Generic placeholder image

Current Cancer Therapy Reviews

Editor-in-Chief

ISSN (Print): 1573-3947
ISSN (Online): 1875-6301

Demethylating Agents as Epigenetic Anticancer Therapeutics

Author(s): Arash Nabbi, Shankha Satpathy and Karl Riabowol

Volume 9, Issue 1, 2013

Page: [24 - 33] Pages: 10

DOI: 10.2174/1573394711309010003

Price: $65

conference banner
Abstract

DNA methylation is an epigenetic phenomenon, which has major effects on gene expression. Increased methylation generally inhibits transcription while hypomethylation is primarily associated with increased transcription. Hypermethylation of tumor suppressor genes occurs frequently in cancer leading to silencing of these growth inhibitory genes. Demethylating agents are a class of anti-cancer drugs which reduce cytosine methylation, promoting transcriptional activation of genes by virtue of reducing methylation in their promoter regions. Most compounds that inhibit methylation are inhibitors of DNA methyltransferases (DNMTs) that are responsible for methylating cytosine residues on DNA. Azacitidine and Decitabine are two such demethylating agents that are approved for use in myelodysplastic syndromes. In this review, we describe the pharmacology of demethylating agents and their use in recent clinical studies. The current literature describing the efficacy of combining these agents with other chemotherapeutics in various types of cancer is also reviewed.

Keywords: Cancer, Demethyating Agents, DNA Methylation, Epigenetics.


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy