3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

Abstract

Histone-lysine acetylation is a vital chromatin post-translational modification involved in the epigenetic regulation of gene transcription. Bromodomains bind acetylated lysines, acting as readers of the histone-acetylation code. Competitive inhibitors of this interaction have antiproliferative and anti-inflammatory properties. With 57 distinct bromodomains… (More)
DOI: 10.1021/jm200640v

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