mislocalization of p27 both being linked to PI3K/AKT activation. However, little is known about the involvement of p27 in the development of EC arising in the setting of obesity, especially its role early in disease progression. Using a panel of EC cell lines, in vitro studies using PI3K inhibitors provided evidence that p27 rescue contributes to the efficacy of interventions that inhibit endometrial cell growth. In "at risk" obese patients, and in an animal model of obesity-associated EC (Tsc2-deficient Eker rats), p27 was moderately-to-severely reduced in both "normal" endometrial glands as well as in endometrial complex atypical hyperplasia (obese women), and endometrial hyperplasia (obese rats). In obese Eker rats, an energy balance intervention; caloric restriction from 2-4 months of age, reduced weight, increased adiponectin and lowered leptin to produce a favorable leptin:adiponectin ratio, and reduced circulating insulin levels. Caloric restriction also increased p27 levels, relocalized this tumor suppressor to the nucleus, and significantly decreased hyperplasia incidence. Thus, dietary and pharmacologic interventions that inhibit growth and decrease risk for development of endometrial lesions are associated with increased expression and nuclear (re)localization of p27. These data suggest that p27 levels and localization may be useful as a biomarker, and possible determinant, of risk for EC arising in the setting of obesity.
子宫内膜癌(EC)在所有癌症中与肥胖的关联最为紧密。这些肿瘤的生长由PI3K/AKT激活驱动,而受到包括结节性硬化复合物2(TSC - 2)和p27在内的肿瘤抑制因子的拮抗,TSC2的失活以及p27的缺失或细胞质异位均与PI3K/AKT激活相关。然而,关于p27在肥胖背景下发生的EC发展过程中的作用,尤其是其在疾病进展早期的作用,人们所知甚少。使用一组EC细胞系,利用PI3K抑制剂进行的体外研究表明,p27的挽救作用有助于抑制子宫内膜细胞生长的干预措施的疗效。在“高危”肥胖患者以及肥胖相关EC的动物模型(Tsc2基因缺陷的艾克大鼠)中,“正常”子宫内膜腺体以及子宫内膜复杂性非典型增生(肥胖女性)和子宫内膜增生(肥胖大鼠)中的p27均有中度至重度降低。在肥胖的艾克大鼠中,一种能量平衡干预措施:从2至4月龄开始限制热量摄入,减轻了体重,增加了脂联素并降低了瘦素水平,从而产生了有利的瘦素:脂联素比值,并降低了循环胰岛素水平。热量限制还增加了p27水平,使这种肿瘤抑制因子重新定位于细胞核,并显著降低了增生发生率。因此,抑制生长并降低子宫内膜病变发生风险的饮食和药物干预与p27表达增加及其细胞核(重新)定位有关。这些数据表明,p27的水平和定位可能作为肥胖背景下发生EC风险的生物标志物及可能的决定因素。