Harnessing massive peptide libraries to explore the inhibition of epigenetic drug targets

Epigenetic regulators finely tune gene regulation in a healthy cell, but their misregulation frequently contributes to disease. In many cases, however, achieving selective inhibition has been challenging, due to the presence of a multiple, closely-related isoforms. Cyclic peptides are an emerging class of natural product-like drugs with diverse structures that can easily be adapted to potently and selectively target any protein of interest. This talk will discuss the use of the RaPID system, a trillion member cyclic peptide discovery platform, to develop potent and selective modulators of two epigenetic drug targets: the rheumatoid arthritis target, PADI4, and the cancer targets, the BET bromodomains.