Advances in Research on Bromodomain Inhibitors and Their Applications in Human Diseases

Bromodomains (BRDs) are a type of conserved protein domains that recognize acetyl-lysine and facilitate the formation of protein complexes that drive active transcription. N-terminal acetylation or deacetylation of histone lysine modifies the structure of chromatin, thereby regulating transcriptional activation and inhibition. Small-molecule inhibitors of BRDs compete with acetyl-lysine in binding the hydrophobic pocket of BRDs, playing important roles in epigenetic regulation and showing great potential in the treatment of tumor, inflammation, autoimmune diseases and cardiovascular diseases. The progress in BRDs inhibitors and their roles in the treatment of diseases, so as to provide reference for the design and development of efficient and selective small-molecule inhibitors of BRDs.