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

作者：Yuan Cheng, He Cai, Manni Wang, Xuelei Ma, Fei Mo, Shengyong Yang, Junhong Han, Xiawei Wei · 发表于：Signal Transduction and Targeted Therapy · 年份：2019 · DOI：10.1038/s41392-019-0095-0 · 被引用次数：1120 · 研究领域：Histone Deacetylase Inhibitors Research、Epigenetics and DNA Methylation、Protein Degradation and Inhibitors

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.