reviewSignal Transduction and Targeted TherapyNov 6, 2023GOLD OA

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

Harbin Medical University · Third Affiliated Hospital of Harbin Medical University · +2 more institutions

PubMed
Indexed incrossrefdoajpubmed

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,…

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