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Target intelligence / Profile preview
Bromodomain-containing protein family (BRD2, BRD3, BRD4) (BET family)
- Target
- BET family
- Molecular classification
- Transcription factor, Epigenetic regulator, Chromatin reader, Bromodomain-containing protein
01
Overview
Bromodomain-containing proteins 2, 3, and 4 (BRD2, BRD3, BRD4) are members of the BET (bromodomain and extraterminal domain) family. These proteins are multifunctional transcriptional regulators that play key roles in reading epigenetic marks on chromatin and regulating gene expression. They bind acetylated lysines on histones via their bromodomains, acting as "readers" of epigenetic marks to regulate chromatin structure and gene expression. BRD4 interacts with P-TEFb to promote RNA polymerase II-dependent transcription elongation. Chromosomal translocations involving these genes are implicated in aggressive cancers like NUT midline carcinoma. BET inhibitors target the conserved bromodomains across all three proteins, displacing them from chromatin.
- Other names
- BRD2BRD3BRD4Bromodomain and extraterminal domain (BET) family proteins
02
Mechanism of action
BET inhibitors block the interaction between BET proteins and acetyl-lysine by mimicking acetyl-lysine, displacing BET proteins from chromatin.
03
Biological functions
Transcription regulationEpigenetic regulationCell cycle progressionDNA damage responseChromatin remodeling
04
Disease associations
CancerNUT midline carcinoma
05
Interacting drugs
BET inhibitors
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