Chorzalska Anna, Kim Javier Flores, Roder Karim, Tepper Alexander, Ahsan Nagib, Rao R Shyama Prasad, Olszewski Adam J, Yu Xiaoqing, Terentyev Dmitry, Morgan John, Treaba Diana O, Zhao Ting C, Liang Olin, Gruppuso Philip A, Dubielecka Patrycja M
1 Signal Transduction Laboratory, Division of Hematology/Oncology, Department of Medicine, Rhode Island Hospital, Warren Alpert Medical School, Brown University , Providence, Rhode Island.
2 Division of Cardiology, Rhode Island Hospital, Warren Alpert Medical School, Brown University , Providence, Rhode Island.
Stem Cells Dev. 2017 May 1;26(9):656-677. doi: 10.1089/scd.2016.0262. Epub 2017 Feb 27.
Despite the success of tyrosine kinase inhibitor (TKI) therapy in chronic myelogenous leukemia (CML), leukemic stem/progenitor cells remain detectable even in the state of deep molecular remission. Mechanisms that allow them to persist despite continued kinase inhibition remain unclear. We have previously shown that prolonged exposure to imatinib mesylate (IM) results in dysregulation of Akt/Erk 1/2 signaling, upregulation of miR-181a, enhanced adhesiveness, and resistance to high IM. To characterize the molecular basis and reversibility of those effects, we applied gene and protein expression analysis, quantitative phosphoproteomics, and direct miR-181a inhibition to our cellular model of CML cells subjected to prolonged exposure to IM. Those cells demonstrated upregulation of pluripotency markers (SOX2, SALL4) and adhesion receptors (CD44, VLA-4, CXCR4), as well as downregulation of Hippo signaling and upregulation of transcription coactivator YAP. Furthermore, inhibition of miR-181a using a microRNA sponge inhibitor resulted in decreased transcription of SOX2 and SALL4, decreased activation of YAP, and increased sensitivity to IM. Our findings indicate that long-term exposure to IM results in dysregulation of stem cell renewal-regulatory Hippo/YAP signaling, acquisition of expression of stem cell markers and that experimental interference with YAP activity may help to restore chemosensitivity to TKI.
尽管酪氨酸激酶抑制剂(TKI)疗法在慢性粒细胞白血病(CML)治疗中取得了成功,但即使在深度分子缓解状态下,白血病干/祖细胞仍可被检测到。尽管持续抑制激酶,这些细胞仍能持续存在的机制尚不清楚。我们之前已经表明,长时间暴露于甲磺酸伊马替尼(IM)会导致Akt/Erk 1/2信号失调、miR-181a上调、黏附性增强以及对高剂量IM产生抗性。为了表征这些效应的分子基础和可逆性,我们对长时间暴露于IM的CML细胞的细胞模型进行了基因和蛋白质表达分析、定量磷酸化蛋白质组学以及直接抑制miR-181a。这些细胞表现出多能性标志物(SOX2、SALL4)和黏附受体(CD44、VLA-4、CXCR4)上调,以及Hippo信号下调和转录共激活因子YAP上调。此外,使用微小RNA海绵抑制剂抑制miR-181a导致SOX2和SALL4转录减少、YAP激活降低以及对IM的敏感性增加。我们的研究结果表明,长期暴露于IM会导致干细胞更新调节性Hippo/YAP信号失调,获得干细胞标志物表达,并且对YAP活性的实验性干扰可能有助于恢复对TKI的化学敏感性。