qHTS to Identify Small Molecule GUS Inhibitors

National Center For Advancing Translational Sciences

Investigators

Linked publications, trials & patents

Abstract

As such, this project aims to screen the chemical libraries at NCATS against a novel, disease relevant microbiome target to identify promising hits that can be further developed and optimized into tomorrows symbiotic drugs. During this period, the collaborative framework for this project was established. Future goals of the project team include miniaturization and optimization of a high-throughput amenable assay to enable identification of the intended GUS-targeting symbiotic drugs. Subsequent work will focus on hit validation, followed by detailed characterization of hit activity against a diverse panel of bacterial GUS enzymes. Promising hit molecules will be advanced for medicinal chemistry SAR-driven optimization to further improve their activity and selectivity.