Department of Oncology, Cross Cancer Institute and University of Alberta, 11560 University Avenue, Edmonton, AB, Canada T6G 1Z2.
Neuro Oncol. 2010 Aug;12(8):822-33. doi: 10.1093/neuonc/noq017. Epub 2010 Feb 23.
Angiogenesis inhibitors, such as sunitinib, represent a promising strategy to improve glioblastoma (GBM) tumor response. In this study, we used the O(6)-methylguanine methyltransferase (MGMT)-negative GBM cell line U87MG stably transfected with MGMT (U87/MGMT) to assess whether MGMT expression affects the response to sunitinib. We showed that the addition of sunitinib to standard therapy (temozolomide [TMZ] and radiation therapy [RT]) significantly improved the response of MGMT-positive but not of MGMT-negative cells. Gene expression profiling revealed alterations in the angiogenic profile, as well as differential expression of several receptor tyrosine kinases targeted by sunitinib. MGMT-positive cells displayed higher levels of vascular endothelial growth factor receptor 1 (VEGFR-1) compared with U87/EV cells, whereas they displayed decreased levels of VEGFR-2. Depleting MGMT using O(6)-benzylguanine suggested that the expression of these receptors was directly related to the MGMT status. Also, we showed that MGMT expression was associated with a dramatic increase in the soluble VEGFR-1/VEGFA ratio, thereby suggesting a decrease in bioactive VEGFA and a shift towards an antiangiogenic profile. The reduced angiogenic potential of MGMT-positive cells is supported by: (i) the decreased ability of their secreted factors to induce endothelial tube formation in vitro and (ii) their low tumorigenicity in vivo compared with the MGMT-negative cells. Our study is the first to show a direct link between MGMT expression and decreased angiogenicity and tumorigenicity of GBM cells and suggests the combination of sunitinib and standard therapy as an alternative strategy for GBM patients with MGMT-positive tumors.
血管生成抑制剂,如舒尼替尼,代表了一种改善胶质母细胞瘤(GBM)肿瘤反应的有前途的策略。在这项研究中,我们使用 O(6)-甲基鸟嘌呤甲基转移酶(MGMT)阴性 GBM 细胞系 U87MG 稳定转染 MGMT(U87/MGMT)来评估 MGMT 表达是否影响对舒尼替尼的反应。我们表明,舒尼替尼联合标准治疗(替莫唑胺[TMZ]和放射治疗[RT])显著改善了 MGMT 阳性细胞的反应,但对 MGMT 阴性细胞没有影响。基因表达谱分析显示,血管生成谱发生了改变,以及几种受体酪氨酸激酶的表达发生了差异,这些激酶是舒尼替尼的作用靶点。MGMT 阳性细胞与 U87/EV 细胞相比,血管内皮生长因子受体 1(VEGFR-1)的水平更高,而 VEGFR-2 的水平则较低。用 O(6)-苯甲基鸟嘌呤(O(6)-benzylguanine)耗尽 MGMT 表明,这些受体的表达与 MGMT 状态直接相关。此外,我们还表明,MGMT 表达与可溶性 VEGFR-1/VEGFA 比值的急剧增加有关,这表明生物活性 VEGFA 减少,血管生成谱向抗血管生成方向转变。MGMT 阳性细胞的血管生成潜力降低得到以下支持:(i)其分泌因子在体外诱导内皮管形成的能力降低,以及(ii)与 MGMT 阴性细胞相比,其在体内的致瘤性降低。我们的研究首次表明,MGMT 表达与 GBM 细胞的血管生成和致瘤性降低之间存在直接联系,并表明舒尼替尼联合标准治疗作为 MGMT 阳性肿瘤患者的替代策略。