Bromodomains on the brain

A Dana-Farber Cancer Institute-led team has found that neuroblastomas with MYCN amplification, which occurs in about 25% of pediatric brain tumors, are sensitive to small molecule inhibitors of the BET family of bromodomains.¹ The findings provide a genetic marker for this emerging epigenetic target, and GlaxoSmithKline plc already is using MYCN amplification as one criterion to select patients for a Phase I trial of its BET bromodomain inhibitor in cancer.

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...