Department of Pediatrics, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China.
Department of Pediatrics, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China.
Gene. 2024 Jan 30;893:147917. doi: 10.1016/j.gene.2023.147917. Epub 2023 Oct 20.
Imatinib is the current gold standard for patients with chronic myeloid leukemia (CML). However, the primary and acquired drug resistance seriously limits the efficacy. To identify novel therapeutic target in Imatinib-resistant CML is of crucial clinical significance. CircRNAs have been demonstrated the essential regulatory roles in the progression and drug resistance of cancers. In this study, we identified a novel circRNA (circ_SIRT1), derived from the SIRT1, which is up-regulated in CML. The high expression of circ_SIRT1 is correlated with drug resistance in CML. Knockdown of circ_SIRT1 regulated K562/R cells viability, invasion and apoptosis. Besides, the inhibition of circ_SIRT1 attenuated autophagy level and reduced IC50 to Imatinib of K562/R cells. Mechanistically, circ_SIRT1 directly binds to the transcription factor Eukaryotic Translation Initiation Factor 4A3(EIF4A3) and regulated EIF4A3-mediated transcription of Autophagy Related 12 (ATG12), thereby affecting Imatinib resistance and autophagy level. Overexpression of ATG12 reversed the regulative effects induced by knockdown of circ_SIRT1. Taken together, our findings revealed circ_SIRT1 acted as a potential tumor regulator in CML and unveiled the underlying mechanism on regulating Imatinib resistance. circ_SIRT1 may serve as a novel therapeutic target and provide crucial clinical implications for Imatinib-resistant CML treatment.
伊马替尼是治疗慢性髓系白血病(CML)的金标准。然而,原发和获得性耐药严重限制了其疗效。因此,寻找新的治疗靶点对于克服伊马替尼耐药的 CML 具有重要的临床意义。CircRNAs 在癌症的发生和耐药性中发挥着重要的调控作用。在本研究中,我们发现了一种新型的 circRNA(circ_SIRT1),来源于 SIRT1,在 CML 中呈上调表达。circ_SIRT1 的高表达与 CML 中的耐药性相关。circ_SIRT1 的敲低可调节 K562/R 细胞的活力、侵袭和凋亡。此外,circ_SIRT1 的抑制可降低自噬水平,并降低 K562/R 细胞对伊马替尼的 IC50。机制上,circ_SIRT1 可直接与转录因子真核翻译起始因子 4A3(EIF4A3)结合,并调节 EIF4A3 介导的自噬相关 12(ATG12)的转录,从而影响伊马替尼耐药性和自噬水平。过表达 ATG12 可逆转 circ_SIRT1 敲低引起的调节作用。综上所述,我们的研究结果表明 circ_SIRT1 作为 CML 中的一种潜在肿瘤调节剂,揭示了其调节伊马替尼耐药的潜在机制。circ_SIRT1 可能成为治疗伊马替尼耐药 CML 的新靶点,并为其治疗提供重要的临床意义。