Rani Harsha, Ganai Shabir Ahmad, Mahadevan Vijayalakshmi
Institute of Bioinformatics and Applied Biotechnology (IBAB), Bangalore, India; Manipal Academy of Higher Education (MAHE), Manipal, India.
SASTRA Deemed University, Thanjavur, 613401, India; Sher-e-Kashmir University of Agricultural Sciences and Technology, Shalimar, Srinagar, Jammu and Kashmir, 190025, India.
Transl Oncol. 2025 Nov;61:102510. doi: 10.1016/j.tranon.2025.102510. Epub 2025 Aug 26.
Histone Deacetylases inhibitors (HDACi) modulate the acetylation profile of lysines on the histone tails to facilitate DNA accessibility to transcription factors. While the phenotypes caused by HDAC inhibition on cancer cells have been studied extensively, the nuclear geometry and expression signatures modulated by these enzymes have not been well understood.This work attempts to understand the functional implication of HDAC inhibitor treatment (NaB and MS275) on cervical cancer cells. We observed an increase in nuclear area upon HDAC inhibition correlating with an increase in expression of active histone marks and lamins and a decrease in levels of repressive epigenetic marks. Our transcriptomic sequencing of HeLa cells treated individually with these inhibitors have identified dysregulation of nucleoporins affecting the nucleocytoplasmic exchange and nucleo-cytoplasmic transport through the nuclear pores. These act in concert with the increase in acetylation due to HDAC inhibition and contribute to the increase in nuclear area. In order to derive clinical implications of the observed mechano signalling genes and epigenetic factors differentially expressed in HeLa cells, we verified these on a TCGA cervical cancer cohort of 148 patients and observed an upregulation of various nucleoporins in cervical cancer patients. Interestingly, the low expression of LMNA and high expression of NUP58 were associated with lower survival rate in the cohort. These signatures have also been validated on Indian cervical cancer tissues. This novel and intricate mechanism of modulating epigenetic regulation and nuclear architecture changes by HDAC inhibition can be utilized for designing targetted epigenetic therapy for cervical cancer.
组蛋白去乙酰化酶抑制剂(HDACi)可调节组蛋白尾部赖氨酸的乙酰化状态,以促进DNA对转录因子的可及性。虽然HDAC抑制对癌细胞造成的表型已得到广泛研究,但这些酶所调节的核几何形状和表达特征尚未得到充分理解。这项工作旨在了解HDAC抑制剂处理(丁酸钠和MS275)对宫颈癌细胞的功能影响。我们观察到HDAC抑制后核面积增加,这与活性组蛋白标记和核纤层蛋白的表达增加以及抑制性表观遗传标记水平的降低相关。我们对单独用这些抑制剂处理的HeLa细胞进行的转录组测序确定了核孔蛋白的失调,这影响了核质交换和通过核孔的核质运输。这些与HDAC抑制导致的乙酰化增加协同作用,导致核面积增加。为了推导在HeLa细胞中差异表达的机械信号基因和表观遗传因子的临床意义,我们在148例患者的TCGA宫颈癌队列中进行了验证,观察到宫颈癌患者中各种核孔蛋白上调。有趣的是,在该队列中,LMNA低表达和NUP58高表达与较低的生存率相关。这些特征也在印度宫颈癌组织中得到了验证。HDAC抑制调节表观遗传调控和核结构变化的这种新颖而复杂的机制可用于设计针对宫颈癌的靶向表观遗传治疗。