Recent Progress and Prospect in Studying Selective Inhibitors Toward Bromodomain Family Members

Bromodomain (BRD)-containing proteins are gaining attention as key targets in epigenetic drug development. BRDs bind to acetylated lysine residues on histones and Other proteins, significantly impacting transcriptional regulation and chromatin remodeling. As our grasp of bromodomain structures and biochemistry deepens, the momentum behind developing small-molecule inhibitors for these BRD domains is triggered and potent inhibitors targeting different family members of BRDs are proposed. In addition, computational simulations have also played a significant role in advancing inhibitor design for the BRD family. This review delves into recent breakthroughs in small-molecule BRD receptor inhibitors and computational studies, spotlighting their biological impact and therapeutic potential, and outlining the research road ahead. This review is expected to provide guidance for future drug design of BRD inhibitors.

bromodomain; deep learning; gatekeeper residue; selective inhibitors.