Fragments in bromodomain drug discovery

Abstract

Fragment-based approaches have been successfully applied to the discovery and optimisation of ligands for a wide range of targets. These concepts are proving valuable for bromodomain-containing proteins, an emerging family of epigenetic regulators. This review gives examples in which fragment-based drug discovery concepts are helping to find and optimise bromodomain inhibitors, with early successes against the BET subfamily now extending to other members of the target class.