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Target intelligence / Profile preview
Bromodomain and PHD finger-containing protein 3 (BRPF3)
- Target
- BRPF3
- Molecular classification
- Chromatin reader, Scaffold protein, Histone modification, Other (Epigenetic regulator)
01
Overview
Bromodomain and PHD finger-containing protein 3 (BRPF3) is a multivalent chromatin reader and scaffold protein that regulates epigenetic functions in the cell nucleus. BRPF3 contains a bromodomain, two plant homeodomain (PHD) fingers, and a PWWP domain, and serves as a central component of the HBO1 (MYST2/KAT7) histone acetyltransferase complex. It preferentially facilitates acetylation of nucleosomal histones H3 and H4 by HBO1, and specifically targets H3K14 for acetylation, promoting DNA replication and regulating the temporal firing of replication origins. BRPF3 is also involved in transcriptional regulation and embryonic stem cell pluripotency and functions as a key regulator of gene expression and chromatin structure. Its distinct interactions and activities differentiate it from its paralogs BRPF1 and BRPF2. Perturbation of BRPF3 function is associated with defects in DNA replication and is linked to some developmental disorders and a potential role in cancer biology[1][2][3][5].
- Other names
- BRPF3KIAA1286bromodomain and PHD finger containing 3bromodomain and PHD finger-containing protein 3
02
Mechanism of action
Modulates substrate specificity and stimulates enzymatic activity of HBO1/MYST2 histone acetyltransferase complex; regulates acetylation of histone H3 at lysine 14 (H3K14ac), affecting chromatin structure and DNA replication origin activation
03
Biological functions
Chromatin modificationDNA replicationGene regulationPositive regulation of DNA replicationEmbryonic developmentCell differentiationMaintenance of pluripotency in stem cells
04
Disease associations
CancerDevelopmental disorders (associated with Lethal Congenital Contracture Syndrome 2)Other (evidence of altered function in disease, but not a direct major disease gene to date)
05
Safety considerations
Safety/therapeutic challenges mostly theoretical; broad chromatin-modifying roles suggest potential for effects on global gene expression and genomic stability if targeted.Knockout in mice does not result in gross developmental lethality, suggesting non-essential function for survival but potential subtler risks.
06
Interacting drugs
none identified directly; no targeted therapeutics currently established
07
Biomarkers
H3K14ac (histone H3 acetylation at lysine 14, as a functional readout of BRPF3-HBO1 complex activity)
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