组蛋白去乙酰化酶抑制剂抗肿瘤的研究进展

Advances in the anticancer effect of histone deacetylase inhibitor

核心组蛋白的乙酰化和去乙酰化与基因调控密切相关。组蛋白去乙酰化酶抑制剂(histone deacety lase inhibitor,HDACI)通过有效上调抑癌基因的表达、阻断肿瘤生长和诱导肿瘤细胞选择性凋亡来治疗肿瘤。近年来,HDACIs成为肿瘤靶向治疗的研究新热点,其对肿瘤细胞迁移、侵袭、转移的抑制作用和抗肿瘤血管生成作用也被证实。

Acetylation and deacetylation of chromatin histone protein by histone deacetylase（HDAC） dynamically is closely correlated with gene transcriptional regulation. The inhibitor of HDAC（HDACI） is highly effective in up - regulating tumour suppressor gene expression, decreasing tumour growth and inducing apoptosis. Due to high anticancer effectivity with little toxicity to normal cells, HDACI has been a focal topic in the research on molecularly targeted anti - tumour agents. Nowadays, it is clear that HDACI anticancer efficacy is in part, dependent on suppression of cancer cell migration, invasion, metastasis and anti - angiogenesis by the modulation of gene transcription.