Fluorous Solution-Phase Synthesis of Peptides

肽的氟溶液相合成

• 批准号: 6993221
• 负责人: NICOLA L. B. POHL
• 金额: $ 17.03万
• 依托单位: FLUOROUS TECHNOLOGIES, INC.
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-08-01 至 2007-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6993221
• 关键词: carbopolycyclic compound; chemical synthesis; chromatography; glycolipids; glycopeptides; glycoproteins; glycosylation; method development; microarray technology; oligopeptides; oligosaccharides

DESCRIPTION (provided by applicant): Ready access to various oligosaccharides and glycopeptides is crucial for the development of glycobiology and glycomics-the system-wide study of the interactions of oligosaccharides with other biomolecules such as proteins. The long-term goal of the proposed project is to develop a new method for preparative scale syntheses of exceptionally pure oligopeptides, oligosaccharides, and glycopeptides utilizing Fluorous Technologies' proprietary tagging and purification techniques. The specific aims during Phase I of this STTR proposal are: 1) the development of fluorous-fluorenylmethoxycarbonyl (F-Fmoc) solution-phase oligopeptide synthesis (F-Fmoc Strategy); 2) the development of fluorous tag aided oligosaccharide synthesis; and 3) the development of fluorous tag aided oligosaccharide microarrays and multiwell-plate arrays. These developments will lay the foundation for the project's Phase II, which will include (1) parallel synthesis of oligosaccharide and glycopeptide libraries that have been reported to exhibit interesting biological activities such as immunogenicity against cancer cells, (2) development of automated solution-phase oligomer synthesis using a parallel synthesizer, a liquid handler, and an automated fluorous flash chromatography system, and (3) further exploration of fluorous tags for direct compound array production.

描述（由申请人提供）：随时获得各种寡糖和糖肽对于糖生物学和糖组学的发展至关重要-糖生物学和糖组学是寡糖与其他生物分子（如蛋白质）相互作用的系统研究。拟议项目的长期目标是开发一种新的方法，利用Fluorous Technologies专有的标记和纯化技术，以制备规模合成非常纯的寡肽、寡糖和糖肽。本STTR提案第I阶段的具体目标是：1）开发氟-芴甲氧羰基（F-Fmoc）液相寡肽合成（F-Fmoc策略）; 2）开发氟标签辅助的寡糖合成; 3）开发氟标签辅助的寡糖微阵列和多孔板阵列。这些进展将为该项目的第二阶段奠定基础，该阶段将包括（1）平行合成寡糖和糖肽文库，据报道，这些文库显示出有趣的生物活性，如抗癌细胞的免疫原性，（2）使用平行合成仪、液体处理器和自动化氟快速色谱系统开发自动化液相低聚物合成，和（3）进一步探索用于直接化合物阵列生产的氟标记物。

项目成果

Production of fluorous-based microarrays with uncharged carbohydrates.

使用不带电荷的碳水化合物生产基于氟的微阵列。

• DOI: 10.1007/978-1-61779-373-8_10
• 发表时间: 2012
• 期刊: Methods in molecular biology (Clifton, N.J.)
• 作者: Nagappayya,SahanaK;Pohl,NicolaLB
• 通讯作者: Pohl,NicolaLB

Mono- Vs. Di-flourous tagged Glucosamines for Iterative Oligosaccharide Synthesis.

• DOI: 10.1016/j.jfluchem.2008.05.001
• 发表时间: 2008-10
• 期刊: JOURNAL OF FLUORINE CHEMISTRY
• 影响因子: 1.9
• 作者: Park, Gisun;Ko, Kwang-Seuk;Zakharova, Aleksandra;Pohl, Nicola L.
• 通讯作者: Pohl, Nicola L.