The long term goal of this proposed research program is to develop small molecule chemical probes to inhibit USP8 for basic research and therapeutic purposes. During this period, the collaborative team worked to optimize and implement automated quantitative high-throughput screening (qHTS) of several small molecule libraries. In addition, orthogonal assays were identified and developed to enable further validation of potential USP8 inhibitors identified in the primary screen. Future work will focus on pursuing medicinal chemistry optimization of select hit molecules to further improve their potency, selectivity and other characteristics.
