Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy.

ABSTRACT: BET proteins, which influence gene expression and contribute to the development of cancer, are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic anticancer treatment. Although preliminary clinical trials have shown the anticancer potential of BET inhibitors, it appears that these drugs have limited effectiveness when used alone. Therefore, given the limited monotherapeutic activity of BET inhibitors, their use in combination with other drugs warrants attention, including the meaningful variations in pharmacodynamic activity among chosen drug combinations. In this paper, we review the function of BET proteins, the preclinical justification for BET protein targeting in cancer, recent advances in small-molecule BET inhibitors, and preliminary clinical trial fi

SUBMITTER: Wang ZQ 

PROVIDER: S-EPMC10625992 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature