Chromosomal translocations-leading to the expression of fusion genes-are well-studied
genetic abberrations associated with the development of leukemias. Most of them represent …

Developmental transitions are guided by master regulatory transcription factors. During
adipogenesis, a transcriptional cascade culminates in the expression of PPARγ and …

Background: Histone acetylation is an essential approach of post-translational modification
(PTM) and a significant component of epigenetic regulation that is mediated by …

Bromodomain and plant homeodomain (PHD) finger containing protein 1 (BRPF1) is a
member of subfamily IV of the human bromodomains. Experimental evidence suggests that …

Ligands for the bromodomain and extra-terminal domain (BET) family of bromodomains
have shown promise as useful therapeutic agents for treating a range of cancers and …

The bromodomain and extra-terminal proteins (BET) have emerged as promising
therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We …

Compound 1 bearing with benzo [cd] indol-2 (1H)-one scaffold was identified as an effective
BRD4 inhibitor through the AlphaScreen-based high-throughput screening and its high …

A combination approach of a fragment screening and “SAR by catalog” was used for the
discovery of bromodomain-containing protein 4 (BRD4) inhibitors. Initial screening of 3695 …

Recently, several kinase inhibitors were found to also inhibit bromodomains, providing a
new strategy for the discovery of bromodomain inhibitors. Along this line, starting from PLK1 …

Prostate cancer is a commonly diagnosed cancer and a leading cause of cancer-related
deaths. The bromodomain and extra terminal domain (BET) family proteins have emerged …