The bromodomain and extraterminal (BET) proteins are a bromodomain subfamily that includes BRD2, BRD3, BRD4, and BRDT.1
The BET proteins utilize the bromodomains to interact with acetylated histone tails of chromatin to mediate downstream functions, such as histone acetylation, chromatin remodeling, and transcriptional regulation.1,3,6
BET family proteins are involved in promoting aberrant oncogene expression in a variety of cancers.7-10
Overexpression and gain-of-function mutations of BET proteins can alter gene transcription, histone modification, DNA repair, and apoptosis.1
BET inhibitors have shown promise in both a variety of solid tumors as well as hematologic malignancies.3,16
The BET family of proteins may be involved in the pathogenesis of AML, particularly in AML harboring mutations in NPM1 and MLL.12
Additionally, the BET family of proteins likely promotes oncogenesis through a number of shared pathways activated in FLT3 AML, including STAT5, AKT, and ERK.9,12
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