Chromatin targeting: A BET inhibitor workaround

The bromodomain structural motifis found in proteins that bind to acetylated lysine residues, which are predominantly present on histones. Thereare 46 proteins in the human genome known to contain at least one bromodomain motif; these proteins impact chromatin architecture, and many regulate transcr...

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Bibliographic Details
Published inNature chemical biology Vol. 12; no. 7; pp. 469 - 470
Main Author Burns, Christopher J
Format Journal Article
LanguageEnglish
Published United States Nature Publishing Group 01.07.2016
Subjects
Chromatin
Genomes
Genotype & phenotype
Humans
Nuclear Proteins
Proteins
Transcription Factors - genetics
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Summary:The bromodomain structural motifis found in proteins that bind to acetylated lysine residues, which are predominantly present on histones. Thereare 46 proteins in the human genome known to contain at least one bromodomain motif; these proteins impact chromatin architecture, and many regulate transcriptional activity1. Therapeutic targeting of bromodomain proteins is of increasing interest, though to date it has been largely focused on inhibition of the BET bromodomain family member BRD4, as preclinical evidence has shown that this controls the expression of well-known oncogenic transcription factors such as MYC and FOSL1. Sdelci et al.2 now reporta new screen that has resulted in the identication of a compound that modulates BRD4-mediated transcription through inhibition of an alternative bromodomain-containing protein, TAF1.
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ISSN:1552-4450
1552-4469
DOI:10.1038/nchembio.2107