Bromodomain Inhibition and Its Application to Human Disease

摘要: Abstract Bromodomains (BRDs) are small epigenetic reader modules that recognize and selectively bind acetylation marks of histones. The human proteome contains 46 unique bromodomain-containing proteins with a total 61 BRDs. Despite their highly conserved sequences structures, BRDs diverse array acetylated residues. Since the discovery first selective bromodomain extraterminal domain (BET) BRD inhibitors JQ1 I-BET762, there has been an explosion research on due to translational potential as targets for treatment numerous diseases including cancers, inflammation cardiovascular disease, invasive infections by parasites, pathogenic fungi or viruses. Recent advances challenges in creation this emerging new class drugs discussed.