The goal of this research program is to identify and develop selective small molecule inhibitors of p300 and explore their efficacy in understanding and treating these diseases. During this period, the collaborative team utilized the previously developed HTS-amenable assay to conduct the envisioned high-throughput screen for inhibitors of p300. Screening hits were identified and cherrypicked for validation, and compounds with verified activity are currently being characterized in a number of secondary assays.
|Sorum, Alexander W; Shrimp, Jonathan H; Roberts, Allison M et al. (2016) Microfluidic Mobility Shift Profiling of Lysine Acetyltransferases Enables Screening and Mechanistic Analysis of Cellular Acetylation Inhibitors. ACS Chem Biol 11:734-41|