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.
