COBRE: UKS: CORE B: HIGH THROUGHPUT SCREENING & TARGET IDENTIFICATION

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 高通量筛选(HTS)已成为生物医学研究的有力工具和药物发现的资源。HTS的目的是筛选大量选择性地与生物靶标相互作用的小分子，以便将它们用作探针，以了解新鉴定的蛋白质的功能，并分析生理过程、细胞现象和疾病机制。堪萨斯大学的HTS实验室(www.hts.ku.edu)是通过Cobre赠款建立的，为Cobre研究人员以及当地和全国研究界提供服务。我们一直支持并将继续支持Cobre研究人员，还将扩大我们的高通量筛查的范围和能力，以满足生物医学研究人员日益增长的需求。我们的目标是(1)加强我们的检测开发能力，以进口生化和基于细胞的检测并将其调整为HTS格式，以及(2)加强我们的高通量筛选能力，以开展有效的筛查活动。我们与个别研究人员合作，调整他们的台式分析以适应HTS操作，并使用这些成功改装的HTS分析来筛选我们现有的小分子有机化合物化学库，以显示生物活性。由于堪萨斯大学现有的HTS设施和人员，我们确信，进一步的扩张将为发现新的有趣的化合物以及从HTS的原始命中衍生出的类似物的设计、合成和评估做出重大贡献。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. High throughput screening (HTS) has become a powerful tool for biomedical research and a resource for drug discovery. The purpose of HTS is to screen large numbers of small molecules that interact selectively with biological targets so that they may be used as probes to understand the function of newly characterized proteins and to analyze physiological e processes, cellular phenomena, and disease mechanisms. The HTS laboratory at the University of Kansas (www.hts.ku.edu) was established through the COBRE grant and has provided service to COBRE investigators, and the local and national research community. We have supported and will continue to support COBRE investigators and will also expand both the scope and capacity of our high throughput screening to meet the increased needs of biomedical researchers. Our objectives are (1) to strengthen our assay development capacity to import and adapt biochemical and cell-based assays to HTS format and (2) to strengthen our high throughput screening capacity to carry out efficient screening campaigns. We work with individual research investigators to adapt their bench-top assays to suit HTS operation and use these successfully adapted HTS assays to screen our existing chemical library of small organic compounds for molecules showing biological activity. Because of the existing HTS facility and personnel at the University of Kansas, we are certain that further expansion will make significant contributions toward the discovery of new interesting compounds and toward the design, synthesis and evaluation of analogues derived from original hits coming from HTS.