组蛋白脱乙酰基酶
聚ADP核糖聚合酶
表观遗传学
组蛋白
癌症研究
PARP抑制剂
染色质
化学
染色质重塑
双重角色
基因沉默
乙酰化
聚合酶
生物
DNA
基因
生物化学
组合化学
作者
Haiying Lu,Lan Bai,Yanping Zhou,Yongping Lu,Zhongliang Jiang,Jianyou Shi
标识
DOI:10.2174/1568026619666190603092407
摘要
The occurrence and development of tumors are closely related to epigenetic instability which modulates gene expression through DNA methylation, histone modification, chromatin remodeling, and RNA-related silencing. Histone deacetylase (HDAC) and poly (ADP-ribose) polymerase (PARP) are targets of epigenetic regulation. Over the years, a large number of studies have shown that HDAC inhibitors and PARP inhibitors have synergistic effects in the treatment of tumors, and there are reports of related dual HDAC/PARP inhibitors. This review will give a brief summary of the synergistic mechanisms of HDAC inhibitors and PARP inhibitors and introduce the design of the first dual HDAC/PARP inhibitor, which may guide the design of more dual HDAC/PARP inhibitors for the treatment of tumors.
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