Abstract
Enhancer of Zeste Homolog 2 (EZH2) is the core component of the polycomb repressive complex 2 (PRC2), possessing the enzymatic activity in generating di/tri-methylated lysine 27 in histone H3. EZH2 has important roles during early development, and its dysregulation is heavily linked to oncogenesis in various tissue types. Accumulating evidences suggest a remarkable therapeutic potential by targeting EZH2 in cancer cells. The first part reviews current strategies to target EZH2 in cancers, and evaluates the available compounds and agents used to disrupt EZH2 functions. Then we provide insight to the future direction of the research on targeting EZH2 in different cancer types. We comprehensively discuss the current understandings of the 1) structure and biological activity of EZH2, 2) its role during the assembling of PRC2 and recruitment of other protein components, 3) the molecular events directing EZH2 to target genomic regions, and 4) post-translational modification at EZH2 protein. The discussion provides the basis to inspire the development of novel strategies to abolish EZH2-related effects in cancer cells.
Keywords: Chemotherapy, DNA methylation, DZNep, EZH2, H3K27me3, LncRNA, PRC2, SET domain.
Current Protein & Peptide Science
Title:Targeting EZH2 for Cancer Therapy: Progress and Perspective
Volume: 16 Issue: 6
Author(s): Chi Han Li and Yangchao Chen
Affiliation:
Keywords: Chemotherapy, DNA methylation, DZNep, EZH2, H3K27me3, LncRNA, PRC2, SET domain.
Abstract: Enhancer of Zeste Homolog 2 (EZH2) is the core component of the polycomb repressive complex 2 (PRC2), possessing the enzymatic activity in generating di/tri-methylated lysine 27 in histone H3. EZH2 has important roles during early development, and its dysregulation is heavily linked to oncogenesis in various tissue types. Accumulating evidences suggest a remarkable therapeutic potential by targeting EZH2 in cancer cells. The first part reviews current strategies to target EZH2 in cancers, and evaluates the available compounds and agents used to disrupt EZH2 functions. Then we provide insight to the future direction of the research on targeting EZH2 in different cancer types. We comprehensively discuss the current understandings of the 1) structure and biological activity of EZH2, 2) its role during the assembling of PRC2 and recruitment of other protein components, 3) the molecular events directing EZH2 to target genomic regions, and 4) post-translational modification at EZH2 protein. The discussion provides the basis to inspire the development of novel strategies to abolish EZH2-related effects in cancer cells.
Export Options
About this article
Cite this article as:
Han Li Chi and Chen Yangchao, Targeting EZH2 for Cancer Therapy: Progress and Perspective, Current Protein & Peptide Science 2015; 16 (6) . https://dx.doi.org/10.2174/1389203716666150409100233
DOI https://dx.doi.org/10.2174/1389203716666150409100233 |
Print ISSN 1389-2037 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5550 |
Call for Papers in Thematic Issues
Advancements in Proteomic and Peptidomic Approaches in Cancer Immunotherapy: Unveiling the Immune Microenvironment
The scope of this thematic issue centers on the integration of proteomic and peptidomic technologies into the field of cancer immunotherapy, with a particular emphasis on exploring the tumor immune microenvironment. This issue aims to gather contributions that illustrate the application of these advanced methodologies in unveiling the complex interplay ...read more
Artificial Intelligence for Protein Research
Protein research, essential for understanding biological processes and creating therapeutics, faces challenges due to the intricate nature of protein structures and functions. Traditional methods are limited in exploring the vast protein sequence space efficiently. Artificial intelligence (AI) and machine learning (ML) offer promising solutions by improving predictions and speeding up ...read more
Nutrition and Metabolism in Musculoskeletal Diseases
The musculoskeletal system consists mainly of cartilage, bone, muscles, tendons, connective tissue and ligaments. Balanced metabolism is of vital importance for the homeostasis of the musculoskeletal system. A series of musculoskeletal diseases (for example, sarcopenia, osteoporosis) are resulted from the dysregulated metabolism of the musculoskeletal system. Furthermore, metabolic diseases (such ...read more
Protein Folding, Aggregation and Liquid-Liquid Phase Separation
Protein folding, misfolding and aggregation remain one of the main problems of interdisciplinary science not only because many questions are still open, but also because they are important from the point of view of practical application. Protein aggregation and formation of fibrillar structures, for example, is a hallmark of a ...read more
Related Journals
- 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
-
The mTOR/4E-BP1/eIF4E Signalling Pathway as a Source of Cancer
Drug Targets
Current Medicinal Chemistry Role of Pancreatic β-Cell Death and Cell Death-Associated Inflammation in Diabetes
Current Molecular Medicine Breast Cancer Resistance Protein and P-Glycoprotein in Brain Cancer: Two Gatekeepers Team Up
Current Pharmaceutical Design Cancer Gene Therapy through Autonomous Parvovirus - Mediated Gene Transfer
Current Gene Therapy Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 1. Selective Enzyme Inhibitors
Current Drug Targets TGF Beta Inhibition for Cancer Therapy
Current Cancer Drug Targets SnoN: Bridging Neurobiology and Cancer Biology
Current Molecular Medicine Identification of AHSA1 as a Potential Therapeutic Target for Breast Cancer: Bioinformatics Analysis and <i>in vitro</i> Studies
Current Cancer Drug Targets Poly(lactide-co-glycolide)-based Micro and Nanoparticles for the Controlled Drug Delivery of Vitamins
Current Nanoscience Stability Testing During Development of Nanopharmaceuticals
Pharmaceutical Nanotechnology Systems Biology of Apoptosis and Survival: Implications for Drug Development
Current Pharmaceutical Design The Role of Connexins in Carcinogenesis: Review of Current Knowledge
Current Signal Transduction Therapy Modified Polysaccharides as Carriers for Biomolecules
Pharmaceutical Nanotechnology Temozolomide: An Update on Pharmacological Strategies to Increase its Antitumour Activity
Medicinal Chemistry Reviews - Online (Discontinued) Receptor Tyrosine Kinases as Therapeutic Targets in Malignant Glioma
Reviews on Recent Clinical Trials The Role and Therapeutic Potential of Ser/Thr Phosphatase PP2A in Apoptotic Signalling Networks in Human Cancer Cells
Current Molecular Medicine Effect of PI3K/AKT/mTOR Signaling Pathway on Regulating and Controlling the Anti-Invasion and Metastasis of Hepatoma Cells by Bufalin
Recent Patents on Anti-Cancer Drug Discovery Therapeutic Polycomb Targeting in Human Cancer
Recent Patents on Regenerative Medicine In Silico Prediction Models for Blood-Brain Barrier Permeation
Current Medicinal Chemistry In Vivo Cellular Imaging for Translational Medical Research
Current Medical Imaging