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 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Inhibition of Anti-Apoptotic Bcl-2 Family Proteins by Natural Polyphenols New Avenues for Cancer Chemoprevention and Chemotherapy
Current Pharmaceutical Design <i>In silico</i> and <i>In vitro</i> Investigation of a Likely Pathway for Anti-Cancerous Effect of Thrombocidin-1 as a Novel Anticancer Peptide
Protein & Peptide Letters Brain Tumor Causes, Symptoms, Diagnosis and Radiotherapy Treatment
Current Medical Imaging Cancer Metastasis as Disrupted Developmental Phenotype
Current Genomics Novel Benzo[B]Furans with Anti-Microtubule Activity Upregulate Expression of Apoptotic Genes and Arrest Leukemia Cells in G2/M Phase
Anti-Cancer Agents in Medicinal Chemistry Alginate Bead-Encapsulated PEDF Induces Ectopic Bone Formation In Vivo in the Absence of Co-Administered Mesenchymal Stem Cells
Current Drug Targets Mining Sarcomas by Proteomics Approaches: Ewing Sarcoma on the Spotlight
Recent Patents on Biotechnology Targeting CSC-Related miRNAs for Cancer Therapy by Natural Agents
Current Drug Targets Targeted Therapies in Bone Sarcomas
Current Cancer Drug Targets Insight View on Possible Role of Fluoroquinolones in Cancer Therapy
Current Topics in Medicinal Chemistry The Medicinal Chemistry of Theragnostics, Multimodality Imaging and Applications of Nanotechnology in Cancer
Current Topics in Medicinal Chemistry The Roles of Endoplasmic Reticulum Stress in the Pathophysiological Development of Cartilage and Chondrocytes
Current Pharmaceutical Design Enasidenib: First Mutant IDH2 Inhibitor for the Treatment of Refractory and Relapsed Acute Myeloid Leukemia
Anti-Cancer Agents in Medicinal Chemistry The Urokinase-type Plasminogen Activator and the Generation of Inhibitors of Urokinase Activity and Signaling
Current Pharmaceutical Design Genetic and Epigenetic Drug Targets in Myelodysplastic Syndromes
Current Pharmaceutical Design Modulation of Gene Transcription by Natural Products - A Viable Anticancer Strategy
Current Pharmaceutical Design Translational Research of Photodynamic Therapy with Acridine Orange which Targets Cancer Acidity
Current Pharmaceutical Design Targeting Sarcomas: Novel Biological Agents and Future Perspectives
Current Drug Targets Preferentially Expressed Antigen in Melanoma (PRAME) and the PRAME Family of Leucine-Rich Repeat Proteins
Current Cancer Drug Targets Regulation of Autophagy by Sphingolipids
Anti-Cancer Agents in Medicinal Chemistry