Abstract
Epigenetics process is the heritable change in gene function that does not involve changes in the DNA sequence. Until now, several types of epigenetic mechanisms have been characterized, including DNA methylation, histone modification (acetylation, methylation, etc.), nucleosome remodeling, and noncoding RNAs. With the biological investigations of these modifiers, some of them are identified as promoters in the process of various diseases, such as cancer, cardiovascular disease and virus infection. Epigenetic changes may serve as potential “first hits” for tumorigenesis. Hence, targeting epigenetic modifiers is being considered as a promising way for disease treatment. To date, six agents in two epigenetic target classes (DNMT and HDAC) have been approved by the US Food and Drug Administration (FDA). Most of these drugs are applied in leukemia, lymphoma therapy, or are combined with other drugs for the treatment of solid tumor. Due to the rapid development of epigenetics and epigenetics targeted drugs, it is becoming an emerging area in targeted drug design.
Keywords: Epigenetic targets, Inhibitors, Cancer therapy, Drug discovery, DNMT, HDAC.
Current Topics in Medicinal Chemistry
Title:The Development of Epigenetics and Related Inhibitors for Targeted Drug Design in Cancer Therapy
Volume: 18 Issue: 28
Author(s): Na Liu, Rongtong Zhao, Yue Ma, Dongyuan Wang, Chen Yan, Dongxian Zhou*, Feng Yin*Zigang Li*
Affiliation:
- Department of Breast Surgery, The Second Affiliated Hospital of Jinan University, Shenzhen People's Hospital, Shenzhen, Guangdong,China
- State Key Laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055,China
- State Key Laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055,China
Keywords: Epigenetic targets, Inhibitors, Cancer therapy, Drug discovery, DNMT, HDAC.
Abstract: Epigenetics process is the heritable change in gene function that does not involve changes in the DNA sequence. Until now, several types of epigenetic mechanisms have been characterized, including DNA methylation, histone modification (acetylation, methylation, etc.), nucleosome remodeling, and noncoding RNAs. With the biological investigations of these modifiers, some of them are identified as promoters in the process of various diseases, such as cancer, cardiovascular disease and virus infection. Epigenetic changes may serve as potential “first hits” for tumorigenesis. Hence, targeting epigenetic modifiers is being considered as a promising way for disease treatment. To date, six agents in two epigenetic target classes (DNMT and HDAC) have been approved by the US Food and Drug Administration (FDA). Most of these drugs are applied in leukemia, lymphoma therapy, or are combined with other drugs for the treatment of solid tumor. Due to the rapid development of epigenetics and epigenetics targeted drugs, it is becoming an emerging area in targeted drug design.
Export Options
About this article
Cite this article as:
Liu Na , Zhao Rongtong, Ma Yue , Wang Dongyuan , Yan Chen, Zhou Dongxian *, Yin Feng *, Li Zigang *, The Development of Epigenetics and Related Inhibitors for Targeted Drug Design in Cancer Therapy, Current Topics in Medicinal Chemistry 2018; 18 (28) . https://dx.doi.org/10.2174/1568026618666181115092623
DOI https://dx.doi.org/10.2174/1568026618666181115092623 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
- Announcements
Related Articles
-
The Immune System in Cancer Prevention, Development and Therapy
Anti-Cancer Agents in Medicinal Chemistry MALDI Mass Spectrometry Imaging, from its Origins up to Today: The State of the Art
Combinatorial Chemistry & High Throughput Screening Surface Modification of Nanocarriers for Cancer Therapy
Current Nanoscience Paraneoplastic Neurological Syndromes - Diagnosis and Management
Current Pharmaceutical Design Astrocytes: Adhesion Molecules and Immunomodulation
Current Drug Targets Roles of EGFR, PI3K, AKT, and mTOR in Heavy Metal-Induced Cancer
Current Cancer Drug Targets Multi-modal Anti-cancer Activities Provided by a Non-replicating Sendai Virus Envelope
Current Cancer Therapy Reviews Thalidomide as an Antiangiogenic Drug in the Treatment of Multiple Myeloma
Letters in Drug Design & Discovery Review of PI3K/mTOR Inhibitors Entering Clinical Trials to Treat Triple Negative Breast Cancers
Recent Patents on Anti-Cancer Drug Discovery Peptido-Targeting of the Mitochondrial Transition Pore Complex for Therapeutic Apoptosis Induction
Current Pharmaceutical Design Advances in Transient Receptor Potential Vanilloid-2 Channel Expression and Function in Tumor Growth and Progression
Current Protein & Peptide Science Rational Targeting of the Urokinase Receptor (uPAR): Development of Antagonists and Non-Invasive Imaging Probes
Current Drug Targets The Roles of Histone Demethylase UTX and JMJD3 (KDM6B) in Cancers: Current Progress and Future Perspectives
Current Medicinal Chemistry Investigation of Image Processing Techniques in MRI Based Medical Image Analysis Methods and Validation Metrics for Brain Tumor
Current Medical Imaging C-glycosyl Flavone from Urginea indica Inhibits Growth and Dissemination of Ehrlich Ascites Carcinoma Cells in Mice
Anti-Cancer Agents in Medicinal Chemistry Natural Monophenols as Therapeutics, Antioxidants and Toxins; Electron Transfer, Radicals and Oxidative Stress
The Natural Products Journal Anti-Angiogenic Approaches to Malignant Gliomas
Current Cancer Drug Targets Signal Transduction Pathways and Transcriptional Mechanisms as Targets for Prevention of Emergence of Multidrug Resistance in Human Cancer Cells
Current Drug Targets Targeting Aberrant TGF-β Signaling in Pre-Clinical Models of Cancer
Anti-Cancer Agents in Medicinal Chemistry Challenges and Strategies in Precision Medicine for Non-Small-Cell Lung Cancer
Current Pharmaceutical Design