qHTS to Identify Small Molecule GUS Inhibitors

qHTS 鉴定小分子 GUS 抑制剂

• 批准号: 10005006
• 负责人: Matthew Hall
• 金额: $ 4.76万
• 依托单位: NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10005006
• 关键词: Bacteria; Beta-glucuronidase; Biological Assay; Disease; Dose-Limiting; Drug toxicity; Enzymes; Future; Goals; Miniaturization; Pharmaceutical Chemistry; Pharmaceutical Preparations; Therapeutic; Toxic effect; Validation; Work; improved; inhibitor/antagonist; microbiome; novel; programs; small molecule; small molecule libraries

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.

因此，该项目旨在针对一种新的疾病相关微生物组靶标筛选NCATS的化学文库，以确定可以进一步开发和优化为明天的共生药物的有希望的命中。 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小型化和优化高通量检测，以识别预期的GUS靶向共生药物。随后的工作将集中在命中验证，然后对不同的细菌GUS酶的命中活性的详细表征。 有前途的命中分子将被推进用于药物化学SAR驱动的优化，以进一步提高其活性和选择性。