Selective Targeting of Protein Interactions Mediated by BET Bromodomains

Selective Targeting of Protein Interactions Mediated by BET Bromodomains 

Susanne Muller, Hannah Lingard, and Stefan Knapp 

Histone acetylation is a hallmark of open and accessible chromatin structure, which results in activation of gene transcription. Histone acetylation leads to the recruitment of a number of bromodomain-containing proteins (BRDs) that exclusively recognize e-Af-acetylated lysine residues. These specific protein interaction modules, also called epigenetic reader domains, are evolutionarily highly conserved. The human proteome encodes 61 bromodomain interaction domains present in 42 proteins comprising chromatin modifying enzymes (histone 

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I 20 Selective Targeting of Protein Interactions Mediated by BET Bromodomains 20.3.4.2 Discovery of Benzo- and Thienodiazepines... 

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