ARTICLE | Strategy

Expanding into new (bromo)domains

April 17, 2014 7:00 AM UTC

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...