HDACs and HDAC Inhibitors in Cancer Development and Therapy

Over the last several decades, it has become clear that epigenetic abnormalities may be one of the hallmarks of cancer. Posttranslational modifications of histones, for example, may play a crucial role in cancer development and progression by modulating gene transcription, chromatin remodeling, and...

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Bibliographic Details
Published in:Cold Spring Harbor perspectives in medicine 2016-10, Vol.6 (10), p.a026831
Main Authors: Li, Yixuan, Seto, Edward
Format: Article
Language:English
Subjects:
Acetylation
Apoptosis - drug effects
Cell Cycle - drug effects
DNA Damage - drug effects
Histone Acetyltransferases - metabolism
Histone Deacetylase Inhibitors - pharmacology
Histone Deacetylases - metabolism
Humans
Neoplasms - drug therapy
Neoplasms - enzymology
Protein Processing, Post-Translational
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Summary:Over the last several decades, it has become clear that epigenetic abnormalities may be one of the hallmarks of cancer. Posttranslational modifications of histones, for example, may play a crucial role in cancer development and progression by modulating gene transcription, chromatin remodeling, and nuclear architecture. Histone acetylation, a well-studied posttranslational histone modification, is controlled by the opposing activities of histone acetyltransferases (HATs) and histone deacetylases (HDACs). By removing acetyl groups, HDACs reverse chromatin acetylation and alter transcription of oncogenes and tumor suppressor genes. In addition, HDACs deacetylate numerous nonhistone cellular substrates that govern a wide array of biological processes including cancer initiation and progression. This review will discuss the role of HDACs in cancer and the therapeutic potential of HDAC inhibitors (HDACi) as emerging drugs in cancer treatment.
ISSN:2157-1422
2472-5412
DOI:10.1101/cshperspect.a026831