He Wei, Liu Suotian, Wei Wei, Qin Run, Tan Jinfeng, Tang Jie, Huang Zhenglan, Gao Miao
Department of Clinical Hematology, Key Laboratory of Laboratory Medical Diagnostics Designated by Ministry of Education, School of Laboratory Medicine, Chongqing Medical University Chongqing 400016, China.
Department of Laboratory Medicine, The Central Hospital of Wuhan No. 26, Shengli Street, Jiang'an District, Wuhan 430000, Hubei, China.
Am J Cancer Res. 2024 Jun 15;14(6):2770-2789. doi: 10.62347/RWLJ3990. eCollection 2024.
Chronic myeloid leukemia (CML) is a common hematopoietic malignancy in adults. Great progress has been made in CML therapy with imatinib. However, resistance to imatinib may occur during treatment. BCR::ABL1 dependent imatinib resistance has been well resolved with more potent tyrosine kinase inhibitors, but BCR::ABL1 independent resistance still remains to be resolved. This study is devoted to find novel targets for BCR::ABL1 independent imatinib-resistant patients. It is reported BCR::ABL1 independent resistance is mainly related to the activation of alternative survival pathway, and mTOR is an important regulator for cell growth especially in tumor cells. Hence, we explored the role of mTOR in BCR::ABL1 independent resistance, the possibility of mTOR to be a therapeutic target for imatinib resistant patients and the related mechanism. We found mTOR was upregulated in imatinib-resistant cells. mTOR inhibition by AZD2014 led to growth inhibition and synergized with imatinib in apoptosis induction in K562/G01. AZD2014 exerted its anti-leukemia effect through enhancing autophagy. mTOR signal pathway is poorly inhibited by imatinib and AZD2014 shows little effect on BCR::ABL1 signal pathway, which indicates that mTOR is involved in imatinib resistance via a BCR::ABL1 independent manner. Taken together, mTOR represents a potential target to overcome BCR::ABL1 independent imatinib resistance.
慢性髓性白血病(CML)是成人常见的造血系统恶性肿瘤。伊马替尼治疗CML已取得巨大进展。然而,治疗期间可能会出现对伊马替尼的耐药性。更有效的酪氨酸激酶抑制剂已很好地解决了BCR::ABL1依赖性伊马替尼耐药问题,但BCR::ABL1非依赖性耐药仍有待解决。本研究致力于为BCR::ABL1非依赖性伊马替尼耐药患者寻找新靶点。据报道,BCR::ABL1非依赖性耐药主要与替代生存途径的激活有关,而mTOR是细胞生长尤其是肿瘤细胞生长的重要调节因子。因此,我们探讨了mTOR在BCR::ABL1非依赖性耐药中的作用、mTOR作为伊马替尼耐药患者治疗靶点的可能性及其相关机制。我们发现mTOR在伊马替尼耐药细胞中上调。AZD2014抑制mTOR导致K562/G01细胞生长受抑制,并与伊马替尼协同诱导凋亡。AZD2014通过增强自噬发挥其抗白血病作用。伊马替尼对mTOR信号通路抑制作用较弱,且AZD2014对BCR::ABL1信号通路影响较小,这表明mTOR通过BCR::ABL1非依赖性方式参与伊马替尼耐药。综上所述,mTOR是克服BCR::ABL1非依赖性伊马替尼耐药的潜在靶点。