![conference banner](/images/conference-banner.jpeg)
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.
Current Cancer Therapy Reviews
Title:Demethylating Agents as Epigenetic Anticancer Therapeutics
Volume: 9 Issue: 1
Author(s): Arash Nabbi, Shankha Satpathy and Karl Riabowol
Affiliation:
Keywords: Cancer, Demethyating Agents, DNA Methylation, Epigenetics.
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.
Export Options
About this article
Cite this article as:
Nabbi Arash, Satpathy Shankha and Riabowol Karl, Demethylating Agents as Epigenetic Anticancer Therapeutics, Current Cancer Therapy Reviews 2013; 9 (1) . https://dx.doi.org/10.2174/1573394711309010003
DOI https://dx.doi.org/10.2174/1573394711309010003 |
Print ISSN 1573-3947 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6301 |
Call for Papers in Thematic Issues
Advancements in Lipid Nanoparticle Delivery Systems for mRNA Therapeutics
The thematic issue "Advancements in Lipid Nanoparticle Delivery Systems for mRNA Therapeutics" aims to explore the cutting-edge developments and innovative strategies in the field of lipid nanoparticle (LNP) technology, particularly focusing on its application in mRNA delivery. This topic has gained unprecedented attention and urgency in the wake of the ...read more
Current progress in Protein Degradation and Cancer Therapy
Targeted Protein Degradation is gaining momentum in cancer therapy, it facilitate targeting undruggable proteins, it overcome cancer resistance and avoid undesirable side effects. Thus small molecules degraders have emerged as novel therapeutic strategy. Targeted protein degradation (TPD), the process of eliminating a protein of interest hold a great promise for ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
The Emerging Role of CSN6 in Biological Behavior and Cancer Progress
Anti-Cancer Agents in Medicinal Chemistry Interaction of Oligomeric Breast Cancer Resistant Protein (BCRP) with Adjudin: A Male Contraceptive with Anti-Cancer Activity
Current Molecular Pharmacology The Use of α-Halo Ethers in the Protection of Alcohols. Years 2012 - 2014
Mini-Reviews in Organic Chemistry Complex 3D Models to Study Drug Targeting of Invadopodia
Clinical Cancer Drugs Image Fusion Based on Estimation Theory: Applied to PET/CT for Radiotherapy
Recent Patents on Medical Imaging Human Papillomavirus Infections, Cervical Cancer and MicroRNAs: An Overview and Implications for Public Health
MicroRNA Bioactive Natural Products from Endophytic Microbes
The Natural Products Journal Telomerase Therapeutics for Degenerative Diseases
Current Molecular Medicine Vitamin D and the Epigenetic Machinery in Colon Cancer
Current Medicinal Chemistry Haloperidol Cytotoxicity and Its Relation to Oxidative Stress
Mini-Reviews in Medicinal Chemistry AMPK as a New Attractive Therapeutic Target for Disease Prevention: The Role of Dietary Compounds AMPK and Disease Prevention
Current Drug Targets Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 1. Selective Enzyme Inhibitors
Current Drug Targets Elastic Bilayer Vesicles of Flurbiprofen for Transdermal Delivery: Development and In-Vitro Characterization
Drug Delivery Letters New Synthesis of Isoindolo[2,1–b]isoquinolines. Preparation and Aqueous Bioavailability of its Silica Nanoparticles Hybrid System
Current Organic Chemistry Pharmacophore Based Drug Design Approach as a Practical Process in Drug Discovery
Current Computer-Aided Drug Design Chimeric Antigen Receptor T Cells: Self-Replicating Drugs for Cancer
Current Drug Targets HPV and Therapeutic Vaccines: Where are We in 2010?
Current Cancer Therapy Reviews Bioactives in Disease Prevention and Health Promotion: Exploiting Combinatorial Effects
Current Bioactive Compounds Editorial [Hot Topic: Boron in Medicinal Chemistry (Guest Editor: M.G.H. Vicente)]
Anti-Cancer Agents in Medicinal Chemistry Lipid-based siRNA Delivery Systems: Challenges, Promises and Solutions Along the Long Journey
Current Pharmaceutical Biotechnology