Abstract
Aberrant histone lysine methylation that is controlled by histone lysine methyltransferases (KMTs) and demethylases (KDMs) plays significant roles in carcinogenesis. Infections by tumor viruses or parasites and exposures to chemical carcinogens can modify the process of histone lysine methylation. Many KMTs and KDMs contribute to malignant transformation by regulating the expression of human telomerase reverse transcriptase (hTERT), forming a fused gene, interacting with proto-oncogenes or being up-regulated in cancer cells. In addition, histone lysine methylation participates in tumor suppressor gene inactivation during the early stages of carcinogenesis by regulating DNA methylation and/or by other DNA methylation independent mechanisms. Furthermore, recent genetic discoveries of many mutations in KMTs and KDMs in various types of cancers highlight their numerous roles in carcinogenesis and provide rare opportunities for selective and tumor-specific targeting of these enzymes. The study on global histone lysine methylation levels may also offer specific biomarkers for cancer detection, diagnosis and prognosis, as well as for genotoxic and non-genotoxic carcinogenic exposures and risk assessment. This review summarizes the role of histone lysine methylation in the process of cellular transformation and carcinogenesis, genetic alterations of KMTs and KDMs in different cancers and recent progress in discovery of small molecule inhibitors of these enzymes.
Keywords: Carcinogenesis, cell transformation, gene mutations, histone lysine-specific demethylases, histone lysine-specific methyltransferases, inhibitors.
Current Cancer Drug Targets
Title:Histone Lysine-Specific Methyltransferases and Demethylases in Carcinogenesis: New Targets for Cancer Therapy and Prevention
Volume: 13 Issue: 5
Author(s): Xuejiao Tian, Saiyang Zhang, Hong-Min Liu, Yan-Bing Zhang, Christopher A. Blair, Dan Mercola, Paolo Sassone-Corsi and Xiaolin Zi
Affiliation:
Keywords: Carcinogenesis, cell transformation, gene mutations, histone lysine-specific demethylases, histone lysine-specific methyltransferases, inhibitors.
Abstract: Aberrant histone lysine methylation that is controlled by histone lysine methyltransferases (KMTs) and demethylases (KDMs) plays significant roles in carcinogenesis. Infections by tumor viruses or parasites and exposures to chemical carcinogens can modify the process of histone lysine methylation. Many KMTs and KDMs contribute to malignant transformation by regulating the expression of human telomerase reverse transcriptase (hTERT), forming a fused gene, interacting with proto-oncogenes or being up-regulated in cancer cells. In addition, histone lysine methylation participates in tumor suppressor gene inactivation during the early stages of carcinogenesis by regulating DNA methylation and/or by other DNA methylation independent mechanisms. Furthermore, recent genetic discoveries of many mutations in KMTs and KDMs in various types of cancers highlight their numerous roles in carcinogenesis and provide rare opportunities for selective and tumor-specific targeting of these enzymes. The study on global histone lysine methylation levels may also offer specific biomarkers for cancer detection, diagnosis and prognosis, as well as for genotoxic and non-genotoxic carcinogenic exposures and risk assessment. This review summarizes the role of histone lysine methylation in the process of cellular transformation and carcinogenesis, genetic alterations of KMTs and KDMs in different cancers and recent progress in discovery of small molecule inhibitors of these enzymes.
Export Options
About this article
Cite this article as:
Tian Xuejiao, Zhang Saiyang, Liu Hong-Min, Zhang Yan-Bing, Blair A. Christopher, Mercola Dan, Sassone-Corsi Paolo and Zi Xiaolin, Histone Lysine-Specific Methyltransferases and Demethylases in Carcinogenesis: New Targets for Cancer Therapy and Prevention, Current Cancer Drug Targets 2013; 13 (5) . https://dx.doi.org/10.2174/1568009611313050007
DOI https://dx.doi.org/10.2174/1568009611313050007 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
-
MicroRNA-183 Functions As an Oncogene by Regulating PDCD4 in Gastric Cancer
Anti-Cancer Agents in Medicinal Chemistry Anti Cancer Activity on Graviola, an Exciting Medicinal Plant Extract vs Various Cancer Cell Lines and a Detailed Computational Study on its Potent Anti-Cancerous Leads
Current Topics in Medicinal Chemistry Recent Advances in Receptor-Targeted Fluorescent Probes for In Vivo Cancer Imaging
Current Medicinal Chemistry Effects of Tea Catechins on Inflammation-Related Cardiovascular Diseases
Current Immunology Reviews (Discontinued) Tumor Stroma Manipulation By MSC
Current Drug Targets Journey of 2′-deoxy-2′-fluoro-5-methyl-1-β-D-arabinofuranosyluracil (FMAU): from Antiviral Drug to PET Imaging Agent
Current Medicinal Chemistry MiR-147: Functions and Implications in Inflammation and Diseases
MicroRNA Transductional and Transcriptional Targeting of Adenovirus for Clinical Applications
Current Gene Therapy Molecular Imaging of Therapeutic Potential of Reporter Probes
Current Drug Targets Meet Our Editorial Board Member
Current Cancer Therapy Reviews Development of RGD-Based Radiotracers for Tumor Imaging and Therapy: Translating from Bench to Bedside
Current Molecular Medicine Recent Approaches in Chemoprevention of Prostate Cancer
Current Cancer Drug Targets Delta Np63 alpha – Responsive microRNA Modulate the Expression of Metabolic Enzymes
Current Pharmaceutical Biotechnology Dietary Fatty Acids in Metabolic Syndrome, Diabetes and Cardiovascular Diseases
Current Diabetes Reviews Multiple Means by Which Nitric Oxide can Antagonize Photodynamic Therapy
Current Medicinal Chemistry 7-O-aminoalkyl-2,3-dehydrosilibinins: Synthesis and in vitro Anti-cancer Efficacy
Anti-Cancer Agents in Medicinal Chemistry Genito-Urological Cancers in Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry Nucleosides, a Valuable Chemical Marker for Quality Control in Traditional Chinese Medicine Cordyceps
Recent Patents on Biotechnology Nonviral Vectors for Cancer Gene Therapy: Prospects for Integrating Vectors and Combination Therapies
Current Gene Therapy Circadian Timekeeping in Anticancer Therapeutics: An Emerging Vista of Chronopharmacology Research
Current Drug Metabolism