![conference banner](/images/conference-banner.jpeg)
Abstract
In recent years, there has been an expansion of the understanding of how epigenetic dysregulation plays a role in tumorigenesis, progression, metastasis and treatment resistance. Evidence has focused on two common and well-studied “epigenetic codes”, i.e., DNA methylation and histone posttranslational modification, which regulate the transcriptional status in various types of cancer and the corresponding target agents.
Aside from “writers” and “erasers”, which refer to enzymes that catalyze and remove posttranslational modifications, respectively, “readers” bind to target proteins and recruit “writers” and “erasers” for regulating gene expression. A number of selective and potent anticancer compounds have been reported, some of which are in preclinical or clinical trials that have shown promising results, primarily against malignant neoplasms such as hematologic malignancies, with the subsequent emerging development of both monotherapy and co-administration with traditional cytotoxic medicines against solid tumors. Second-generation epigenetic agents such as EZH2 and BET inhibitors have greatly progressed. Epigenetic dysregulation has also provided feasibility for the diagnosis and treatment of cancer. In this review, we summarize the progress in epigenetics and drug discovery for cancer and certain clinical trials that may provide a perspective for future development.
Keywords: Epigenetic, anticancer drug discovery, DNA methylation, histone posttranslational modification.
Anti-Cancer Agents in Medicinal Chemistry
Title:Current Status of Epigenetics and Anticancer Drug Discovery
Volume: 16 Issue: 6
Author(s): Ping Jin and Xiaofei Chen
Affiliation:
Keywords: Epigenetic, anticancer drug discovery, DNA methylation, histone posttranslational modification.
Abstract: In recent years, there has been an expansion of the understanding of how epigenetic dysregulation plays a role in tumorigenesis, progression, metastasis and treatment resistance. Evidence has focused on two common and well-studied “epigenetic codes”, i.e., DNA methylation and histone posttranslational modification, which regulate the transcriptional status in various types of cancer and the corresponding target agents.
Aside from “writers” and “erasers”, which refer to enzymes that catalyze and remove posttranslational modifications, respectively, “readers” bind to target proteins and recruit “writers” and “erasers” for regulating gene expression. A number of selective and potent anticancer compounds have been reported, some of which are in preclinical or clinical trials that have shown promising results, primarily against malignant neoplasms such as hematologic malignancies, with the subsequent emerging development of both monotherapy and co-administration with traditional cytotoxic medicines against solid tumors. Second-generation epigenetic agents such as EZH2 and BET inhibitors have greatly progressed. Epigenetic dysregulation has also provided feasibility for the diagnosis and treatment of cancer. In this review, we summarize the progress in epigenetics and drug discovery for cancer and certain clinical trials that may provide a perspective for future development.
Export Options
About this article
Cite this article as:
Jin Ping and Chen Xiaofei, Current Status of Epigenetics and Anticancer Drug Discovery, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (6) . https://dx.doi.org/10.2174/1871520616666151116124432
DOI https://dx.doi.org/10.2174/1871520616666151116124432 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Advances in Nanomedicines and Targeted Therapies for Colorectal Cancer
Colorectal cancer remains a significant global health challenge, with high incidence and mortality rates despite advancements in treatment strategies. Conventional therapies often face limitations such as systemic toxicity, drug resistance, and suboptimal targeting. The advent of nanomedicines and innovative drug delivery systems offers new hope for overcoming these challenges and ...read more
Discovery of Lead compounds targeting transcriptional regulation
Transcriptional regulation plays key physiological functions in body growth and development. Transcriptional dysregulation is one of the important biomarkers of tumor genesis and progression, which is involved in regulating tumor cell processes such as cell proliferation, differentiation, and apoptosis. Additionally, it plays a pivotal role in angiogenesis and promotes tumor ...read more
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes that aid in stabilizing chromosomal makeup. The resynthesis of telomeres is supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no telomerase activity in human somatic cells, but the stem cells and germ cells undergo ...read more
Innovative targets in medicinal chemistry
Medicinal chemistry continuously evolves in response to emerging healthcare needs and advancements in scientific understanding. This special issue explores the current landscape of innovative targets in medicinal chemistry, highlighting the quest for novel therapeutic avenues. From traditional drug targets such as enzymes and receptors to emerging targets like protein-protein interactions ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Motor Unit and Neuromuscular Junction Remodeling with Aging
Current Aging Science Lipid-Protamine-DNA-Mediated Antigen Delivery
Current Drug Delivery The Relationship Between Oncogene Expression and Clinical Outcome in Endometrial Carcinoma
Current Cancer Drug Targets <i>In Silico</i> Approach for Designing a Novel Recombinant Fusion Protein as a Candidate Vaccine Against HPV
Current Proteomics Integrin-Targeted Peptide- and Peptidomimetic-Drug Conjugates for the Treatment of Tumors
Recent Patents on Anti-Cancer Drug Discovery Therapeutic Potential of HDAC Inhibitors in the Treatment of Cardiac Diseases: A Short Review
Current Drug Targets Withdrawal Notice: Electrophoresis as a Tool for Early Cancer Diagnosis
Anti-Cancer Agents in Medicinal Chemistry VDAC1 as a Player in Mitochondria-Mediated Apoptosis and Target for Modulating Apoptosis
Current Medicinal Chemistry Application of Quantum Dots in Drug Delivery
Nanoscience & Nanotechnology-Asia Current Patents on Osteoinductive Molecules for Bone Tissue Engineering
Recent Patents on Biomedical Engineering (Discontinued) Lessons from Viruses: Controlling the Function of Transmembrane Proteins by Interfering Transmembrane Helices
Current Medicinal Chemistry A Review on Colorimetric Sensing of Tumor Markers Based on Enzyme-Mimicking Nanomaterials
Current Medicinal Chemistry Exfoliated Epithelial Cells: A Non-Invasive way to Evaluate the Physiological State of Gastrointestinal Epithelium
Recent Patents on Biomedical Engineering (Discontinued) Anti-Cancer, Pharmacokinetic and Biodistribution Studies of Cremophor EL Free Alternative Paclitaxel Formulation
Current Drug Safety Triazole and Oxadiazole Containing Natural Products: A Review
The Natural Products Journal Cationic Liposomes as Non-viral Vector for RNA Delivery in Cancer Immunotherapy
Recent Patents on Drug Delivery & Formulation Decoding the Emerging Patterns Exhibited in Non-coding RNAs Characteristic of Lung Cancer with Regard to Their Clinical Significance
Current Genomics Selectively Replicating Adenoviruses for Oncolytic Therapy
Current Cancer Drug Targets Zerumbone Sensitizes the Anti-Cancer Efficacy of Cisplatin in Hepatocellular Carcinoma Cells
Anti-Cancer Agents in Medicinal Chemistry Contemporary Review of Drugs Used to Treat Obesity
Cardiovascular & Hematological Agents in Medicinal Chemistry