G9a inhibitors belong to a class of chemical compounds that specifically target the enzyme G9a, which plays a critical role in epigenetic regulation. Epigenetics refers to modifications in gene expression that occur without changes in the DNA sequence itself. G9a, also known as EHMT2 (euchromatic histone-lysine N-methyltransferase 2), is an enzyme responsible for adding methyl groups to histone proteins, specifically on lysine 9 of histone H3 (H3K9). These methyl groups can act as epigenetic marks, influencing the way DNA is packaged and, consequently, gene expression.
G9a inhibitors are designed to disrupt the activity of the G9a enzyme, preventing it from methylating histone proteins. This inhibition can lead to changes in chromatin structure, making genes more or less accessible to the cellular machinery responsible for gene expression. By altering the epigenetic landscape in this way, G9a inhibitors have the potential to modulate gene expression patterns and influence various cellular processes. Researchers are particularly interested in these compounds for their implications in understanding epigenetic regulation in diseases such as cancer, neurodegenerative disorders, and developmental disorders, as well as for their potential in studying fundamental biological processes like cellular differentiation and embryonic development.