摘要
表观遗传修饰在肿瘤中起重要作用,对基因表达有重要影响的是染色质组蛋白乙酰化,依靠组蛋白乙酰化转移酶(histone acetyltransferases,HATs)和组蛋白去乙酰化酶(histone deacetylases,HDACs)的调控来平衡。染色质的乙酰化状态能导致肿瘤抑制基因或促凋亡基因低表达。组蛋白去乙酰化酶抑制剂(histone deacetylase inhibitors,HDACi)可通过提高染色质特定区域组蛋白乙酰化,从而影响基因的表达,成为一类新的抗肿瘤药物。HDACi具有诱导细胞周期抑制和凋亡的抗肿瘤潜能。已有几种HDACi进入临床试验阶段。
It has been shown that epigenetic modifications play an important role in tumorigenesis. Among the key chromatin modifying enzymes,chromatin histone acetylation influences gene expression,Balanced by the activities of histone acetyltransferases （HATs） and histone deacetylases （HDACs）, determining the acetylation status of histones. With a consequent hypoaeetylated state of chromatin that can be strictly correlated with low expression of either tumor suppressor or pro-apoptotic genes. Histone deacetylase inhibitors （HDACi）represent a new and promising class of antitumor drugs that influence gene expression by enhancing acetylation of histones in specific chromatin domains. HDACi have been shown to exert potent anticancer activities inducing cell cycle arrest and apoptosis. Several HDACi are currently under clinical investigation.
出处
《国际妇产科学杂志》
CAS
2010年第4期267-270,共4页
Journal of International Obstetrics and Gynecology
