生物
磷酸化
癌症研究
髓系白血病
白血病
重编程
干细胞
造血
激酶
转录因子
细胞生物学
髓样
阿扎胞苷
祖细胞
磷酸蛋白质组学
下调和上调
分子生物学
威尼斯人
癌变
P300-CBP转录因子
白细胞介素3
平方毫米
转录调控
运行x1
幼年粒单核细胞白血病
状态5
个人识别码1
核心结合因子
信号转导
细胞培养
综合征如奈梅亨破损综合症
Jurkat细胞
作者
Yufei Lei,Yanru Lai,Yan Li,Yuxing Wang,Haiqi Fan,Qiang Gong,Feng Wu,Qinrong Yan,Hanqing Zeng,Jianchuan Deng,Yu Hou,Zhe Chen
出处
期刊:Blood
[Elsevier BV]
日期:2026-06-30
标识
DOI:10.1182/blood.2025032710
摘要
Leukemia stem cells (LSCs) drive acute myeloid leukemia (AML) initiation, relapse, and chemoresistance, yet the core post-translational events sustaining LSC maintenance remain poorly defined. Here, through phosphoproteomic profiling of normal hematopoietic stem and progenitor cells (HSPCs) versus LSC-enriched populations, we identify DEK phosphorylation as a critical modification during leukemogenesis. Functional studies in MLL-AF9- and HOXA9/MEIS1-driven AML mouse models, as well as patient-derived xenografts (PDXs), demonstrate that DEK deficiency impairs LSC maintenance and AML progression. Moreover, DEK deletion enhances LSC chemosensitivity to the standard-of-care combination of azacitidine and venetoclax (Aza/Ven), whereas DEK overexpression confers robust chemoresistance. Mechanistically, DEK recruits the transcription factor GABPA to upregulate the transcriptional cofactor PBX3, a key oncogenic driver in AML, thereby sustaining the leukemogenic transcriptional program. This DEK-GABPA interaction strictly depends on DEK phosphorylation at Ser301/303/306/307 (the 4S sites), which stabilizes the conformation of the DEK-GABPA complex. We identify casein kinase 2 (CK2) as the upstream kinase that directly phosphorylates DEK-4S sites. Importantly, blockade of DEK phosphorylation via 4S site mutagenesis or treatment with the clinical-stage CK2 inhibitor CX-4945 selectively depletes LSCs while sparing normal HSPCs. Furthermore, combining CX-4945 with venetoclax promotes LSC apoptosis and represses the PBX3-driven leukemogenic transcriptional program, exhibiting synergistic anti-AML effects both in vitro and in vivo. Collectively, our findings uncover a previously unrecognized phosphorylation event (DEK-4S phosphorylation) that sustains LSCs and establish the CK2-DEK axis as a promising LSC-specific therapeutic strategy for AML.
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