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.

项目摘要（请参阅说明）： 高通量筛选核心将继续针对定义的目标或表型对小分子库进行筛选。目前，该核心的资源包括超过25万种药物样的化合物以及较小的纯化天然化合物和批准/研究药物的收集，以及使用光学（荧光，吸光度，吸光度，吸收性， 发光）测定。核心的功能包括化合物存储和处理，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完成经过验证的“命中”（具有针对定义目标或表型活性的化合物）的初步优化。 在与核心协商的单个项目中，进一步的“命中”开发是进行的。在当前项目期间，该核心已被广泛使用，并成功地识别和表征了新型离子转运蛋白和感染的调节剂。 28个正在进行的和新的CF相关项目将大量利用核心。