Identification of small molecule degraders of XPB for inflammatory diseases

炎症性疾病 XPB 小分子降解剂的鉴定

• 批准号: 10688964
• 负责人: Mark Henderson
• 金额: $ 14.62万
• 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/10688964
• 关键词: Biological Assay; Cells; Collaborations; Development; Disease; ERCC3 gene; Extramural Activities; Goals; Inflammatory; Informatics; Modeling; Nuclear Protein; Pharmaceutical Chemistry; Phenocopy; Process; Production; Proteins; Research; Spironolactone; Translations; United States National Institutes of Health; Work; base; cytokine; high throughput screening; screening; small molecule

During this period, the team has developed a strategy for a cell-based high-throughput screen of XPB expression and progressed towards implementing a 1536-well version of the assay for screening. This collaborative team aims to build on previous research by identifying small molecules that phenocopy the effect of spironolactone on XPB protein stability. XPB is a nuclear protein that regulates the production of inflammatory cytokines. The Early Translation Branch's (ETB) overall goal is to uncover and develop new small molecule probes and catalyze the process of early development through a model of collaborative research. With each collaboration, NIH and extramural disease experts work with the ETB's early discovery teams, who specialize in small molecule screening, medicinal chemistry and informatics.

在此期间，该团队开发了一种基于细胞的XPB表达高通量筛选策略，并朝着实施1536孔版本的筛选试验取得了进展。 这个合作团队的目标是在以前的研究基础上，通过鉴定小分子来复制螺内酯对XPB蛋白稳定性的影响。 XPB是一种调节炎症细胞因子产生的核蛋白。早期翻译分支（ETB）的总体目标是发现和开发新的小分子探针，并通过合作研究模式促进早期开发过程。在每次合作中，NIH和校外疾病专家都与ETB的早期发现团队合作，这些团队专门从事小分子筛选，药物化学和信息学。