MTDH∆7介导的mTOR激活驱动三阴性乳腺癌对阿霉素的耐药性:mTORC1抑制对化学增敏作用的相关性
MTDH∆7-mediated mTOR activation drives doxorubicin resistance in triple-negative breast cancer: Relevance of mTORC1 inhibition on chemosensitization.
作者信息
Sahoo Shashikanta, Kumari Sunita, Neeli Praveen Kumar, Pulipaka Sriravali, Kuncha Madhusudana, Chandra Yogesh, Annamaneni Sandhya, Kotamraju Srigiridhar
机构信息
Department of Applied Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India; Academy of Scientific and Innovative Research, Ghaziabad 201002, India.
Department of Applied Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
出版信息
Cell Signal. 2025 Aug;132:111864. doi: 10.1016/j.cellsig.2025.111864. Epub 2025 May 13.
Cancer chemoresistance poses a major hurdle in the management of several cancers, including breast cancer. Herein, we identified MTDH∆7, a splice variant of an oncogene, metadherin (MTDH), promotes doxorubicin (Dox)-induced chemoresistance in triple-negative breast cancer (TNBC) cells. Increased MTDH∆7 levels were positively correlated with the elevated levels of ABC transporters like ABCB1, ABCC1, and ABCG2, which in turn caused reduced intracellular Dox accumulation. Interestingly, everolimus, an mTORC1 inhibitor, potentiated Dox-induced cytotoxicity by inhibiting MTDH∆7-mediated increase in the aforementioned ABC transporters. Moreover, MTDH∆7 overexpression increased mTORC1 levels, possibly due to MTDH∆7-induced accentuation of mitochondrial respiration, ATP production, and AMPK inactivation. Mechanistically, enhanced phosphorylation of mTORC1 caused NF-κB-dependent activation of cAMP-regulatory element-binding protein (CREB). Further, activated CREB led to an increase in the levels of ABCB1, ABCC1, and ABCG2. Inhibition of either mTORC1 by everolimus or NF-κB by BAY-11-7082 or CREB by H89 reversed these effects and mitigated MTDH∆7-mediated Dox efflux. Accordingly, while Dox administration alone marginally caused tumor regression in SCID mice bearing LV.MTDH∆7-MDA-MB-231 cells, administration of everolimus greatly sensitized these mice to Dox-induced tumor regression. In agreement, intriguingly, a positive correlation was observed between elevated MTDH∆7, mTORC1 activation, and ABC transporters level in human breast cancer patient cohort tumor samples. Collectively, MTDH∆7, by promoting mTOR signaling causes breast cancer chemoresistance, and that targeting MTDH∆7-mTOR signaling axis effectively enhances chemosensitization.
癌症化疗耐药性是包括乳腺癌在内的多种癌症治疗中的主要障碍。在此,我们鉴定出致癌基因黏附素(MTDH)的剪接变体MTDH∆7可促进三阴性乳腺癌(TNBC)细胞对多柔比星(Dox)诱导的化疗耐药性。MTDH∆7水平升高与ABCB1、ABCC1和ABCG2等ABC转运蛋白水平升高呈正相关,进而导致细胞内Dox积累减少。有趣的是,mTORC1抑制剂依维莫司通过抑制MTDH∆7介导的上述ABC转运蛋白增加,增强了Dox诱导的细胞毒性。此外,MTDH∆7过表达增加了mTORC1水平,这可能是由于MTDH∆7诱导的线粒体呼吸、ATP生成增强以及AMPK失活所致。从机制上讲,mTORC1磷酸化增强导致cAMP调节元件结合蛋白(CREB)的NF-κB依赖性激活。此外,激活的CREB导致ABCB1、ABCC1和ABCG2水平升高。依维莫司抑制mTORC1或BAY-11-7082抑制NF-κB或H89抑制CREB均可逆转这些效应,并减轻MTDH∆7介导的Dox外排。因此,单独给予Dox仅能使携带LV.MTDH∆7-MDA-MB-231细胞的SCID小鼠的肿瘤略有消退,而给予依维莫司则极大地提高了这些小鼠对Dox诱导的肿瘤消退的敏感性。有趣的是,在人类乳腺癌患者队列肿瘤样本中,观察到MTDH∆7升高、mTORC1激活与ABC转运蛋白水平之间呈正相关。总体而言,MTDH∆7通过促进mTOR信号传导导致乳腺癌化疗耐药,而靶向MTDH∆7-mTOR信号轴可有效增强化疗敏感性。