Core A Verkman Screening Core

核心 A Verkman 筛选核心

• 批准号: 8564917
• 负责人: ALAN S VERKMAN
• 金额: $ 16.07万
• 依托单位: UNIVERSITY OF CALIFORNIA, SAN FRANCISCO
• 依托单位国家: 美国
• 财政年份: 2012
• 资助国家: 美国
• 起止时间: 2012-06-01 至 2015-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8564917
• 关键词: Biological Assay; Collection; Consultations; Data Analyses; Development; Fluorescence; Individual; Infection; Instruction; Investigational Drugs; Ions; Lead; Optics; Pharmaceutical Preparations; Phase; Phenotype; Research Personnel; Resources; Screening procedure; Solutions; Synthesis Chemistry; Validation; analog; base; design; high throughput screening; instrumentation; luminescence; novel; small molecule; small molecule libraries

PROJECT SUMMARY (See instructions): The high-throughput screening core will continue to carry out screening of small-molecule libraries against defined targets or phenotypes. Resources of the core at present include more than 250,000 drug-like compounds and smaller collections of purified natural compounds and approved/investigational drugs, and automated instrumentation for high-throughput screening utilizing optical (fluorescence, absorbance, luminescence) assays. Functions of the core include compound storage and handling, assay design and validation, assay execution, and data analysis. Initial optimization of validated 'hits' (compounds with activity against defined targets or phenotypes) is done by screening of commercially purchased compound analogs. Further 'hit-to-lead' development is done in individual projects in consultation with the core. The core has been utilized extensively during the current project with successful identification and characterization of novel modulators of ion transporters and infection. The core will be heavily utilized by 28 ongoing and new CF related projects.

项目总结（见说明）： 高通量筛选核心将继续针对确定的靶标或表型进行小分子文库的筛选。目前核心的资源包括超过250，000种药物样化合物和纯化的天然化合物和批准/研究药物的较小集合，以及利用光学（荧光，吸光度， 发光）测定。核心的功能包括化合物储存和处理、测定设计和验证、测定执行和数据分析。通过筛选商业购买的化合物类似物来进行经验证的“命中物”（具有针对定义的靶标或表型的活性的化合物）的初始优化。 与核心协商，在各个项目中进行进一步的“击中领先”开发。该核心已被广泛使用，在当前的项目中，成功地识别和表征了离子转运蛋白和感染的新型调节剂。核心资源将被28个正在进行的和新的与气候变化有关的项目大量利用。