Journal
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 58
Volume 58, Issue -, Pages 187-207Publisher
ANNUAL REVIEWS
DOI: 10.1146/annurev-pharmtox-010716-105106
Keywords
epigenetics; DNA methylation; histone acetylation; histone methylation; epigenetic readers; anticancer therapies
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Funding
- NCI NIH HHS [R01 CA195732, R01 CA180475, U54 CA193419] Funding Source: Medline
- NATIONAL CANCER INSTITUTE [R01CA180475, R01CA195732, U54CA193419] Funding Source: NIH RePORTER
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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.
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