Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials

被引：662
作者：
Cheng, Yuan [1 ,2 ]
He, Cai [1 ,2 ]
Wang, Manni [1 ,2 ]
Ma, Xuelei [1 ,2 ]
Mo, Fei [1 ,2 ]
Yang, Shengyong [1 ,2 ]
Han, Junhong [1 ,2 ]
Wei, Xiawei [1 ,2 ]
机构：
[1] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Lab Aging Res & Canc Drug Target, Chengdu, Sichuan, Peoples R China
[2] Sichuan Univ, West China Hosp, Canc Ctr, Natl Clin Res Ctr Geriatr, Chengdu, Sichuan, Peoples R China
来源：
SIGNAL TRANSDUCTION AND TARGETED THERAPY | 2019年 / 4卷 / 1期
关键词：
ACUTE MYELOID-LEUKEMIA; CELL LUNG-CANCER; EPITHELIAL-MESENCHYMAL-TRANSITION; TUMOR-SUPPRESSOR GENE; HISTONE DEACETYLASE INHIBITORS; SMALL-MOLECULE INHIBITOR; DE-NOVO METHYLATION; MESSENGER-RNA EXPRESSION; PROTEIN ARGININE METHYLTRANSFERASE; RUBINSTEIN-TAYBI-SYNDROME;
D O I：
10.1038/s41392-019-0095-0
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Epigenetic alternations concern heritable yet reversible changes in histone or DNA modifications that regulate gene activity beyond the underlying sequence. Epigenetic dysregulation is often linked to human disease, notably cancer. With the development of various drugs targeting epigenetic regulators, epigenetic-targeted therapy has been applied in the treatment of hematological malignancies and has exhibited viable therapeutic potential for solid tumors in preclinical and clinical trials. In this review, we summarize the aberrant functions of enzymes in DNA methylation, histone acetylation and histone methylation during tumor progression and highlight the development of inhibitors of or drugs targeted at epigenetic enzymes.
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页数：39
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