Abstract

Histone acetylation by chromatin-modifying enzymes enables differential gene expression across tissues and cell types in response to external stimuli. This modification is recognised by epigenetic readers such as bromodomain-containing proteins which then recruit additional factors to drive transcription. The development of small molecule tool compounds, also referred to as chemical probes, that disrupt the bromodomain-histone interaction have greatly facilitated further functional studies evaluating the involvement of bromodomain-containing proteins in physiology and disease and accelerated the development of inhibitors for potential therapeutic applications. This talk will focus on a few recent case studies involving novel chemical probes and highlight the complementarity of high quality tool compounds and genetic approaches for drug target validation