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
Current progress in Protein Degradation and Cancer Therapy
argeted 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
- 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
-
Fetal Undernutrition and the Programming of Blood Pressure
Current Nutrition & Food Science Tumor Escape from Immune Response: Mechanisms and Targets of Activity
Current Drug Targets Intramammary Application of Non-Methylated-CpG Oligodeoxynucleotides (CpG) Inhibits both Local and Systemic Mammary Carcinogenesis in Female BALB/c Her-2/neu Transgenic Mice
Current Cancer Drug Targets Non Steroidal Anti-Inflammatory Drug Induced Damage on Lower Gastro-Intestinal Tract: Is There an Involvement of Microbiota?
Current Drug Safety New Treatment Approaches in Acute Myeloid Leukemia: Review of Recent Clinical Studies
Reviews on Recent Clinical Trials Astrocytes: Adhesion Molecules and Immunomodulation
Current Drug Targets Berberine Effects on NFκB, HIF1A and NFE2L2/AP-1 Pathways in HeLa Cells
Anti-Cancer Agents in Medicinal Chemistry Assessment of Nutritional Status in Cancer – The Relationship Between Body Composition and Pharmacokinetics
Anti-Cancer Agents in Medicinal Chemistry Plasminogen Activator Inhibitor with Very Long Half-life (VLHL PAI-1) can Reduce Bleeding in PAI-1-deficient Patients
Cardiovascular & Hematological Disorders-Drug Targets Luminol As In Situ Light Source in Meso-Tetraphenylporphyrin-Mediated Photodynamic Therapy
Current Medicinal Chemistry Editorial [Hot topic: Molecular Mechanisms of Cancer Cell Death (Executive Editor: Ricardo Perez-Tomas)]
Current Pharmaceutical Design Selection of Reprogramming Factors of Induced Pluripotent Stem Cells Based on the Protein Interaction Network and Functional Profiles
Protein & Peptide Letters An Overview of Labeled Porphyrin Molecules in Medical Imaging
Recent Patents and Topics on Imaging (Discontinued) mRNA as a Therapeutic Target in Lung Disease
Drug Design Reviews - Online (Discontinued) Nucleoprotein-Derived and Unbound Ribonucleosides: Bioactivity and Potential Applications
Current Pharmaceutical Design Telomeres, Genomic Instability, DNA Repair and Breast Cancer
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Nephrotoxicity Associated with Antiretroviral Therapy in HIV-Infected Patients
Current Drug Safety Dasatinib in the Treatment of Chronic Myeloid Leukemia
Current Signal Transduction Therapy Prediction of Degeneration of Native and Bioprosthetic Aortic Valves:Issue-Related Particularities of Diabetes Mellitus
Infectious Disorders - Drug Targets Transmucosal Delivery of Linagliptin for the Treatment of Type- 2 Diabetes Mellitus by Ultra-Thin Nanofibers
Current Drug Delivery