Rapisarda A, Melillo G
Tumor Hypoxia Laboratory, Developmental Therapeutics Program, SAIC-Frederick, Inc., NCI at Frederick, Frederick, MD 21702, USA.
Oncogene. 2007 Oct 18;26(48):6875-84. doi: 10.1038/sj.onc.1210489. Epub 2007 May 14.
Hypoxia inducible factor 1 (HIF-1) is a key player in cancer progression and an attractive target for cancer therapy. Several small molecule inhibitors of HIF-1alpha also induce a DNA damage response. However, whether or not DNA damage is required for or associated with the inhibition of HIF-1alpha protein accumulation is poorly understood. In this report we investigated the effects of distinct DNA damaging conditions on the hypoxic induction of HIF-1alpha protein in cancer cell lines. We demonstrate that in addition to topotecan (TPT), a known inhibitor of HIF-1alpha, UVC, but not other DNA damaging agents (cisplatin, ionizing radiation and doxorubicin), inhibited HIF-1alpha protein accumulation in a dose-dependent, p53-independent fashion. Low doses UVC decreased HIF-1alpha translation without affecting global protein synthesis. Inhibition of HIF-1alpha by UVC required ongoing RNA transcription, but not DNA replication. Moreover, a functional ATR was required for the activation of DNA damage-dependent responses by both UVC and TPT, but was dispensable for the inhibition of HIF-1alpha protein. Notably, unlike TPT, inhibition of HIF-1alpha protein by UVC did not require topoisomerase I, suggesting a similar yet distinct mode of action. Our data reveal that UVC is a novel signal associated with inhibition of HIF-1alpha protein accumulation, and they uncouple the DNA damage-dependent signaling pathway exerted by UVC and TPT from HIF-1alpha inhibition.
缺氧诱导因子1(HIF-1)是癌症进展中的关键因子,也是癌症治疗的一个有吸引力的靶点。几种HIF-1α的小分子抑制剂也会诱导DNA损伤反应。然而,DNA损伤是否是抑制HIF-1α蛋白积累所必需的或与之相关,目前还知之甚少。在本报告中,我们研究了不同DNA损伤条件对癌细胞系中HIF-1α蛋白缺氧诱导的影响。我们证明,除了已知的HIF-1α抑制剂拓扑替康(TPT)外,紫外线C(UVC)而非其他DNA损伤剂(顺铂、电离辐射和阿霉素)以剂量依赖性、p53非依赖性方式抑制HIF-1α蛋白积累。低剂量UVC降低了HIF-1α的翻译,而不影响整体蛋白质合成。UVC对HIF-1α的抑制需要持续的RNA转录,但不需要DNA复制。此外,功能性的共济失调毛细血管扩张症突变基因(ATR)对于UVC和TPT激活DNA损伤依赖性反应是必需的,但对于抑制HIF-1α蛋白则是可有可无的。值得注意的是,与TPT不同,UVC对HIF-1α蛋白的抑制不需要拓扑异构酶I,这表明其作用方式相似但又不同。我们的数据表明,UVC是一种与抑制HIF-1α蛋白积累相关的新信号,并且它们将UVC和TPT所施加的DNA损伤依赖性信号通路与HIF-1α抑制作用分离开来。