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

Yuan Cheng; Cai He; Manni Wang; Xuelei Ma; Fei Mo; Shengyong Yang; Junhong Han; Xiawei Wei

doi:10.1038/s41392-019-0095-0

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

Signal Transduct Target Ther. 2019 Dec 17:4:62. doi: 10.1038/s41392-019-0095-0. eCollection 2019.

Authors

Yuan Cheng^#¹, Cai He^#¹, Manni Wang¹, Xuelei Ma¹, Fei Mo¹, Shengyong Yang¹, Junhong Han¹, Xiawei Wei¹

Affiliation

¹ Laboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, China.

^# Contributed equally.

Abstract

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.

Keywords: Cancer epidemiology; Drug development.

Publication types

Review
Research Support, Non-U.S. Gov't