Department of Pulmonary Medicine, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kyoto, Japan.
Department of Drug Discovery Medicine, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kyoto, Japan.
Mol Cancer Ther. 2024 Feb 1;23(2):212-222. doi: 10.1158/1535-7163.MCT-23-0138.
Few treatment options exist for pleural mesothelioma (PM), which is a progressive malignant tumor. However, the efficacy of molecular-targeted monotherapy is limited, and further therapeutic strategies are warranted to treat PM. Recently, the cancer cell-cycle checkpoint inhibitors have attracted attention because they disrupt cell-cycle regulation. Here, we aimed to establish a novel combinational therapeutic strategy to inhibit the cell-cycle checkpoint kinase, ATR in PM cells. The siRNA screening assay showed that anexelekto (AXL) knockdown enhanced cell growth inhibition when exposed to ATR inhibitors, demonstrating the synergistic effects of the ATR and AXL combination in some PM cells. The AXL and ATR inhibitor combination increased cell apoptosis via the Bim protein and suppressed cell migration when compared with each monotherapy. The combined therapeutic targeting of AXL and ATR significantly delayed regrowth compared with monotherapy. Thus, optimal AXL and ATR inhibition may potentially improve the PM outcome.
针对胸膜间皮瘤(PM)这种进行性恶性肿瘤,目前的治疗选择有限。然而,分子靶向单药治疗的疗效有限,因此需要进一步的治疗策略来治疗 PM。最近,细胞周期检查点抑制剂引起了关注,因为它们破坏了细胞周期调控。在这里,我们旨在建立一种新的联合治疗策略,以抑制 PM 细胞中的细胞周期检查点激酶 ATR。siRNA 筛选试验表明,AXL 敲低可增强对 ATR 抑制剂的细胞生长抑制作用,表明在一些 PM 细胞中 ATR 和 AXL 的联合具有协同作用。与每种单药治疗相比,AXL 和 ATR 抑制剂联合治疗通过 Bim 蛋白增加细胞凋亡并抑制细胞迁移。与单药治疗相比,AXL 和 ATR 的联合治疗靶向治疗可显著延迟肿瘤再生长。因此,最佳的 AXL 和 ATR 抑制可能会改善 PM 的预后。