Abstract

CURRENT KNOWLEDGE OF BET INHIBITOR AS A TARGET OF BROMODOMAIN IN EPIGENETIC REGULATION- REVIEW ARTICLE

Kamrudeen Samani*, Uday Raj Sharma, Abhishek Raj Joshi, Surendra V., Manjunath P. M. and Md. Imran Mansur

Abstract

The structure of bromodomain consist of 110 amino acid, acts as a ‘reader’ for recognizing an acetylated lysine residue on N-terminal of histones tails and acetylated lysine responsible for uncoiling of chromatin structure feature of DNA, shows positive transcriptional elongation and helps in promoting transcriptional and chromatin remodeling. It was found that novel identified molecules has ability to alter effect of prostate cancer mainly in gene encoding process and helps in regulation of chromatin biology in epigenetic regulation. The bromodomain family that is BET inhibitors, disrupt the binding sites of proteins to acetylated histones help in preventing employ of RNA polymerase 2 to enhancers and promoters, especially super-enhancers, to inhibit gene transcription. The Bet inhibitors play essential role in treatment of both cancer and inflammatory disease. We review and update a key role of epigenetic therapy that targets the BET bromodomain, prostate cancer progression, therapy resistance and biomarkers.

Keywords: bromodomain, chromatin, epigenetic, inflammatory disease.