Bromodomain-containing protein 4 (BRD4) belongs to the bromodomain and extra-terminal (BET) family of proteins, which regulate gene expression by binding to acetylated histones and transcription factors and then recruiting other transcriptional regulators. The discovery and development of BET inhibitors have greatly advanced our understanding of the cellular effects of BET proteins and their therapeutic relevance to different diseases. In the field of cardiovascular research, BET bromodomain inhibition by small molecules has been investigated and has demonstrated promising effects on various heart diseases. Whereas results from these preclinical investigations have shown promise, clinical trials are still in early phases at this time. In this review, considering the rapidly expanding evidence for targeting BET family proteins in heart disease, we will summarize the preclinical and clinical investigations of the therapeutic potential of BET bromodomain inhibition in heart disease, with a focus on heart failure and diabetic cardiomyopathy.
BET inhibition, BRD4, Diabetic cardiomyopathy, Heart failure, Mitochondrial homeostasis