Bromodomain and Extraterminal Domain Proteins (BET Proteins)

Bromodomain and Extraterminal Domain Proteins Overview

Bromodomain and extraterminal domain (BET) proteins are a family of proteins, including BRD2, BRD3, BRD4, and BRDT, characterized by two tandem N-terminal bromodomains that recognize acetylated lysine residues on histones, an extraterminal (ET) domain involved in recruiting components of the transcriptional complex, and in some members (BRD4/BRDT), a C-terminal domain important for protein interactions. BET proteins regulate chromatin structure and gene expression, playing crucial roles in cellular processes such as cell cycle progression, proliferation, differentiation, inflammation response, and oncogenesis. Inhibitors of BET proteins block the interaction between bromodomains and acetylated histones, repressing transcriptional programs driven by key oncogenes.

Mechanism of Action

Reversibly binds to bromodomains, preventing interaction with acetylated histones and disrupting chromatin targeting, repressing transcriptional programs.

Biological Functions

Safety Considerations

Interacting Drugs