组蛋白去乙酰基化酶及其抑制剂在卵巢癌中的应用

Application of histone deacetylase and its inhibitors in ovarian cancer

卵巢癌是女性常见的恶性肿瘤,其死亡率位于女性生殖系统肿瘤之首。组蛋白乙酰化和去乙酰化是表观遗传学研究的重要内容,二者处于一种动态平衡,共同调节组蛋白活性转录与抑制。组蛋白乙酰化作用指组蛋白乙酰化转移酶通过在组蛋白赖氨酸残基乙酰化,激活基因转录,而组蛋白去乙酰基化酶(HDAC)使组蛋白去乙酰化,抑制基因转录。当二者失去平衡时癌症发生率将明显增高。HDAC抑制剂可抑制HDAC的活性,解除对抑癌基因转录的抑制,促进抑癌基因表达,抑制癌细胞增殖,促进凋亡。近年来,组蛋白去乙酰化及其抑制剂在卵巢癌中的研究备受关注。

Ovarian cancer is a common malignant tumor in women,and its mortality rate is the first among female reproductive system tumors.Histone acetylation and deacetylation are the important contents in epigenetic research,and they are in a dynamic balance,which jointly regulate the transcription and inhibition of histone activity.Histone acetylation refers to histone acetylation transferases activate gene transcription by acetylation of lysine residues of histone,while histone deacetylase(HDAC)deacetylates histone and inhibits the gene transcription.When the two are out of balance,the incidence of cancer will be significantly increased.The HDAC inhibitors can inhibit the activity of HDAC,relieve the inhibition of tumor suppressor gene transcription,promote the expression of tumor suppressor gene,inhibit the proliferation of cancer cells and promote apoptosis.In recent years,histone deacetylation and its inhibitors have attracted much attention in the studies of ovarian cancer.