Amatori Stefano, Bagaloni Irene, Donati Benedetta, Fanelli Mirco
Molecular Pathology and Oncology Lab. "PaoLa," Department of Biomolecular Sciences, University of Urbino "Carlo Bo," Fano, Italy.
Genes Cancer. 2010 Mar;1(3):197-209. doi: 10.1177/1947601910365081.
Despite the involvement of genetic alterations in neoplastic cell transformation, it is increasingly evident that abnormal epigenetic patterns, such as those affecting DNA methylation and histone posttranslational modifications (PTMs), play an essential role in the early stages of tumor development. This finding, together with the evidence that epigenetic changes are reversible, enabled the development of new antineoplastic therapeutic approaches known as epigenetic therapies. Epigenetic modifications are involved in the control of gene expression, and their aberrant distribution is thought to participate in neoplastic transformation by causing the deregulation of crucial cellular pathways. Epigenetic drugs are able to revert the defective gene expression profile of cancer cells and, consequently, reestablish normal molecular pathways. Considering the emerging interest in epigenetic therapeutics, this review focuses on the approaches affecting DNA methylation, evaluates novel strategies and those already approved for clinical use, and compares their therapeutic potential.
尽管基因改变参与了肿瘤细胞的转化，但越来越明显的是，异常的表观遗传模式，如那些影响DNA甲基化和组蛋白翻译后修饰（PTM）的模式，在肿瘤发展的早期阶段起着至关重要的作用。这一发现，连同表观遗传变化是可逆的证据，促成了被称为表观遗传疗法的新型抗肿瘤治疗方法的发展。表观遗传修饰参与基因表达的调控，其异常分布被认为通过导致关键细胞通路的失调而参与肿瘤转化。表观遗传药物能够逆转癌细胞有缺陷的基因表达谱，从而重新建立正常的分子通路。鉴于对表观遗传治疗的兴趣日益浓厚，本综述重点关注影响DNA甲基化的方法，评估新策略和已批准用于临床的策略，并比较它们的治疗潜力。
