qHTS to Identify Small Molecule GUS Inhibitors

因此，该项目旨在根据一种新的与疾病相关的微生物组目标筛选NCATS的化学库，以确定有希望的目标，这些目标可以进一步开发和优化为未来的共生药物。 在此期间，建立了该项目的合作框架。该项目团队的未来目标包括高通量顺应性分析的微型化和优化，以便能够识别预期的GUS靶向共生药物。随后的工作将集中在HIT验证，随后是针对一系列细菌GUS酶的HIT活性的详细表征。有希望的HIT分子将被提出用于药物化学的SAR驱动优化，以进一步提高其活性和选择性。

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.