Epigenetic regulatory proteins known as bromodomains have attracted considerable interest as therapeutic targets in cancer, heart disease, and contraception research. The research in this report focuses on a subset of these bromodomains called BET bromodomains and our efforts towards developing isoform selective inhibitors. In these studies, both a virtual and publically available library were screened against several bromodomain using a combination of fluorescence anisotropy, protein-observed <sup>19</sup>F NMR, and thermal shift assays, revealing a potent class of inhibitors on a novel scaffold. In an effort towards streamlining the screening process, paramagnetic metals were added to reduce the relaxation time and therefore enable a more sensitive experiment. Ultimately, we hope to apply these techniques to the development of a more potent and selective bromodomain inhibitor.

Chemical biology approaches for inhibiting protein recognition of acetylated histones

252nd National Meeting (2016)

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