The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

Epigenetic mechanisms for controlling gene expression through heritable modifications to
DNA, RNA, and proteins, are essential processes in maintaining cellular homeostasis. As a …

Blocking the interactions between bromodomain and extraterminal (BET) proteins and
acetylated lysines of histones by small molecules has important implications for the …

Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively
target one of the two bromodomains in the BET proteins, have begun to emerge in the …

Cancer is frequently dependent on aberrant gene expression programs that might be
vulnerable to targeting with novel therapeutics. Bromodomain and extraterminal domain …

Multiple sclerosis (MS) is a neuroinflammatory autoimmune disease and lacks effective
therapeutic agents. Dysregulation of transcription mediated by bromodomain and extra …

Pan-BD2 inhibitors have been shown to retain an antileukemia effect and display less dose-
limiting toxicities than pan-BET inhibitors. However, it is necessary to consider the potential …

Epigenetics mainly refers to covalent modifications to DNA or histones without affecting
genomes, which ultimately lead to phenotypic changes in cells or organisms. Given the …

Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but
exhibit pharmacology-driven toxicities in clinical trials. The development of domain-selective …

A series of novel heteroaromatic-difluoro-biphenyl-diarylpyrimidines were designed as non-
nucleoside anti-HIV inhibitors targeting reverse transcriptase by a fragment-based …