BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications.

ABSTRACT: The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. They are epigenetic readers of histone acetylation with broad specificity. BET proteins are linked to cancer progression due to their interaction with numerous cellular proteins including chromatin-modifying factors, transcription factors, and histone modification enzymes. The spectacular growth in the clinical development of small-molecule BET inhibitors underscores the interest and importance of this protein family as an anticancer target. Current approaches targeting BET proteins for cancer therapy rely on acetylation mimics to block the bromodomains from binding chromatin. Howeve

SUBMITTER: To KKW 

PROVIDER: S-EPMC10096006 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature