Abstract
Background: G9a is the primary enzyme for mono- and dimethylation at Lys 9 of histone H3 and forms predominantly the heteromeric complex as a G9a-GLP (G9a-like protein) that is a functional histone lysine methltransferase in vivo. Mounting evidence suggests that G9a catalyzes methylation of histone and nonhistone proteins, which plays a crucial role in diverse biological processes and human diseases.
Methods: In this study, the current knowledge on biological functions of G9a and inhibitors were summarized. Results: we review the current knowledge on biological functions of G9a, with particular emphasis on regulating gene expression and cell processes, and involvement in human diseases. We outline a perspective on various classes of G9a inhibitors to date from both articles and patents with an emphasis on their discovery, activity and the current research status. Conclusion: We highlight the key knowledge on potential biological functions and various human diseases. We also reviewed the discovery and characterization of the reported G9a inhibitors. However, we also propose the challenges and future opportunities in study of G9a. This review could make a crucial contribution to the long journey to develop drug-like molecules targeting G9a.Keywords: Histone Lysine Methltransferase, G9a, Biological functions, inhibitors, diseases, antineoplastic target.
Current Cancer Drug Targets
Title:G9a - An Appealing Antineoplastic Target
Volume: 17 Issue: 6
Author(s): Wei-Lin Chen, Hao-Peng Sun, Dong-Dong Li, Zhi-Hui Wang, Qi-Dong You*Xiao-Ke Guo*
Affiliation:
- Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009,China
- State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009,China
Keywords: Histone Lysine Methltransferase, G9a, Biological functions, inhibitors, diseases, antineoplastic target.
Abstract: Background: G9a is the primary enzyme for mono- and dimethylation at Lys 9 of histone H3 and forms predominantly the heteromeric complex as a G9a-GLP (G9a-like protein) that is a functional histone lysine methltransferase in vivo. Mounting evidence suggests that G9a catalyzes methylation of histone and nonhistone proteins, which plays a crucial role in diverse biological processes and human diseases.
Methods: In this study, the current knowledge on biological functions of G9a and inhibitors were summarized. Results: we review the current knowledge on biological functions of G9a, with particular emphasis on regulating gene expression and cell processes, and involvement in human diseases. We outline a perspective on various classes of G9a inhibitors to date from both articles and patents with an emphasis on their discovery, activity and the current research status. Conclusion: We highlight the key knowledge on potential biological functions and various human diseases. We also reviewed the discovery and characterization of the reported G9a inhibitors. However, we also propose the challenges and future opportunities in study of G9a. This review could make a crucial contribution to the long journey to develop drug-like molecules targeting G9a.Export Options
About this article
Cite this article as:
Chen Wei-Lin, Sun Hao-Peng, Li Dong-Dong, Wang Zhi-Hui, You Qi-Dong*, Guo Xiao-Ke*, G9a - An Appealing Antineoplastic Target, Current Cancer Drug Targets 2017; 17 (6) . https://dx.doi.org/10.2174/1568009616666160512145303
| DOI https://dx.doi.org/10.2174/1568009616666160512145303 |
Print ISSN 1568-0096 |
| Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Bioactive Polysaccharides From Natural Resources For Cancer Therapy
Bioactive polysaccharides from natural resources exhibit diverse therapeutic properties including anticancer, antioxidant, antidiabetic, immunostimulatory activity, and promotion of wound healing. In the past decades, most studies focused on the extraction and identification of polysaccharides, as well as their biological activities. A large number of bioactive polysaccharides with different structural features ...read more
Emerging Targets and Therapeutic Strategies in Modern Cancer Drug Development
This thematic issue focuses on hot and emerging areas in cancer drug targets, aiming to compile 10-12 high-quality articles that explore cutting-edge research, including but not limited to the discovery of novel targets, development of targeted therapeutics, clinical translation of promising strategies, and addressing challenges like drug resistance. It seeks ...read more
Innovative Cancer Drug Targets: A New Horizon in Oncology
Cancer remains one of the most challenging diseases, with its complexity and adaptability necessitating continuous research efforts into more effective and targeted therapeutic approaches. Recent years have witnessed significant progress in understanding the molecular and genetic basis of cancer, leading to the identification of novel drug targets. These include, but ...read more
Innovative Drug Research Propelling a New Era of Precision Oncology
Drug-oncology research is leading a new era of precision medicine, becoming a frontier hotspot in cancer treatment. Advancements in molecular biology, genomics, and medicinal chemistry have driven revolutionary changes in cancer cognition and treatment strategies. Gene-targeted drugs provide more precise treatments, improving survival rates for certain cancers. Network pharmacology offers ...read more
- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
The Use of 68Ga-DOTA-(Tyr3)-Octreotate PET/CT for Improved Target Definition in Radiotherapy Treatment Planning of Meningiomas – A Case Report
Current Radiopharmaceuticals Clustering and Sampling of the c-Met Conformational Space: A Computational Drug Discovery Study
Combinatorial Chemistry & High Throughput Screening SV40 Pseudovirions as Highly Efficient Vectors for Gene Transfer and their Potential Application in Cancer Therapy
Current Pharmaceutical Biotechnology Exploring the Bio-efficacies of Methanolic Extracts of Nostoc muscorum and Calothrix brevissima with their Characterization Using GC-MS
The Natural Products Journal Carbonic Anhydrase I and II Inhibition with Natural Products: Abrus precatorius
Current Enzyme Inhibition Apixaban - Metabolism, Pharmacologic Properties and Drug Interactions
Current Drug Metabolism Intracellular Delivery of Potential Therapeutic Genes: Prospects in Cancer Gene Therapy
Current Gene Therapy Investigation of the Antiproliferative Action of the Quinoline Alkaloids Kokusaginine and Skimmianine on Human Cell Lines
Current Signal Transduction Therapy Editorial [ Infectious Diseases: What is in our future? ]
Infectious Disorders - Drug Targets Caspases: Structure-Guided Design of Drugs to Control Cell Death
Mini-Reviews in Medicinal Chemistry Estrogens as Potential Therapeutic Agents in Multiple Sclerosis
Central Nervous System Agents in Medicinal Chemistry Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity
Letters in Drug Design & Discovery Recent Progress of Supercritical Carbon Dioxide in Producing Natural Nanomaterials
Mini-Reviews in Medicinal Chemistry Immunotoxins and Other Conjugates: Pre-clinical Studies
Mini-Reviews in Medicinal Chemistry Anticancer Advances of Matrine and Its Derivatives
Current Pharmaceutical Design A Novel Approach for Aerobic Construction of Iron Oxide Nanoparticles by Acinetobacter radioresistens and their Effects on Red Blood Cells
Current Nanoscience QSAR and 3D-QSAR Models in the Field of Tubulin Inhibitors as Anticancer Agents
Current Topics in Medicinal Chemistry Pharmacogenetics of Anticancer Drug Sensitivity and Toxicity in Colorectal Cancer
Current Pharmaceutical Design The Brain, the Penis and Steroid Hormones: Clinical Correlates with Endothelial Dysfunction
Current Pharmaceutical Design Immunostimulatory Oligonucleotides
Recent Patents on Inflammation & Allergy Drug Discovery





