Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

Innate immunity serves as the rapid and first-line defense against invading pathogens, and
this process can be regulated at various levels, including epigenetic mechanisms. The …

Epigenetic mechanisms, especially DNA methylation and histone modifications, are
dynamic processes that regulate the gene expression transcriptional program in normal and …

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

The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine
residues on histone proteins. The four BET bromodomains—BRD2, BRD3, BRD4, and …

The profound efficacy, yet associated toxicity of pan-BET inhibitors is well documented. The
possibility of an ameliorated safety profile driven by significantly selective (> 100-fold) …

Infiltrating and tissue-resident myeloid cells are essential regulators of innate and adaptive
immunity. During inflammation, and in response to microbial products, these cells can adapt …

Selective inhibitors targeting the first bromodomain (BD1) or the second bromodomain
(BD2) of the bromodomain and extra terminal domain (BET) proteins have triggered …

PBRM1 is a subunit of the PBAF chromatin remodeling complex that uniquely contains six
bromodomains. PBRM1 can operate as a tumor suppressor or tumor promoter. PBRM1 is a …

Pan-bromodomain and extra terminal domain (BET) inhibitors interact equipotently with the
eight bromodomains of the BET family of proteins and have shown profound efficacy in a …