What are Bromodomain and Extra Terminal Domain Inhibitors?
Bromodomain and extra terminal domain inhibitors (BETi) are a class of compounds that target the BET family of proteins, which include BRD2, BRD3, BRD4, and BRDT. These proteins are crucial in regulating gene expression by recognizing acetylated lysine residues on histone tails, thus influencing chromatin structure and function. BETi work by binding to the bromodomains of these proteins, preventing their interaction with acetylated histones and thereby disrupting the expression of genes involved in cancer progression.