SBIR Phase II: High-Throughput Purification of Combinatorial Libraries

SBIR 第二阶段：组合文库的高通量纯化

• 批准号: 0321765
• 负责人: Jack Syage
• 金额: $ 50万
• 依托单位: SYAGEN TECHNOLOGY INC
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2003
• 资助国家: 美国
• 起止时间: 2003-07-01 至 2006-06-30
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=0321765&HistoricalAwards=false
• 关键词: SBIR; Phase; II; Throughput; Purification

This SBIR Phase II project aims to develop a prototype of a highly-parallel, mass-selected purification system for large pharmaceutical drug libraries. High-throughput purification is driven by the industry recognition that combinatorial chemistry samples must still be purified even after chemical screening. This project will examine monolithic parallel preparative liquid chromatography configurations. The key enabling technology is low-pressure photoionization mass spectrometry (LPPI MS), which permits accurate molecular detection in mixtures of compounds without the problems of competition-for-charge and ion suppressions that plague conventional ionization methods. A practical purification rate of 1 sample/min (12 parallel purifications in 12 min column cycle time) corresponding to a potential 16-hr daily rate of 960 sample purifications/day is expected. This work will transition into a Phase II prototype involving strategic partners to commercialize the technology. The proposed high throughput purification system for combinatorial libraries has the potential to dominate an important niche market for molecular analysis and screening for drug discovery. This rapidly growing market will fuel applications in many other directions of drug development. The proposed activity will have a broad and profound impact on society as a whole by providing valuable information that can lead to improved drug therapy and early detection of disease. The practical outcome is to improve health care and reduce costs. This project also has the potential for explosive commercial growth, which will stimulate economic development.

该SBIR第二阶段项目旨在为大型药物库开发高度并行的质量选择纯化系统的原型。高通量纯化是由行业认识驱动的，即即使在化学筛选之后，组合化学样品仍然必须被纯化。本计画将检视整体式平行制备液相层析配置。关键的使能技术是低压光电离质谱法（LPPI MS），它允许在化合物的混合物中进行精确的分子检测，而没有困扰传统电离方法的电荷竞争和离子供应的问题。预计实际纯化速率为1份样品/min（在12 min色谱柱循环时间内进行12次平行纯化），对应于960份样品纯化/天的潜在16 h日速率。这项工作将过渡到第二阶段的原型，涉及战略合作伙伴，以使该技术商业化。所提出的组合文库的高通量纯化系统有可能主导用于药物发现的分子分析和筛选的重要利基市场。这个快速增长的市场将推动药物开发的许多其他方向的应用。 拟议的活动将对整个社会产生广泛而深刻的影响，因为它提供了宝贵的信息，有助于改进药物治疗和早期发现疾病。实际结果是改善医疗保健和降低成本。该项目还具有爆炸性商业增长的潜力，这将刺激经济发展。