Identification of small molecule inhibitors of DUB3

National Center For Advancing Translational Sciences

Investigators

Abstract

The goal of this project to identify compounds that can selectively inhibit DUB3 through a de novo chemical screen of compounds from NCATS collections. During this reporting period, the collaborative research team optimized and implemented a high-throughput biochemical assay and screened NCATS compound collections for selective DUB3 inhibitors. The identified hits have been validated in cellular assays for their effect on ER and AR levels, and a medicinal chemistry campaign has been initiated for the most promising chemotypes.