Epigenetics has emerged as a promising frontier in the quest to effectively treat various human diseases. It involves modifications to DNA or DNA-associated proteins, like histones, without altering the DNA sequence itself. These modifications play a pivotal role in determining whether a gene is active or inactive, as well as the level of its activity. Remarkably, this pattern of modifications varies across different cells and organs in the body and can respond to diverse physiological stimuli. Increasing evidence supports the notion that disruptions in these epigenetic patterns contribute to the development of multiple diseases, as the level of gene activity often determines the delicate balance between a healthy physiology and disease onset. Consequently, the realm of epigenetics has become a captivating frontier for the exploration of novel therapeutic interventions.
Three primary types of epigenetic modifications to DNA and DNA-associated proteins are acetylation, methylation, and phosphorylation. These modifications are catalyzed by specialized enzymes called “writers,” while other enzymes known as “erasers” remove them.
Furthermore, “reader” proteins play a critical role in epigenetic regulation. Rather than modifying histone marks, these “reader” proteins recognize specific patterns of modifications and recruit additional proteins to regulate gene activity. Various protein domains have been identified for this purpose, with bromodomains being one of them.
In this context, Zenith focuses on a specific group of “reader” proteins called BET (Bromodomain and ExtraTerminal domain) proteins. These BET proteins present a promising therapeutic target due to their ability to regulate disease markers at the gene expression level. Among the four members of this protein family, namely BRD2, BRD3, BRD4, and BRDT, BRD4 has demonstrated particularly strong associations with the regulation of critical genes involved in cancer, autoimmune diseases, and cardiovascular disorders. This makes BRD4 an attractive candidate for potential therapeutic interventions in these pathologies.
reference: https://www.zenithepigenetics.com/Sci…/what-is-epigenetics and EL-Sayed Mahgoub