Targeting Epigenetics in Cancer

被引:183
作者
Bennett, Richard L. [1 ]
Licht, Jonathan D. [1 ]
机构
[1] Univ Florida, Dept Med, Hlth Canc Ctr, Div Hematol & Oncol, Gainesville, FL 32606 USA
来源
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 58 | 2018年 / 58卷
关键词
epigenetics; DNA methylation; histone acetylation; histone methylation; epigenetic readers; anticancer therapies; HISTONE DEACETYLASE INHIBITOR; ACUTE MYELOID-LEUKEMIA; GENOME-WIDE ANALYSIS; PHASE-I; DNA METHYLATION; OPEN-LABEL; SOMATIC MUTATIONS; CHEMICAL PROBE; HDAC INHIBITOR; INACTIVATING MUTATIONS;
D O I
10.1146/annurev-pharmtox-010716-105106
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Alterations of genes regulating epigenetic processes are frequently found as cancer drivers and may cause widespread alterations of DNA methylation, histone modification patterns, or chromatin structure that disrupt normal patterns of gene expression. Because of the inherent reversibility of epigenetic changes, inhibitors targeting these processes are promising anticancer strategies. Small molecules targeting epigenetic regulators have been developed recently, and clinical trials of these agents are under way for hematologic malignancies and solid tumors. In this review, we describe how the writers, readers, and erasers of epigenetic marks are dysregulated in cancer and summarize the development of therapies targeting these mechanisms.
引用
收藏
页码:187 / 207
页数:21
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