Targeting epigenetic regulations in cancer

• Published in: Acta biochimica et biophysica Sinica 2016-01, Vol.48 (1), p.97-109
• Main Authors: Ning, Bo, Li, Wenyuan, Zhao, Wei, Wang, Rongfu
• Format: Article
• Language: English
• Subjects: Acetylation; Animals; Chromatin - metabolism; DNA (Cytosine-5-)-Methyltransferase 1; DNA (Cytosine-5-)-Methyltransferases - genetics; DNA Methylation; DNA甲基化; Epigenesis, Genetic; Gene Expression Regulation, Neoplastic; Gene Silencing; Histone Code; Histones - metabolism; Humans; Mice; Neoplasms - genetics; Neoplasms - metabolism; Protein Processing, Post-Translational; Reviews; Transcription, Genetic; 染色质重塑; 癌症治疗; 组蛋白乙酰化; 组蛋白修饰; 表观遗传; 遗传基因; 遗传调控
• ISSN: 1672-9145; 1745-7270
• DOI: 10.1093/abbs/gmv116

Epigenetic regulation of gene expression is a dynamic and reversible process with DNA methylation, histone modifications, and chromatin remodeling. Recently, groundbreaking studies have demon- strated the importance of DNA and chromatin regulatory proteins from different aspects, including stem cell, development, and tumor genesis. Abnormal epigenetic regulation is frequently associated with diseases and drugstargeting DNA methylation and histone acetylation have been approved for cancer therapy. Although the network of epigenetic regulation is more complex than people expect, new potential druggable chromatin-associated proteins are being discovered and tested for clinical application. Here we review the key proteins that mediate epigenetic regulations through DNA methylation, the acetylation and methylation of histones, and the reader proteins that bind to modi- fied histories. We also discuss cancer associations and recent progress of pharmacological develop- ment of these proteins.