Abstract
The term "epigenetics" is defined as "heritable changes in gene expression that occur without changes in DNA sequence". Recently, it has been revealed that DNA methylation and histone modifications such as acetylation, methylation and phosphorylation are epigenetic mechanisms according to this definition. In other words, these posttranslational modifications are important factors in determining when and where a gene will be expressed. To date, several enzymes that catalyze DNA or histone modifications have been identified, such as DNA methyltransferases and histone deacetylases. Inhibitors and activators of enzymes controlling epigenetic modifications are considered useful not only as tools for the elucidation of cellular and biological phenomena, but also as therapeutic agents, since disruption of the balance of epigenetic networks is known to cause some disease states such as cancer. In this review, we present natural products and synthetic molecules that inhibit or activate enzymes catalyzing DNA methylation or histone modifications, and discuss the potential of epigenetic therapy.
Keywords: Hydrazones, Hydrazides, Hydrolysis, Isoniazid, Mycobacterium, Tuberculosis, QSAR
Current Medicinal Chemistry
Title: Epigenetic Control Using Natural Products and Synthetic Molecules
Volume: 13 Issue: 8
Author(s): T. Scior and S. J. Garces-Eisele
Affiliation:
Keywords: Hydrazones, Hydrazides, Hydrolysis, Isoniazid, Mycobacterium, Tuberculosis, QSAR
Abstract: The term "epigenetics" is defined as "heritable changes in gene expression that occur without changes in DNA sequence". Recently, it has been revealed that DNA methylation and histone modifications such as acetylation, methylation and phosphorylation are epigenetic mechanisms according to this definition. In other words, these posttranslational modifications are important factors in determining when and where a gene will be expressed. To date, several enzymes that catalyze DNA or histone modifications have been identified, such as DNA methyltransferases and histone deacetylases. Inhibitors and activators of enzymes controlling epigenetic modifications are considered useful not only as tools for the elucidation of cellular and biological phenomena, but also as therapeutic agents, since disruption of the balance of epigenetic networks is known to cause some disease states such as cancer. In this review, we present natural products and synthetic molecules that inhibit or activate enzymes catalyzing DNA methylation or histone modifications, and discuss the potential of epigenetic therapy.
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Cite this article as:
Scior T. and Garces-Eisele J. S., Epigenetic Control Using Natural Products and Synthetic Molecules, Current Medicinal Chemistry 2006; 13 (8) . https://dx.doi.org/10.2174/092986706776361067
DOI https://dx.doi.org/10.2174/092986706776361067 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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