Target intelligence / Profile preview

Bromodomain-containing protein 8 (BRD8)

Target
BRD8
Molecular classification
Bromodomain-containing protein, Epigenetic reader, Histone modification protein, Nuclear receptor coactivator, Accessory subunit of histone acetyltransferase complex
01

Overview

Bromodomain-containing protein 8 (BRD8) is a nuclear protein encoded by the BRD8 gene, characterized by the presence of one or two bromodomains which recognize acetylated lysine residues on histones and transcription factors. BRD8 functions as an accessory subunit of histone acetyltransferase complexes such as NuA4/TIP60, where it regulates chromatin structure, genome stability, and gene expression in concert with other complex members. As a nuclear receptor coactivator, it modulates transcription driven by thyroid hormone, androgen, estrogen, glucocorticoid, progesterone, and retinoid X receptors, among others. BRD8 plays a prominent role in cell cycle progression, DNA repair, and cell proliferation, particularly in cancers where it is frequently overexpressed and promotes resistance to cytotoxic therapies. BRD8 is under investigation as an epigenetic and oncologic therapeutic target due to its pivotal role in chromatin regulation and cancer cell survival[1][2][3][4][5].

Other names
SMAPSMAP2TrCP120p120Skeletal muscle abundant proteinSkeletal muscle abundant protein 2Thyroid hormone receptor coactivating protein of 120 kDathyroid hormone receptor coactivatortrCP120
02

Mechanism of action

Small molecule inhibitors of bromodomains block acetyl-lysine recognition and transcriptional coactivation functions\nTargeting BRD8 can suppress cell proliferation and induce cell cycle arrest and apoptosis in cancer models[1][2][4].

03

Biological functions

Chromatin modification and remodelingTranscriptional regulationNuclear receptor coactivationCell cycle progressionDNA repairCell proliferationApoptosis regulation
04

Disease associations

CancerDrug resistance (notably to spindle poisons and proteasome inhibitors)Other (potential relevance in other proliferative or chromatin-modification related disorders)
05

Safety considerations

Limited clinical dataPotential safety concerns may stem from broad roles in chromatin biology and gene regulation, suggesting the risk of adverse effects on genomic stability and normal cell proliferation with pan-bromodomain or chromatin-modulating therapies[1][2][4].
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Interacting drugs

No clinically approved drugs are currently listed that directly target BRD8. However, the protein is considered a promising target for the development of bromodomain inhibitors[1][2][4].
07

Biomarkers

Increased BRD8 expression in tumor tissues (notably colorectal cancer) can potentially serve as a biomarker for disease progression and drug sensitivity[1][2][4].

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