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Updated: Mar 15, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Recent Progress and Prospect in Studying Selective Inhibitors Toward Bromodomain Family Members
Jianzhong Chen1, Yu'e Huang2, Jian Wang1
1School of Science, Shandong Jiaotong University, Jinan 250357, China.
Abstract:
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.
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