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Target intelligence / Profile preview
Bromodomain and Extra-Terminal Domain (BET) Family Proteins (BET Family)
- Target
- BET Family
- Molecular classification
- Epigenetic reader, Transcription factor
01
Overview
Bromodomain and Extra-Terminal Domain (BET) family proteins are epigenetic "reader" proteins that play a central role in regulating gene transcription by recognizing acetylated lysine residues on histone tails, thereby influencing chromatin structure and gene expression. The mammalian BET family includes BRD2, BRD3, BRD4, and BRDT. They facilitate assembly of the transcriptional machinery at active chromatin regions, regulate cellular proliferation, differentiation, immune responses, and cell cycle progression, and act as scaffolds for recruitment of coactivators or elongation factors such as P-TEFb. Aberrant BET protein activity is linked to various diseases, including cancer, where overexpression or dysregulation can drive tumorigenesis.
- Other names
- Extra-terminal domain-containing proteinsBRD2BRD3BRD4BRDT
02
Mechanism of action
Inhibition of bromodomain binding to acetylated lysines, disrupting BET protein interaction with chromatin and downstream signaling.
03
Biological functions
Gene transcription regulationChromatin remodelingCellular proliferationCell differentiationImmune responseCell cycle progression
04
Disease associations
CancerInflammationMultiple sclerosisCardiovascular diseaseViral infection
05
Interacting drugs
BET inhibitors (small-molecule)
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