High Throughput Screening of HIV Entry Inhibitors (RMI)

HIV 进入抑制剂 (RMI) 的高通量筛选

• 批准号: 7021829
• 负责人: Michael S. Caffrey
• 金额: $ 7.75万
• 依托单位: UNIVERSITY OF ILLINOIS AT CHICAGO
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-09-30 至 2007-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7021829
• 关键词: HIV envelope protein gp120; HIV envelope protein gp41; HeLa cells; antiviral agents; bioassay; biotechnology; colorimetry; drug discovery /isolation; high throughput technology; host organism interaction; human immunodeficiency virus; lead; protein binding; protein protein interaction; proteomics; robotics; small molecule; ultracentrifugation; virus envelope; virus infection mechanism; virus protein

DESCRIPTION (provided by applicant): Human immunodeficiency virus (HIV) enters target cells by specific interactions between the viral envelope proteins gp41 and gp120 and human target cell receptors. The long term goal of this project is to discover small, drug-like, molecules that disrupt HIV entry by binding to viral envelope or human target cell receptor proteins. The specific aims are: Specific Aim 1: Develop the pseudo typing assay of HIV envelope-mediated viral entry for application to high throughput screening (HTS) of small drug-like molecules by robotic systems. Specific Aim 2: Extend the HIV entry assay for discrimination between small molecule inhibitors that bind to HIV envelope proteins, from small molecule inhibitors that bind to human target receptor proteins.

描述（由申请人提供）：人类免疫缺陷病毒（HIV）通过病毒包膜蛋白gp41和gp120与人类靶细胞受体之间的特异性相互作用进入靶细胞。该项目的长期目标是发现通过结合病毒包膜或人类靶细胞受体蛋白来阻断HIV进入的类似药物的小分子。具体目标：1：开发HIV包膜介导病毒进入的伪分型试验，用于机器人系统高通量筛选小药物样分子。特异性目标2：扩展HIV进入测定，以区分结合HIV包膜蛋白的小分子抑制剂和结合人类靶受体蛋白的小分子抑制剂。