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Transcriptome analysis of dominant-negative Brd4 mutants identifies Brd4-specific target genes of small molecule inhibitor JQ1.

Scientific reports - 10 May 2017

Decker Tim-Michael, Kluge Michael, Krebs Stefan, Shah Nilay, Blum Helmut, Friedel Caroline C, Eick Dirk

Abstract excerpt

The bromodomain protein Brd4 is an epigenetic reader and plays a critical role in the development and maintenance of leukemia. Brd4 binds to acetylated histone tails and activates transcription by recruiting the positive elongation factor P-TEFb. Small molecule inhibitor JQ1 competitively binds the bromodomains of Brd4 and displaces the protein from acetylated histones. However, it remains unclear whether genes...

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PMID: 28490802
DOI: 10.1038/s41598-017-01943-6
PMCID: PMC5431861

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