Laboratory of Molecular Pathology, Department of Pharmacy, College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Korea.
Carcinogenesis. 2010 Jun;31(6):974-83. doi: 10.1093/carcin/bgp336. Epub 2010 Jan 6.
Unlike epigenetic silencing of tumor suppressor genes, the role of epigenetic derepression of cancer-promoting genes or oncogenes in carcinogenesis remains less well understood. The tight junction proteins claudin-3 and claudin-4 are frequently overexpressed in ovarian cancer and their overexpression was previously reported to promote the migration and invasion of ovarian epithelial cells. Here, we show that the expression of claudin-3 and claudin-4 is repressed in ovarian epithelial cells in association with promoter 'bivalent' histone modifications, containing both the activating trimethylated histone H3 lysine 4 (H3K4me3) mark and the repressive mark of trimethylated histone H3 lysine 27 (H3K27me3). During ovarian tumorigenesis, derepression of CLDN3 and CLDN4 expression correlates with loss of H3K27me3 in addition to trimethylated histone H4 lysine 20 (H4K20me3), another repressive histone modification. Although CLDN4 repression was accompanied by both DNA hypermethylation and repressive histone modifications, DNA methylation was not required for CLDN3 repression in immortalized ovarian epithelial cells. Moreover, activation of both CLDN3 and CLDN4 in ovarian cancer cells was associated with simultaneous changes in multiple histone modifications, whereas H3K27me3 loss alone was insufficient for their derepression. CLDN4 repression was robustly reversed by combined treatment targeting both DNA demethylation and histone acetylation. Our study strongly suggests that in addition to the well-known chromatin-associated silencing of tumor suppressor genes, epigenetic derepression by the conversely related loss of repressive chromatin modifications also contributes to ovarian tumorigenesis via activation of cancer-promoting genes or candidate oncogenes.
与肿瘤抑制基因的表观遗传沉默不同,促进癌症的基因或癌基因的表观遗传去抑制在癌症发生中的作用仍知之甚少。紧密连接蛋白 Claudin-3 和 Claudin-4 在卵巢癌中经常过表达,其过表达先前被报道可促进卵巢上皮细胞的迁移和侵袭。在这里,我们表明 Claudin-3 和 Claudin-4 的表达在与启动子“双价”组蛋白修饰相关的卵巢上皮细胞中受到抑制,包含激活的三甲基化组蛋白 H3 赖氨酸 4(H3K4me3)标记和抑制性标记三甲基化组蛋白 H3 赖氨酸 27(H3K27me3)。在卵巢肿瘤发生过程中,CLDN3 和 CLDN4 表达的去抑制与除三甲基化组蛋白 H4 赖氨酸 20(H4K20me3)外,另一种抑制性组蛋白修饰的 H3K27me3 的丢失相关。尽管 CLDN4 的抑制伴随着 DNA 超甲基化和抑制性组蛋白修饰,但在永生化卵巢上皮细胞中,CLDN3 的抑制不需要 DNA 甲基化。此外,卵巢癌细胞中 CLDN3 和 CLDN4 的激活与多个组蛋白修饰的同时变化相关,而单独的 H3K27me3 丢失不足以使其去抑制。CLDN4 的抑制通过靶向 DNA 去甲基化和组蛋白乙酰化的联合治疗得到了强有力的逆转。我们的研究强烈表明,除了众所周知的肿瘤抑制基因的染色质相关沉默之外,通过相反相关的抑制性染色质修饰的表观遗传去抑制也通过激活促进癌症的基因或候选癌基因有助于卵巢肿瘤发生。
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