Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites.

ABSTRACT: Bromodomains are readers of the epigenetic code that specifically bind acetyl-lysine containing recognition sites on proteins. Recently the BET family of bromodomains has been demonstrated to be druggable through the discovery of potent inhibitors, sparking an interest in protein-protein interaction inhibitors that directly target gene transcription. Here, we assess the druggability of diverse members of the bromodomain family using SiteMap and show that there are significant differences in predicted druggability. Furthermore, we trace these differences in druggability back to unique amino acid signatures in the bromodomain acetyl-lysine binding sites. These signatures were then used to generate a new classification of the bromodomain family, visualized as a classification tree. This repre

SUBMITTER: Vidler LR 

PROVIDER: S-EPMC3441041 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature