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Abstract
DNA is packaged in an octamer of histones, forming chromatin, a complex of DNA and proteins. The structural matrix of a chromosome, chromatin and its changes are now regarded as important factors in controlling gene expression, which has sparked a lot of interest in understanding genetic pathways governing various diseases, including cancer. DNA methylation in the CpG dinucleotide as a transcriptional silencing mechanism, post-translational histone modifications such as acetylation, methylation, and others that affect chromatin structure, ATP-dependent chromatin remodelling, and miRNA-mediated gene silencing are all found to be important in various types of cancer. In this review, we analyze the main alterations in gene expression, epigenetic modification patterns in cancer cells, the main modulators and inhibitors of each epigenetic mechanism, and the molecular evolution of the most representative inhibitors, all of which point to a promising future for HAT, HDAC, non-glycoside DNMT inhibitors, and domain inhibitors.
Keywords: Cancer, chromatin, histone, DNA, epigenetic inhibitor, epigenoma.
Current Medicinal Chemistry
Title:Epigenetic Modulators as Treatment Alternative to Diverse Types of Cancer
Volume: 29 Issue: 9
Author(s): Jorseth Rodelo Gutiérrez, Arturo René Mendoza Salgado, Marcio De Ávila Arias, Homero San-Juan-Vergara, Wendy Rosales Rada and Carlos Mario Meléndez Gómez*
Affiliation:
- Organic and Biomedical Chemistry Research Group, Faculty of Basic Sciences, Universidad del Atlántico, Barranquilla, Colombia
Keywords: Cancer, chromatin, histone, DNA, epigenetic inhibitor, epigenoma.
Abstract: DNA is packaged in an octamer of histones, forming chromatin, a complex of DNA and proteins. The structural matrix of a chromosome, chromatin and its changes are now regarded as important factors in controlling gene expression, which has sparked a lot of interest in understanding genetic pathways governing various diseases, including cancer. DNA methylation in the CpG dinucleotide as a transcriptional silencing mechanism, post-translational histone modifications such as acetylation, methylation, and others that affect chromatin structure, ATP-dependent chromatin remodelling, and miRNA-mediated gene silencing are all found to be important in various types of cancer. In this review, we analyze the main alterations in gene expression, epigenetic modification patterns in cancer cells, the main modulators and inhibitors of each epigenetic mechanism, and the molecular evolution of the most representative inhibitors, all of which point to a promising future for HAT, HDAC, non-glycoside DNMT inhibitors, and domain inhibitors.
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Gutiérrez Rodelo Jorseth, Salgado René Mendoza Arturo, Arias De Ávila Marcio, San-Juan-Vergara Homero, Rada Rosales Wendy and Gómez Mario Meléndez Carlos*, Epigenetic Modulators as Treatment Alternative to Diverse Types of Cancer, Current Medicinal Chemistry 2022; 29 (9) . https://dx.doi.org/10.2174/0929867329666211228111036
DOI https://dx.doi.org/10.2174/0929867329666211228111036 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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