Abstract

Epigenetics in Cancer Drug Discovery: Reading the Right Mark

Susanta Samajdar, Vice President, Aurigene Discovery Technologies Limited

Post-translational modifications of histone proteins that are involved in organizing DNA structure influences gene expression both in normal and cancer cells. Acetylation of lysine residues hanging as tails of histone proteins are some of the most important epigenetic modifications of open structure chromatin and active gene transcription. These acetyl marks on histone get recognized by bromodomain and extra-terminal (BET) proteins known as epigenetic readers. Utilizing its tandem bromodomain (BD) modules BET proteins recognize and dock themselves on the acetylated lysine tails thereby helping recruitment of transcription factors and chromatin organizers required in transcription initiation and elongation. Inhibition of acetyl lysine binding ability of BET proteins appears to be an attractive therapeutic target in cancer drug discovery. Sharing some of our recent experience in finding novel leads for this target will be the objective.