Liang Limiao, Dong Dandan, Sun Jiaxue, Zhang Qin, Yang Xiayun, Wei Gong-Hong, Zhang Peng
MOE Key Laboratory of Metabolism and Molecular Medicine, Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Fudan University Shanghai Cancer Center, Shanghai Medical College of Fudan University, Shanghai 200032, China.
Disease Networks Research Unit, Faculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, 90220 Oulu, Finland.
Cells. 2025 Jul 2;14(13):1008. doi: 10.3390/cells14131008.
Hypoxia is a hallmark of aggressive prostate cancer, but how it disrupts lineage-specific transcriptional programs to drive progression remains unclear. Here, we identify the HIF1α-PHD1-FOXA1 axis as a critical mediator of hypoxic adaptation and androgen signaling suppression. Using genome-wide profiling, we demonstrate that hypoxia reprograms HIF1α chromatin occupancy, shifting its cooperation from AR to FOXA1. Mechanistically, HIF1α physically interacts with FOXA1, destabilizing it via PHD1-mediated hydroxylation-a previously unrecognized post-translational regulatory node. Under hypoxia, loss of FOXA1 attenuates androgen-responsive transcription while activating hypoxia-inducible genes, demonstrating a dual role for this axis in hypoxia adaptation and prostate cancer progression. Genetic or pharmacological disruption of HIF1α-PHD1-FOXA1 impairs prostate cancer proliferation and migration, underscoring its translational relevance. Our findings establish oxygen-dependent FOXA1 degradation as a linchpin connecting microenvironmental stress to transcriptional plasticity in advanced prostate cancer, offering new therapeutic avenues.
缺氧是侵袭性前列腺癌的一个标志,但它如何破坏特定谱系的转录程序以驱动肿瘤进展仍不清楚。在这里,我们确定HIF1α-PHD1-FOXA1轴是缺氧适应和雄激素信号抑制的关键介质。通过全基因组分析,我们证明缺氧会重新编程HIF1α的染色质占据情况,将其合作对象从AR转变为FOXA1。从机制上讲,HIF1α与FOXA1发生物理相互作用,通过PHD1介导的羟基化作用使其不稳定——这是一个以前未被认识的翻译后调控节点。在缺氧条件下,FOXA1的缺失会减弱雄激素反应性转录,同时激活缺氧诱导基因,表明该轴在缺氧适应和前列腺癌进展中具有双重作用。对HIF1α-PHD1-FOXA1进行基因或药物干扰会损害前列腺癌的增殖和迁移,强调了其转化相关性。我们的研究结果确立了氧依赖性FOXA1降解是连接晚期前列腺癌微环境应激与转录可塑性的关键环节,为新的治疗途径提供了依据。