Nucleosome remodeling provides access to genomic DNA for recruitment of the transcriptional machinery to mediate gene expression. The aberrant function of nucleosome remodeling complexes has been correlated to human cancer, making them emerging therapeutic targets. The bromodomain PHD finger transcription factor, BPTF, is the largest member of the human nucleosome remodeling factor NURF. Over the last five years, BPTF has become increasingly identified as a protumorigenic factor, prompting investigations into the molecular mechanisms associated with BPTF function. Despite a druggable bromodomain, small molecule discovery is at an early stage. Here we highlight recent investigations into the biology being discovered for BPTF, chemical biology approaches used to study its function, and small molecule inhibitors being designed as future chemical probes and therapeutics.
Bibliographical noteFunding Information:
This work was supported by the National Institute of General Medical Sciences [R01GM121414-04], the National Institutes of Health Biotechnology Training Grant [5T32GM008347-23, N.M.O], and the University of Minnesota IEM Engineering in Medicine Doctoral Fellowship 2020 (H.Z) for financial support. We would also like to acknowledge BioRender, which was used to create all figures in this report.
© 2021 Elsevier Ltd
- Chemical epigenetics
- Chemical probe
PubMed: MeSH publication types
- Journal Article
- Research Support, N.I.H., Extramural
- Research Support, Non-U.S. Gov't