This article reviews progress in epigenetic therapies that hope to improve the treatment of cancer. Tumors show widespread, aberrant epigenetic changes, leading to changes in the expression of genes involved in all the hallmarks of cancer. These epigenetic changes can potentially be reversed using small-molecule inhibitors of enzymes involved in maintenance of the epigenetic state. DNA-demethylating agents and histone deacetylase inhibitors have shown anti-tumor activity against certain hematological malignancies; however, their activity in solid tumors remains more uncertain. Major challenges remain in delivery of epigenetic therapy, maintenance of a pharmacodynamic response and achievement of a therapeutic index. We believe histone lysine methyl transferases are a highly promising epigenetic target, which has yet to be clinically exploited. Crystallographic studies on histone lysine methyl transferases provide insights into their mechanism and specificity crucial for the design and development of small-molecule inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.4155/fmc.12.7 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
An Open-Label Phase II Trial of Pembrolizumab, an Immune Checkpoint Inhibitor Alone or in Combination With Oral Azacitidine as Second-Line Therapy for Advanced Head and Neck Squamous Cell Cancers.
Health Sci Rep
January 2025
Medical Oncology Healthcare Global Bangalore India.
Background And Aims: Sensitivity to immune checkpoint inhibitor (ICI) therapy depends in part on the genetic and epigenetic makeup of cancer cells, and CD8 T-lymphocytes that mediate immune responses. Epigenetics are heritable reversible changes in gene expression that occur without any changes in the nuclear DNA sequence or DNA copy number.
Primary Objective: i.
The current state of knowledge on the role of NKG2D ligands in multiple sclerosis and other autoimmune diseases.
Front Mol Neurosci
January 2025
Neurology Clinic, Military Institute of Medicine- National Research Institute, Warsaw, Poland.
Multiple sclerosis (MS) is a chronic central nervous system (CNS) disease with demyelinating inflammatory characteristics. It is the most common nontraumatic and disabling disease affecting young adults. The incidence and prevalence of MS have been increasing.
View Article and Find Full Text PDFPersonalized statin therapy: Targeting metabolic processes to modulate the therapeutic and adverse effects of statins.
Heliyon
January 2025
Xinjiang Key Laboratory of Biological Resources and Genetic Engineering, College of Life Science and Technology, Xinjiang University, Urumqi, Xinjiang, 830046, China.
Statins are widely used for treating lipid disorders and cardiovascular diseases. However, the therapeutic efficiency and adverse effects of statins vary among different patients, which numerous clinical and epidemiological studies have attributed to genetic polymorphisms in statin-metabolizing enzymes and transport proteins. The metabolic processes of statins are relatively complex, involving spontaneous or enzyme-catalyzed interconversion between more toxic lactone metabolites and active acid forms in the liver and bloodstream, influenced by multiple factors, including the expression levels of many metabolic enzymes and transporters.
View Article and Find Full Text PDFSystemic Lupus Erythematous: Gene Polymorphisms, Epigenetics, Environmental, Hormonal and Nutritional Factors in the Consideration of Personalized Therapy.
Arch Intern Med Res
December 2024
Department of Translational Research, College of Osteopathic Medicine of the Pacific, Western University of Health Sciences, Pomona, California 91766 USA.
Systemic Lupus Erythematosus (SLE) is a chronic illness that can affect many tissues through the production of autoantibodies. A definite etiology has not been conclusively established, but current research points to the influences which include genetic, hormonal and environmental factors. SLE is difficult to treat due to its multifactorial pathogenesis and heterogeneity in clinical manifestations.
View Article and Find Full Text PDFKetogenic diet with oxyresveratrol and zinc inhibits glioblastoma and restores memory function and motor coordination.
Oncol Res
January 2025
Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, 576104, India.
Background: To date, there is no effective cure for the highly malignant brain tumor glioblastoma (GBM). GBM is the most common, aggressive central nervous system tumor (CNS). It commonly originates in glial cells such as microglia, oligodendroglia, astrocytes, or subpopulations of cancer stem cells (CSCs).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!