Expanding into new (bromo)domains

The Neomed Institute has begun development of its first cancer therapeutic, a bromodomain containing 4 inhibitor from Epigenetix Inc. that the not-for-profit organization thinks could have a selectivity advantage over competing molecules.

Bromodomain-containing proteins are a class of epigenetic regulators. These domains bind to histones in which lysine residues are modified by an acetyl group to regulate chromatin remodeling and gene transcription.^1,2 Two independent papers in Nature in 2010 first showed the potential druggability of bromodomains by identifying JQ1 and I-BET as selective inhibitors of the BET bromodomain family, which includes bromodomain containing 2 (BRD2), BRD3 and BRD4.^3,4...