Abstract
Histone lysine methylation can be modified by various writers and erasers. Different from other epigenetic modifications, mono-, di, and tri- methylation distinctly modulate chromatin structure and thereby contribute to the regulation of DNA-based nuclear processes such as transcription, replication and repair on their target genes depending on different sites. Modulators with opposing catalytic activities dynamically and precisely control levels of histone lysine methylation, and individual enzymes within these families have become candidate oncology targets in recent years. Until now, plenty of medicinal chemists try to pursue potent and selective inhibitor for KMTs and KDMs in order to have the potential anti-cancer agent, and several of the inhibitors have already enrolled in clinic. Here, we discuss three histone lysine methylation modulators with their inhibitors in clinical trials.
Keywords: Lysine methyltransferase, lysine demethylase, inhibitor, cancer.
Current Pharmaceutical Design
Title:Writers and Erasers of Histone Lysine methylation with Clinically Applied Modulators: Promising Target for Cancer Therapy
Volume: 22 Issue: 39
Author(s): Yi-Chao Zheng, Jin-Lian Ma, Ying Liu and Hong M. Liu
Affiliation:
Keywords: Lysine methyltransferase, lysine demethylase, inhibitor, cancer.
Abstract: Histone lysine methylation can be modified by various writers and erasers. Different from other epigenetic modifications, mono-, di, and tri- methylation distinctly modulate chromatin structure and thereby contribute to the regulation of DNA-based nuclear processes such as transcription, replication and repair on their target genes depending on different sites. Modulators with opposing catalytic activities dynamically and precisely control levels of histone lysine methylation, and individual enzymes within these families have become candidate oncology targets in recent years. Until now, plenty of medicinal chemists try to pursue potent and selective inhibitor for KMTs and KDMs in order to have the potential anti-cancer agent, and several of the inhibitors have already enrolled in clinic. Here, we discuss three histone lysine methylation modulators with their inhibitors in clinical trials.
Export Options
About this article
Cite this article as:
Zheng Yi-Chao, Ma Jin-Lian, Liu Ying and Liu M. Hong, Writers and Erasers of Histone Lysine methylation with Clinically Applied Modulators: Promising Target for Cancer Therapy, Current Pharmaceutical Design 2016; 22 (39) . https://dx.doi.org/10.2174/1381612822666160715125417
DOI https://dx.doi.org/10.2174/1381612822666160715125417 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
-
Theranostic Radiopharmaceuticals Targeting Cancer-Associated Fibroblasts
Current Radiopharmaceuticals Withdrawal Notice: Drug Repurposing for Prospective Anti-Cancer Agents Along with the Clinical Status of the Repurposed Drug
Anti-Cancer Agents in Medicinal Chemistry Snake Venom Phospholipases A2: A New Class of Antitumor Agents
Protein & Peptide Letters Berberine Exerts Anti-cancer Activity by Modulating Adenosine Monophosphate- Activated Protein Kinase (AMPK) and the Phosphatidylinositol 3-Kinase/ Protein Kinase B (PI3K/AKT) Signaling Pathways
Current Pharmaceutical Design Paeonol Inhibits Migration, Invasion and Bone Adhesion of Small Cell Lung Cancer Cells
Current Signal Transduction Therapy MicroRNAs in the Intracellular Space, Regulation of Organelle Specific Pathways in Health and Disease
MicroRNA The Correspondence Between Magnetic Resonance Images and the Clinical and Intraoperative Status of Patients with Spinal Tumors
Current Medical Imaging Cordycepin Affects Multiple Apoptotic Pathways to Mediate Hepatocellular Carcinoma Cell Death
Anti-Cancer Agents in Medicinal Chemistry Imaging Features of Primary Tumors of the Hand
Current Medical Imaging Cancer Drug Discovery Targeting Histone Methyltransferases: An Update
Current Medicinal Chemistry Ewing Sarcoma Family Tumors: Past, Present and Future Prospects
Current Cancer Therapy Reviews Inflammatory Signaling in Cartilage: MAPK and NF-κ B Pathways in Chondrocytes and the Use of Inhibitors for Research into Pathogenesis and Therapy of Osteoarthritis
Current Drug Targets Resveratrol as an Enhancer of Apoptosis in Cancer: A Mechanistic Review
Anti-Cancer Agents in Medicinal Chemistry Targeting Matrix Metalloproteinases in Acute Inflammatory Shock Syndromes
Combinatorial Chemistry & High Throughput Screening Evaluation of the Ability of an Organic Derivative of Ruthenium(II) to Reinforce the Cytotoxicity of Fast Neutron Against Malignant Cells in Culture
Letters in Drug Design & Discovery Computational and Synthetic Biology Approaches for the Biosynthesis of Antiviral and Anticancer Terpenoids from <i>Bacillus subtilis</i>
Medicinal Chemistry The Key Role of Canonical Wnt/β-catenin Signaling in Cartilage Chondrocytes
Current Drug Targets The Role of miR-129-5p in Cancer: A Novel Therapeutic Target
Current Molecular Pharmacology Histotype in Non-Small Cell Lung Cancer Therapy and Staging: The Emerging Role of an Old and Underrated Factor
Current Respiratory Medicine Reviews A Review of the Current Role of Proton Therapy in Modern Oncology
Current Drug Therapy