Chapter 13: Targeting the Acetylation Reader Family: Bromodomain Proteins

The development of chemical probes for the bromodomain (BRD) and extra terminal (BET) family of BRD-containing proteins has demonstrated that acetylation reader domains are druggable protein interaction domains and major regulators of tissue and disease specific transcription of genes implicated in many diseases. The extraordinary success of BET inhibitors in preclinical models has led to many clinical studies but it has also spurred the development of BRD inhibitors for non-BET family members as well as other structurally diverse acetylation readers such as YEATS (Yaf9, ENL, AF9, Taf14, Sas5) domains. This review summarizes the recent developments in BRD ligands and chemical probes and their potential therapeutic uses.