Identification of small molecule inhibitors of USP8

National Center For Advancing Translational Sciences

Investigators

Abstract

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 has screened several additional small-molecule libraries to identify novel chemotypes exhibiting inhibitory activity towards USP8. 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.