Abstract
The chromatin structure of a gene plays an important role in regulating its expression. This structure is established through the action of various protein complexes that remodel nucleosomes, catalyse post-translational modifications, deposit histone variants and methylate DNA. Together these complexes establish epigenetic marks that influence expression of the gene. Some of these epigenetic marks are transient while others, such as those involved in silencing genes are more stable and can require several cell divisions to be fully implemented or reversed. Deregulated gene expression programs are a feature of cancer biology and it is now apparent that epigenetic changes, as well as genetic changes, are important in establishing these aberrant expression patterns. However, unlike genetic alterations, epigenetic changes are reversible. The complexes that catalyse these modifications therefore represent valuable targets for therapeutic intervention. Here we will review the most recent literature describing the protein complexes that catalyse epigenetic modifications and the inhibitors of these complexes that are being pursued as cancer drugs. In addition we will highlight those epigenetic modifiers that provide promise as therapeutic targets but for which inhibitors are not currently available.
Keywords: Epigenetics, HDAC, DNA methyltransferase, histone methyltransferase
Current Medicinal Chemistry
Title: Targeting Epigenetic Modifiers in Cancer
Volume: 14 Issue: 24
Author(s): A. F. Holloway, P. C. Oakford, A. F. Holloway and P. C. Oakford
Affiliation:
Keywords: Epigenetics, HDAC, DNA methyltransferase, histone methyltransferase
Abstract: The chromatin structure of a gene plays an important role in regulating its expression. This structure is established through the action of various protein complexes that remodel nucleosomes, catalyse post-translational modifications, deposit histone variants and methylate DNA. Together these complexes establish epigenetic marks that influence expression of the gene. Some of these epigenetic marks are transient while others, such as those involved in silencing genes are more stable and can require several cell divisions to be fully implemented or reversed. Deregulated gene expression programs are a feature of cancer biology and it is now apparent that epigenetic changes, as well as genetic changes, are important in establishing these aberrant expression patterns. However, unlike genetic alterations, epigenetic changes are reversible. The complexes that catalyse these modifications therefore represent valuable targets for therapeutic intervention. Here we will review the most recent literature describing the protein complexes that catalyse epigenetic modifications and the inhibitors of these complexes that are being pursued as cancer drugs. In addition we will highlight those epigenetic modifiers that provide promise as therapeutic targets but for which inhibitors are not currently available.
Export Options
About this article
Cite this article as:
Holloway F. A., Oakford C. P., Holloway F. A. and Oakford C. P., Targeting Epigenetic Modifiers in Cancer, Current Medicinal Chemistry 2007; 14 (24) . https://dx.doi.org/10.2174/092986707782023271
DOI https://dx.doi.org/10.2174/092986707782023271 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
- Announcements
Related Articles
-
ATP Site-Directed Inhibitors of Protein Kinase CK2: An Update
Current Topics in Medicinal Chemistry The Expanding Role of APRIL in Cancer and Immunity
Current Molecular Medicine Laccases in Pharmaceutical Chemistry: A Comprehensive Appraisal
Mini-Reviews in Organic Chemistry Vybrant DyeCycle Violet Stain Discriminates Two Different Subsets of CD34+ Cells
Current Stem Cell Research & Therapy Nuclear Magnetic Resonance Spectroscopy of Lipids in Cancer
Current Organic Chemistry Novel and Emerging Drugs for Chronic Lymphocytic Leukemia
Current Cancer Drug Targets Novel Classes of Dimer Antitumour Drug Candidates
Current Pharmaceutical Design Role of Growth Factors in the Pathogenesis of Tissue Fibrosis in Systemic Sclerosis
Current Rheumatology Reviews Future Prospects for Targeted Alpha Therapy
Current Radiopharmaceuticals Recent Patents Concerning Modulators of Protein Kinase C
Recent Patents on DNA & Gene Sequences Drug Treatment of Obesity: Established and Emerging Therapies
Mini-Reviews in Medicinal Chemistry On the Origin of Epidermal Cancers
Current Molecular Medicine What are the Cancer Risks in BRCA Carriers Apart from Those Regarding the Breast and the Ovary?
Current Women`s Health Reviews Nucleosides with Modified Sugar Ring: Synthesis and Biological Activities
Current Organic Chemistry Humoral Immunity in HIV-1 Exposure: Cause or Effect of HIV Resistance?
Current HIV Research Heat Shock Protein 90 – a Potential Target in the Treatment of Human Acute Myelogenous Leukemia
Current Cancer Drug Targets Interplay between DNA Methyltransferase 1 and microRNAs During Tumorigenesis
Current Drug Targets Serpins for Diagnosis and Therapy in Cancer
Cardiovascular & Hematological Disorders-Drug Targets Compendious Review on Bioactive Constituents and Pharmacotherapeutic Profile of Heliotropium indicum Linn
The Natural Products Journal Current Advances in the Development of Anticancer Drugs Targeting Tyrosine Kinases of the Src Family
Current Drug Therapy