ARTICLE | Targets & Mechanisms

Doubling the BET

December 2, 2010 8:00 AM UTC

Less than seven weeks after a group of academics reported the first potent bromodomain inhibitor1 and showed the molecule's efficacy in cancer, a separate group of researchers at GlaxoSmithKline plc and The Rockefeller Universityhas generated a selective bromodomain inhibitor that has therapeutic activity in preclinical models of sepsis and endotoxic shock.2

Proteins that contain bromodomains provide a scaffold for the assembly of chromatin complexes that modulate gene expression, including increasing the expression of inflammatory genes...