Tanaka Kosuke, Osada Hirotaka, Murakami-Tonami Yuko, Horio Yoshitsugu, Hida Toyoaki, Sekido Yoshitaka
Division of Molecular Oncology, Aichi Cancer Center Research Institute, Nagoya, Japan; Department of Cancer Genetics, Program in Function Construction Medicine, Nagoya University Graduate School of Medicine, Nagoya, Japan; Department of Thoracic Oncology, Aichi Cancer Center Hospital, Nagoya, Japan.
Division of Molecular Oncology, Aichi Cancer Center Research Institute, Nagoya, Japan; Department of Cancer Genetics, Program in Function Construction Medicine, Nagoya University Graduate School of Medicine, Nagoya, Japan.
Cancer Lett. 2017 Jan 28;385:215-224. doi: 10.1016/j.canlet.2016.10.020. Epub 2016 Oct 20.
Malignant mesothelioma (MM) frequently exhibits Hippo signaling pathway inactivation (HPI) mainly due to NF2 and/or LATS2 mutations, which leads to the activation of YAP transcriptional co-activator. Here, we show antitumor effects of statin on MM cells with HPI, through the interplay of the mevalonate and Hippo signaling pathways. Statin attenuated proliferation and migration of MM cells harboring NF2 mutation by accelerating YAP phosphorylation/inactivation. CD44 expression was decreased by statin, in parallel with YAP phosphorylation/inactivation. Importantly, we discovered that YAP/TEAD activated CD44 transcription by binding to the CD44 promoter at TEAD-binding sites. On the other hand, CD44 regulated Merlin phosphorylation according to cell density and sequentially promoted YAP transcriptional co-activator, suggesting that CD44 plays two pivotal functional roles as an upstream suppressor of the Hippo pathway and one of downstream targets regulated by YAP/TEAD. Moreover, the YAP/CD44 axis conferred cancer stem cell (CSC)-like properties in MM cells leading to chemoresistance, which was blocked by statin. Together, our findings suggest that YAP mediates CD44 up-regulation at the transcriptional level, conferring CSC-like properties in MM cells, and statin represents a potential therapeutic option against MM by inactivating YAP.
恶性间皮瘤(MM)常表现出Hippo信号通路失活(HPI),主要是由于NF2和/或LATS2突变,这导致YAP转录共激活因子的激活。在此,我们通过甲羟戊酸途径和Hippo信号通路的相互作用,展示了他汀类药物对具有HPI的MM细胞的抗肿瘤作用。他汀类药物通过加速YAP磷酸化/失活,减弱了携带NF2突变的MM细胞的增殖和迁移。他汀类药物降低了CD44的表达,同时伴随着YAP磷酸化/失活。重要的是,我们发现YAP/TEAD通过在TEAD结合位点与CD44启动子结合来激活CD44转录。另一方面,CD44根据细胞密度调节Merlin磷酸化,并依次促进YAP转录共激活因子,这表明CD44作为Hippo通路的上游抑制因子和YAP/TEAD调节的下游靶点之一,发挥着两个关键的功能作用。此外,YAP/CD44轴赋予MM细胞癌症干细胞(CSC)样特性,导致化疗耐药,而他汀类药物可阻断这一过程。总之,我们的研究结果表明,YAP在转录水平介导CD44上调,赋予MM细胞CSC样特性,而他汀类药物通过使YAP失活,代表了一种针对MM的潜在治疗选择。