Laboratory of Molecular Neuro-Oncology, Department of Neurosurgery, School of Medicine, Emory University, Atlanta, Georgia 30322, USA.
J Clin Invest. 2012 Apr;122(4):1283-95. doi: 10.1172/JCI38596. Epub 2012 Mar 1.
Malignant gliomas are the most common and the most lethal primary brain tumors in adults. Among malignant gliomas, 60%-80% show loss of P14ARF tumor suppressor activity due to somatic alterations of the INK4A/ARF genetic locus. The tumor suppressor activity of P14ARF is in part a result of its ability to prevent the degradation of P53 by binding to and sequestering HDM2. However, the subsequent finding of P14ARF loss in conjunction with TP53 gene loss in some tumors suggests the protein may have other P53-independent tumor suppressor functions. Here, we report what we believe to be a novel tumor suppressor function for P14ARF as an inhibitor of tumor-induced angiogenesis. We found that P14ARF mediates antiangiogenic effects by upregulating expression of tissue inhibitor of metalloproteinase-3 (TIMP3) in a P53-independent fashion. Mechanistically, this regulation occurred at the gene transcription level and was controlled by HDM2-SP1 interplay, where P14ARF relieved a dominant negative interaction of HDM2 with SP1. P14ARF-induced expression of TIMP3 inhibited endothelial cell migration and vessel formation in response to angiogenic stimuli produced by cancer cells. The discovery of this angiogenesis regulatory pathway may provide new insights into P53-independent P14ARF tumor-suppressive mechanisms that have implications for the development of novel therapies directed at tumors and other diseases characterized by vascular pathology.
恶性神经胶质瘤是成年人中最常见和最致命的原发性脑肿瘤。在恶性神经胶质瘤中,由于 INK4A/ARF 基因座的体细胞改变,有 60%-80%的肿瘤表现出 P14ARF 肿瘤抑制活性丧失。P14ARF 的肿瘤抑制活性部分是由于其能够通过与 HDM2 结合并隔离 HDM2 来防止 P53 的降解。然而,随后在一些肿瘤中发现 P14ARF 缺失与 TP53 基因缺失的同时存在,表明该蛋白可能具有其他与 P53 无关的肿瘤抑制功能。在这里,我们报告了我们认为 P14ARF 的一个新的肿瘤抑制功能,作为肿瘤诱导的血管生成的抑制剂。我们发现 P14ARF 通过以 P53 非依赖性方式上调组织金属蛋白酶抑制剂 3 (TIMP3) 的表达来介导抗血管生成作用。在机制上,这种调节发生在基因转录水平上,由 HDM2-SP1 相互作用控制,其中 P14ARF 缓解了 HDM2 与 SP1 之间的显性负相互作用。P14ARF 诱导的 TIMP3 表达抑制了内皮细胞迁移和血管形成,以响应癌细胞产生的血管生成刺激。这种血管生成调节途径的发现可能为 P53 非依赖性 P14ARF 肿瘤抑制机制提供新的见解,这些机制对开发针对肿瘤和其他以血管病理学为特征的疾病的新型治疗方法具有重要意义。