Target intelligence / Profile preview

Bromodomain PHD finger transcription factor (BPTF)

Target
BPTF
Molecular classification
Transcription factor, Chromatin remodeler, Epigenetic reader, Nucleosome-remodeling factor (NURF) subunit, Bromodomain-containing protein, PHD finger-containing protein
01

Overview

Bromodomain PHD finger transcription factor (BPTF) is a large, multi-domain nuclear protein functioning as the central and largest subunit of the nucleosome-remodeling factor (NURF) complex, a key ATP-dependent chromatin remodeler[1][3][5]. BPTF contains a plant homeodomain (PHD) finger and a bromodomain, enabling it to read specific histone modifications such as H3K4me3 and H4K16ac[1][2][5]. Through its recognition of these epigenetic marks, BPTF facilitates nucleosome sliding and the modulation of chromatin structure, thereby controlling DNA accessibility and transcriptional activity[2][4][5]. BPTF is critical for early embryonic development, lineage specification, and tissue differentiation in mammals[1][2][4]. Genetic alteration or dysregulation of BPTF is implicated in various cancers, including melanoma, lung cancer, neuroblastoma, and bladder cancer, and its overexpression correlates with poor prognosis in several malignancies[2][5]. Additionally, high levels of the protein and certain isoforms have been detected in fetal brain and in neurodegenerative disease states[3][5]. The essential chromatin- and transcription-associated functions of BPTF, and its dysregulation in disease, make it a promising therapeutic target for the development of selective small-molecule inhibitors, though challenges remain due to its indispensability in normal development and tissue homeostasis[1][2].

Other names
Nucleosome-remodeling factor subunit BPTFFAC1FALZNURF301Fetal Alz-50 clone 1 proteinFetal Alzheimer antigenfetal Alz-50 reactive clone 1nucleosome remodeling factor, large subunit
02

Mechanism of action

Inhibition of chromatin association by blocking bromodomain or PHD finger interaction with acetylated or methylated histone tails Disruption of NURF complex formation or chromatin remodeling function

03

Biological functions

Chromatin remodelingEpigenetic regulationGene expression regulationEmbryonic developmentCell fate specificationTissue differentiationTranscriptional control through histone mark recognition
04

Disease associations

CancerNeurodevelopmental disorderNeurodegenerative disease
05

Safety considerations

Potential global dysregulation of gene expression with inhibitionImpact on normal tissue development and cell differentiation due to essential roles in embryogenesisUnknown long-term effects in adult tissues
06

Interacting drugs

Bromodomain inhibitors (experimental; specific drug names are not yet clinically established but several small-molecule inhibitors are under study)
07

Biomarkers

BPTF overexpression (prognostic in cancers such as melanoma, lung cancer, and neuroblastoma)Circ-BPTF (circular RNA; investigated in bladder cancer)

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