Mancini Manuela, Castagnetti Fausto, Soverini Simona, Leo Elisa, De Benedittis Caterina, Gugliotta Gabriele, Rosti Gianantonio, Bavaro Luana, De Santis Sara, Monaldi Cecilia, Martelli Margherita, Santucci Maria Alessandra, Cavo Michele, Martinelli Giovanni
Department of Experimental, Diagnostic and Specialty Medicine-DIMES, Institute of Hematology L. and A. Seràgnoli-University of Bologna, Bologna, Italy.
J Cell Biochem. 2017 Nov;118(11):3968-3975. doi: 10.1002/jcb.26052. Epub 2017 May 30.
FOXM1 transcription factor is a central component of tumor initiation, growth, and progression due to its multiple effects on cell cycle, DNA repair, angiogenesis and invasion, chromatin, protein anabolism, and cell adhesion. Moreover, FOXM1 interacts with β-catenin promoting its nuclear import and transcriptional activation. Here, we show that FOXM1 is involved in the advantage of chronic myeloid leukemia hematopoiesis over the normal counterpart. FOXM1 hyper-activation associated with BCR-ABL1 results from phosphorylation by the fusion protein kinase-dependent activation of Polo-like kinase 1. FOXM1 phosphorylation lets its binding with β-catenin and β-catenin transcriptional activation, a key event for persistence of the leukemic stem cell compartment under tyrosine kinase inhibitor therapy. Polo-like kinase 1 inhibitor BI6727, already advanced for clinical use, breaks β-catenin interaction with FOXM1, hence hampering FOXM1 phosphorylation, β-catenin binding, nuclear import, and downstream signaling. In conclusion, our results support Polo-like kinase 1/FOXM1 axis as a complementary target to eradicate leukemic early progenitor/stem cell compartment in chronic myeloid leukemia. J. Cell. Biochem. 118: 3968-3975, 2017. © 2017 Wiley Periodicals, Inc.
FOXM1转录因子是肿瘤起始、生长和进展的核心组成部分,因为它对细胞周期、DNA修复、血管生成和侵袭、染色质、蛋白质合成代谢以及细胞黏附具有多种影响。此外,FOXM1与β-连环蛋白相互作用,促进其核转运和转录激活。在此,我们表明FOXM1参与了慢性髓性白血病造血相对于正常造血的优势。与BCR-ABL1相关的FOXM1过度激活是由Polo样激酶1的融合蛋白激酶依赖性激活磷酸化所致。FOXM1磷酸化使其与β-连环蛋白结合以及β-连环蛋白转录激活,这是酪氨酸激酶抑制剂治疗下白血病干细胞池持续存在的关键事件。已进入临床应用阶段的Polo样激酶1抑制剂BI6727可破坏β-连环蛋白与FOXM1的相互作用,从而阻碍FOXM1磷酸化、β-连环蛋白结合、核转运及下游信号传导。总之,我们的结果支持Polo样激酶1/FOXM1轴作为根除慢性髓性白血病中白血病早期祖细胞/干细胞池的互补靶点。《细胞生物化学杂志》118: 3968 - 3975, 2017年。© 2017威利期刊公司