BET-family bromodomain proteins are important players in the regulation of gene transcription in complex organisms. They have also become prime therapeutic targets for a wide range of human diseases – more than a dozen clinical trials have sprung up in the last few years that are testing BET protein inhibitors.
Our understanding of the biochemistry of these proteins – how they actually work – has lagged considerably behind the excitement about their therapeutic possibilities, and our lab has been working to try to fill in some of the gaps. This work will hopefully improve our understanding of the mechanisms of transcriptional regulation and also perhaps inform future drug discovery efforts in the area.