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
-
Targeting the Perpetrator: Breast Cancer Stem Cell Therapeutics
Current Drug Targets The Protease of Human T-Cell Leukemia Virus Type-1 is a Potential Therapeutic Target
Current Pharmaceutical Design The Genetic Basis of New Treatment Modalities in Melanoma
Current Drug Targets Novel and Emerging Drugs for Acute Lymphoblastic Leukemia
Current Cancer Drug Targets Methotrexate-Induced Pneumonitis: Heterogeneity of Bronchoalveolar Lavage and Differences between Cancer and Rheumatoid Arthritis
Inflammation & Allergy - Drug Targets (Discontinued) Pathobiology and Therapeutic Implications of Tumor Acidosis
Current Medicinal Chemistry Effects of Drug Transporters on Pharmacological Responses and Safety
Current Drug Metabolism Modelling and Measuring Redox Cycling and Cytotoxicity of Quinones
Drug Metabolism Letters Monoclonal Antobodies: Application in Radiopharmacy
Current Radiopharmaceuticals Overview of Ribonucleotide Reductase Inhibitors: An Appealing Target in Anti-Tumour Therapy
Current Medicinal Chemistry Epidemiology and Prevention of Bacterial Infections in Patients with Hematologic Malignancies
Infectious Disorders - Drug Targets Microenvironmental Regulation of Cancer Stem Cell Phenotypes
Current Stem Cell Research & Therapy Implications of FLT3 Mutations in the Therapy of Acute Myeloid Leukemia
Reviews on Recent Clinical Trials Regulation of Arylamine N-Acetyltransferases
Current Drug Metabolism STAT-3 Inhibitors: State of the Art and New Horizons for Cancer Treatment
Current Medicinal Chemistry Beyond Photodynamic Therapy: Light-Activated Cancer Chemotherapy
Current Medicinal Chemistry Antibody-Based Preventive and Therapeutic Strategies Against HIV
Current HIV Research Pathobiology and Prevention of Cancer Chemotherapy-Induced Bone Growth Arrest, Bone Loss, and Osteonecrosis
Current Molecular Medicine Vasoproliferation and Antiproliferative Treatment Options in Pulmonary Arterial Hypertension
Recent Patents on Cardiovascular Drug Discovery PI3K/Akt Signalling Pathway Specific Inhibitors: A Novel Strategy to Sensitize Cancer Cells to Anti-Cancer Drugs
Current Pharmaceutical Design