Article
Cell-based protein stabilization assays for the detection of interactions between small-molecule inhibitors and BRD4.
Journal of biomolecular screening - 1 Feb 2015
Schulze Jessica, Moosmayer Dieter, Weiske Joerg, Fernández-Montalván Amaury, Herbst Christopher, Jung Marie, Haendler Bernard, Bader Benjamin
Abstract excerpt
Bromodomain protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) protein family, acts as a central element in transcriptional elongation and plays essential roles in cell proliferation. Inhibition of BRD4 binding to acetylated histone tails via its two bromodomains, BD1 and BD2, with small-molecule inhibitors has been shown to be a valid strategy to prevent cancer growth. We have evaluated and...
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