权益分类	功能权益	普通用户	{{item.name}}会员
{{category.name}}	{{benefitItem.name}}

Administration and Mgmt (California)

行政和管理（加利福尼亚州）

基本信息

批准号：
8538720
负责人：
HUGH ROSEN
金额：
$ 94.88万
依托单位：
SCRIPPS RESEARCH INSTITUTE, THE
依托单位国家：
美国
项目类别：
财政年份：
2012
资助国家：
美国
起止时间：
2012-06-01 至 2014-05-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8538720
关键词：
Affinity Automation Binding Biochemical Biochemical Pathway Biological Assay Biology California Cells Chemicals Chemistry Collection DNA Databases Detection Development Enzymes Florida Fluorescence Resonance Energy Transfer Home environment Hydrolase Information Technology Insecta Ions Isomerase Kinetics Libraries Ligase Lyase Mammalian Cell Membrane Potentials Molecular Molecular Bank Molecular Target Oxidoreductase Parasites Pharmaceutical Chemistry Pharmaceutical Preparations Production Protein Conformation Proteins PubChem Quality Control RNA Reporter Genes Reporting Research Institute Sampling Screening Result Screening procedure Second Messenger Systems System Testing Toxic effect Transferase United States National Institutes of Health Writing Yeasts base cheminformatics drug discovery drug market high throughput screening protein protein interaction receptor repository second messenger small molecule transcription factor

项目摘要

High Throughput Screening (HTS) leverages automation, chemistry, biology and information technologies to rapidly assay the pharmacologic activity of drug-like molecules. As applied to drug discovery, it has been successful for discovering the precursors of marketed drugs as well as probes of various cellular and biochemical pathways. Scripps Florida is the home of the "ultra" HTS (uHTS) Implementation core of the Scripps Research Institute Molecular Screening Center (SRIMSC). Core staff are responsible for developing and implementing the SRIMSC's screening assays, managing the Molecular Libraries Small Molecule Repository (MLSMR) screening collection of >360,000 samples, screening the MLSMR library at a throughput in excess of 1 million samples per day, quality control & reporting of all screening results to the NIH's publically available database (PubChem), cheminformatics support and overall project management for the SRIMSC. The core sustains full production capabilities for the NIH by screening the entire MLSMR compound library against more than 25 unique targets per year. As of this writing core staff have completed more than 185 high throughput screening campaigns for 175 molecular targets, with more than 40 million wells tested. Staff also execute lower-throughput bioassays to support the SRIMSC's hit-to-probe medicinal chemistry efforts, participating in more than 50 probe development projects per year. Target classes screened by the core include receptors, transcription factors, transferases, hydrolases, oxidoreductases, lyases, isomerases and ligases; protein interactions (protein-protein, protein-DNA, and protein-RNA) and phenotypic bioassays. Targets have been purified for screening (e.g. enzymes or proteins) or assayed in whole-cell mammalian, bacterial, insect, yeast/fungal, and parasite systems. Screening formats include biochemical enzymatic & binding affinity assays, as well as whole-cell reporter gene, second messenger, membrane potential, ion flux, complementation, protein conformation, renaturation and toxicity assays. A variety of plate-based detection formats including kinetic (FLIPR, Alphascreen, TR-FRET, FP etc.) and high content analysis (HCA) are utilized for screening efforts. More information can be found at: http://hts.florida.scripps.edu/

高通量筛选（HTS）利用自动化、化学、生物学和信息技术来快速测定药物样分子的药理活性。应用于药物发现，它已成功地发现上市药物的前体以及各种细胞和生化途径的探针。佛罗里达斯克里普斯是斯克里普斯研究所分子筛选中心（SRIMSC）“超级”HTS（uHTS）实施核心的所在地。核心工作人员负责开发和实施SRIMSC的筛选测定，管理分子库小分子库（MLSMR）筛选收集> 360，000个样品，筛选MLSMR库，每天的通量超过100万个样品，质量控制和将所有筛选结果报告给NIH的药物可用数据库（PubChem），化学信息学支持和SRIMSC的整体项目管理。该核心通过每年针对超过25个独特靶标筛选整个MLSMR化合物库来维持NIH的全部生产能力。截至撰写本文时，核心工作人员已经完成了175个分子靶点的185次高通量筛选活动，测试了超过4000万个威尔斯孔。工作人员还执行低通量生物测定，以支持SRIMSC的命中探针药物化学工作，每年参与50多个探针开发项目。核心筛选的靶类别包括受体、转录因子、转移酶、水解酶、氧化还原酶、裂解酶、异构酶和连接酶;蛋白质相互作用（蛋白质-蛋白质、蛋白质-DNA和蛋白质-RNA）和表型生物测定。已经纯化了靶标用于筛选（例如酶或蛋白质）或在全细胞哺乳动物、细菌、昆虫、酵母/真菌和寄生虫系统中测定。筛选形式包括生化酶和结合亲和力测定，以及全细胞报告基因、第二信使、膜电位、离子通量、互补、蛋白质构象、复性和毒性测定。各种基于板的检测形式，包括动力学（FLIPR，Alphascreen，TR-FRET，FP等）和高含量分析（HCA）用于筛选工作。更多信息请访问：http://hts.florida.scripps.edu/